lysosomal hydrolases of the epidermis. i. distinct glycosidases (ec 3.2) have been characterized in guinea-pig epidermis. their properties indicate them to be of lysosomal origin. the 'profile' of the epidermal glycosidases is significantly different from that reported for whole skin, the activities of beta-galactosidase and beta-acetylglucosaminidase being very high and those of the remaining enzymes relatively low in epidermis.197530
lysosomal hydrolases of the epidermis. 2. ester hydrolases.five distinct ester hydrolases (ec 3-1) have been characterized in guinea-pig epidermis. these are carboxylic esterase, acid phosphatase, pyrophosphatase, and arylsulphatase a and b. their properties are consistent with those of lysosomal enzymes.197531
proceedings: comparison of the effects of selective alpha and beta-receptor agonists on intracellular cyclic amp levels and glycogen phosphorylase activity in guinea-pig liver. 1975118
the involvement of lysophosphoglycerides in neurotransmitter release; the composition and turnover of phospholipids of synaptic vesicles of guinea-pig cerebral cortex and torpedo electric organ and the effect of stimulation.(1) crude synaptosomal fractions (p2) derived from guinea-pig cerebral cortex were incubated in the presence of 50 mm kcl in a krebs-glucose medium. torpedo marmorata electric organs were stimulated electrically in vivo at 5 pulses/sec for 30 min by electrodes placed on the electric lobe. synaptic vesicles were isolated from each source and the phospholipid compositions analysed and compared with vesicles from unstimulated controls. (2) lysophosphatidylcholine was the only lysophosphoglyceride ...1975129
further studies on the ganglionic and smooth muscle stimulating effect of potassium on the peristaltic reflex of the guinea-pig isolated ileum. 1975639
the relation between myosin adenosinetriphosphatase activity and inactivation of myosin under alkaline conditions of heart muscles in mammals of different size.atpase activity of myosin in the heart muscle of the mouse, rat, guinea-pig, rabbit and pig was studied at neutral ph and under mild alkaline conditions. at neutral ph the atpase activity of myosin is inversely related to body size of the animal species. the decrease of atpase activity of myosin after alkaline preincubation depends on the degree of atpase activity of intact myosin, i.e. myosin from the heart of the mouse exhibits high atpase activity ae same relationship was found, when comparin ...1975651
the stimulation by synaptic transmitters of the incorporation of oleate into the phospholipid of synaptic membranes.noradrenaline stimulated the incorporation of oleate into choline glycerophospholipids of guinea-pig brain synaptic membranes incubated in sodium phosphate buffer. in the presence of 1 mm-naf, noradrenaline stimulated the incorporation of oleate into the choline glycerophospholipids, phosphatidylinositol, ethanolamine glycerophospholipids, phosphatidylserine and phosphatidic acid of synaptic membranes incubated in 10 mm-tris-hcl buffer. in tris-chl containing 1 mm-naf, stimulation of incorporati ...1975993
lysosomal hydrolases of the epidermis. 3. peptide hydrolases.four distinct peptide hydrolases (ec 3-4) have been characterized in guinea-pig epidermis; these are cathepsin b1, cathepsin c, cathepsin d and arylamidase. their properties are consistent with those of lysosomal enzymes. cathepsin e was not detected.19751081
beta-adrenergic receptors in vas deferens of guineapigs. 19751343
demonstration of a nonadrenergic inhibitory nervous system in the trachea of the guinea pig.a nonadrenergic inhibitory nervous system has been demonstrated in the guinea pig trachea. electrical field stimulation of this system, in the presence of adrenergic and cholinergic blockade, resulted in relaxation of tracheal rings contracted by the mediators of immediate hypersensitivity or histamine. the relaxation was blocked by tetrodotoxin, which indicated that nerve stimulation was responsible for the relaxation. the gastrointestinal tract, which has a similar embryological origin to the ...19751437
amphetamine tachyphylaxis in the pithed guinea-pig.a single dose of (+)-amphetamine (8 mg kg-1, i.p.) administered 4 h before experimentation, reduced the pressor and positive chronotropic effects elicited by this drug (0-6 mg kg-1, i.v.) and augmented the rate of the development of tachyphylaxis to these responses in the pithed guinea-pig preparation. amphetamine pretreatment reduced the pressor and positive chronotropic effects of phenylephrine (0-1 mg kg-1, i.v.) and the positive chronotropic effects of angiotensin (30 mug kg-1, i.v.). the ra ...19751490
the effect of sulfhydryl reagents on the heart rate and coronary flow of the isolated perfused guinea-pig heart.the action of a number of compounds able to react with thiols was tested on guinea-pig hearts perfused at constant pressure. the sh reagents used were nano2, oxidized glutathione, cystamine, diamide, 1,5-difluoro-2,4-dinitrobenzene, nitroglycerol, sodium nitroferricyanide and hgcl2. 6,6'-dithiodinicotinic acid, an sh reagent that does not penetrate the cell, produced no effect. all the other sh reagents produced an increase in coronary flow. all except oxidized glutathione and nitroglycerol incr ...19752119
action of six commonly used benzodiazepines on isolated guinea-pig ileum preparation.the spasmolytic activity of six commonly used benzodiazepines was investigated on isolated guinea-pig ileum preparation. all six substances proved to be non-competitive antagonists of carbachol and barium chloride, the pd'2 values ranging between 3.23 and 4.37 in the presence of either agonist. the significance of these findings is discussed.19752123
assessment in the guinea-pig ileum and mouse vas deferens of benzomorphans which have strong antinociceptive activity but do not substitute for morphine in the dependent monkey.1 four benzomorphans which have potent antinociceptive activity in the hot-plate and writhing tests in the mouse but do not suppress or precipitate withdrawal symptoms in the morphine-dependent monkey, have been examined for their pharmacological actions in the guinea-pig ileum and mouse vas deferens. 2 in the guinea-pig ileum their agonist potencies are 1.5 to 400 times greater than that of normorphine of morphine whereas in the mouse vas deferens their potencies relative to morphine are 0.3 to ...19752359
cardiovascular and beta-adrenergic blocking effects of timolol.the haemodynamic effects of timolol and its inhibiting action on the cardiovascular and bronchial effects of isoproterenol have been studied. splanchnic nerve activity was recorded. the antiarrhythmic action of timolol was studied on guinea pig isolated atria, using arrhythmias induced by epinephrine, ouabain or coronary ligation in the dog. timolol is a very potent beta-adrenoceptor blocking agent, without specificity on beta1- or beta2-receptors. no intrinsic beta-stimulating or depressant eff ...19762481
cerebral monoamine metabolism in guinea-pigs with ascorbic acid deficiency.guinea-pigs kept on a diet deficient in vitamin c showed, after 3 weeks, a marked decrease of ascorbic acid in brain and blood leucocytes as well as of the activity of alkaline phosphatase in blood plasma. pair-fed animals did not exhibit these changes. the alpha-methyl-p-tyrosine (alpha mpt)-induced diminution of noradrenaline in the hypothalamus and the rest of the brain was attenuated in pair-fed animals, but restored in guinea-pigs deficient in ascorbic acid. the cerebral noradrenaline conte ...19752659
the evaluation of the novel pressor activity of gamma-piperidinobutyramide (wy 20051, df480).1 gamma-piperidinobutyramide (wy 20051, df480) injected intravenously evoked pressor responses in the anaesthetized ganglion blocked rat preparation over the dose range 2.4 x 10(-6)-3.0 x 10(-4) mol/kg. 2 high doses (greater than 3.8 x 10(-5) mol/kg) or even repeated submaximal doses (1.9 x 10(-5) mol/kg) of wy 20051 caused tachyphylaxis of this pressor response. 3 the noradrenaline pressor-response curve was shifted significantly to the right of the control curve following a dose of wy 20051 (1 ...19763247
ultrastructural hypoxic changes in ammon's horn and purkinje cells.guinea pigs were exposed for varying periods to different degrees of hypoxia by respiration of controlled mixtures of o2-n2 and the cns subjected to both light and electron microscopic examination after aldehyde fixation by perfusion. the subacute anoxia experiments revealed an alteration in the rough endoplasmic reticulum of the purkinje cells consisting of the formation of 'paired cisternae'. in the chronic anoxia experiments, small ultrastructural alterations of the same cells were found in a ...19763263
action of h1 and h2 inhibitors on the response of histamine sensitive adenyly cyclase from guinea-pig the guinea-pig, it has been shown that homogenates of mucosa from the fundus contain an adenylyl cyclase system that is activated by histamine as well as by prostaglandins pge1 and pga1. the effects of burimamide, an h2-inhibitor, and mepyramine and chlorpheniramide, both h1-inhibitors, were tested. both h1 and h2 inhibitors behaved kinetically as competitive inhibitors of histamine, but the km derived for burimamide (2.5 - 4.1 . 10(-5)) was significantly lower than that for either chlorpheni ...19763419
effects of aminophylline, imidazole and indomethacin on spontaneous and prostaglandin induced ovarian contractions in vitro.imidazole, acetylcholine, phenylephrine prostaglandin f2alpha, and methyl prostaglandin f2alpha increased the contractility of guinea pig and human ovaries in vitro. this effect was suppressed by aminophylline. indomethacin inhibited ovarian contractions. the inhibitory effect of indomethacin was reversed by prostaglandin f2alpha or by its methyl derivative. prostaglandin e2 decreased the amplitude and frequency of the spontaneous and prostaglandin f2alpha induced contractions of guinea pig ovar ...19753482
acid secretion by guinea-pig isolated isolated stomach preparation from the guinea-pig is described. 2. both histamine acid phosphate (1-4 mug/ml.) and theophylline hydrate (0-2-3-2 mg/ml.) separately stimulated hydrochloric acid, hcl, secretion from the guinea-pig stomach preparation. a linear dose-response relationship was obtained for theophylline. 3. addition of theophylline (0-2 and 1-6 mg/ml.) during maximal response to histamine increased the secretion further, whereas addition of histamine during maximal response to theop ...19763644
comparison of the pa2 of various beta blocking agents.the drug industry is now putting out specific beta 1 or beta 2 beta-blocking agents. the pa2 of various beta-blocking agents were determined on isolated organs-guinea pig atrium and trachea: practolol and acebutolol were considered as specific beta-1 inhibitors; butoxamine was a specific beta-2 inhibitor, while pindolol, oxprenolol, propranolol and alprenolol were specificity free. the pa2 quantifies the action exerted by an inhibitor. cardioselectivity is expressed by the pa2 left atrium/pa2 tr ...19753766
influence of industrial toxic compounds on pregnancy. vi. some tissue enzymes in pregnant guinea pigs exposed to the action of triethylenetetramine.gamma-glutamyl transpeptidase activity in kidney homogenates, aspartate and alanine aminotransferase activities in liver homogenates, and cholinesterase activity in brain homogenates were determined in nonpregnant and pregnant guinea pigs exposed to absorption through the skin of the epoxy resin triethylenetetramine. elevated activity of gamma-glutamyl transpeptidase in the kidneys of pregnant animals, and aspartate aminotransferase in the liver of nonpregnant guinea pigs were observed.19754046
proceedings: an interaction between the alpha and beta actions of catecholamines in guinea-pig liver slices. 19764183
studies on the mode of antagonism between adrenergic beta-mimetics and beta-blocking agents (ii). analysis by the uptake saturation model.curves of experimentally plotted log (dose ratio-1) vs.-log b for the antagonism between adrenergic beta-mimetics, isoproterenol (iso) and trimetoquinol (tmq), and various beta-antagonists in relaxation of guinea-pig trachea could not be reasonably fitted to schild's equation which has been commonly used in the analysis of drug-antagonism. taking into consideration the saturable uptake process of the drug used herein, the equation presented in this paper fitted fairly well to the experimental cu ...19764640
suppression of experimental allergic encephalomyelitis in guinea-pigs with poly-l-lysine.poly-l-lysin (pll) given subcutaneously in a dose of 3 mg/day suppresses experimental allergic encephalomyelitis in guinea-pigs. the suppressive effect of pll can still be demonstrated when administration is begun 8 days post-immunization. the effect is disease- and species-specific since pll (3 mg/day) does not suppress experimental allergic orchitis in guinea-pigs, nor does it suppress eae in rats (1-5 mg/day). pll (0-2 mg/day) does not decrease the severity of graft-versus-host disease (gvh) ...19755213
the in vitro effect of adrenergic agents and related compounds on triglyceride levels of guinea-pig lymphoid cells.isoproterenol, epinephrine and norepinephrine were highly potent in decreasing the triglyceride levels of the splenic lymphoid cells from guinea-pigs in vitro, while they were quite inert upon the inguinal lymph node cells.19765282
enzyme system and coenzymes involved in the energy metabolism of leukocytes. function and metabolism of polymorphonuclear neutrophils.mitochondria may be isolated from various types of leukocyte (neutrophil polymorphs and lymphocytes from human blood, neutrophil polymorphs and macrophages from peritoneal exudates of the guinea pig) after destruction by heparin of the cell membrane. this procedure is very simple and less traumatic for these subcellular structures than the usual mechanical procedures. the enzyme activities of the respiratory chain and oxygen consumption may be measured in these mitochondrial preparations. the ox ...19755934
study of the natural antihistamine-like substance in bile in mammals.a natural antihistamine substance (nas) present in bile has been investigated. it was found that the antihistamine activity was not due to proteins, lipids, pigments, or amino acids. on ion exchange chromatography and thin-layer chromatography, this activity was associated with bile acids. many bile acids could, in varying degrees, inhibit this histamine induced guinea pig ileum contraction, desoxycholic acid being the most potent. however nas activity could be separated from bile acids and thei ...19765181
protein phosphorylation in respiring slices of guinea-pig cerebral cortex. evidence for a role for noradrenaline and adenosine 3':5'-cyclic monophosphate in the increased phosphorylation observed on application of electrical pulses.1. exposure of slices of cerebral cortex from guinea pigs to electrical pulses for 10s or to noradrenaline, 5-hydroxytryptamine or histamine increases the rate of phosphorylation of unidentified proteins in the tissue; the increases in protein phosphorylation due to electrical pulses and noradrenaline were non-additive, whereas the increases due to pulses and 5-hydroxytryptamine or histamine were additive. 2. the stimulating effects of electrical pulses and noradrenaline on protein phosphorylati ...19766016
letter: synthesis of prostaglandins durin anaphlaxis in guinea pig lung. 19764856
sterol synthesis in the liver, intestine, and lung of the guinea pig.the relative rates of sterol synthesis in the liver, ileum, and lung of the guinea pig have been studied by measuring the incorporation by tissue slices of 14c-labeled acetate into digitonin-precipitable sterols. the liver showed maximum incorporation of acetate at ph 6.5, the ileum at ph 7.5, and the lung at ph 6.0. the incorporation of acetate approached the maximum rate at a concentration of 10 mm with the liver and lung and 5 mm with the ileum. using these conditions of assay, sterol synthes ...19764689
adjuvant and immunostimulating activities of water-soluble substances extracted from mycobacterium tuberculosis (var. hominis).water-soluble substances have been extracted from two strains of mycobacterium tuberculosis var. hominis: the native hydrosoluble part (polysaccharide and peptidoglycan), a substance in which the polysaccharide moiety is less abundant than in the latter, the acetylated peptidoglycan and, finally a tetrasaccharide-heptapeptide. all four types of substances, when they were injected together with freund's incomplete adjuvant, exerted an adjuvant effect on the production of delayed-type hypersensiti ...19754166
study of guinea pigs fed swiss chard grown on municipal sludge-amended soil. multi-element content of chard, field-grown on soil amended with 100 dry tons per acre of municipal sewage sludge from washington, dc, was fed to guinea pigs for 28 days. control animals were fed swiss chard grown on unfortified soi. forty-one elements were determined in the sludge, the plant material, and liver, kidney, muscle, adrenal, and spleen tissues by neutron activation and other methods. elevated concentrations of several elements found in the swiss chard grown on the sludge-soil mixture also appeared at ...19764038
use of the mouse jumping test for estimating antagonistic potencies of morphine antagonists.the potencies of 19 reference morphine antagonists have been compared in a modified version of the mouse jumping test. mice were each implanted subcutaneously with one 75 mg pellet of morphine. antagonist challenge took place 72 h later and the incidence of repetitive vertical-jumping was monitored over 1 h. a high pearson correlation coefficient (r = 0.997) was found between quantitative assays based on the total number of jumps per mouse and quantal assays based on mice jumping at least 6 time ...19766688
the effect of propranolol on sympathetic nerve stimulation in isolated vasa deferentia.(+/-)-propranolol hydrochloride (0.5 mg kg(-1) twice daily, subcutaneously, for 3 days or approximately 2.4 mg kg(-1) daily, orally, for 21 days) failed to produce ptosis or to affect responses to transmural stimulation of isolated vasa deferentia removed from treated mice. in guinea-pig isolated vasa deferentia responses to transmural stimulation through parallel electrodes were reduced by propranolol (1 to 20 mug ml(-1); blockade was concentration dependent, fast to equilibrium (45 min), easil ...19766693
the isolated cremaster muscle preparation and (external) spermatic nerve-cremaster muscle preparation of the guinea-pig.the isolated cremaster muscle preparation and spermatic nerve-cremaster muscle preparation of the guinea-pig were studied in vitro to determine their suitability as pharmacological test models. the preparation was contracted by acetylcholine, carbachol, succinylcholine and decamethonium (pd2 values, 4-2, 5-3, 7-3 and 7-4, respectively) through an action on a curare-sensitive cholinoceptor. lobeline and dmpp were ineffective. nicotine contracted the muscle, but there was tachyphylaxis. tubocurari ...19766717
mediation of prostaglandin e2 in the biphasic response to atp of the isolated tracheal muscle of guinea-pigs.atp, at a dose higher than 0-1 mug m1(-1), showed a biphasic action consisting of an initial increase followed by a gradual decrease of muscle tension in the isolated tracheal strip-chains of guinea-pigs. the pattern of this biphasic response to atp varied with the level of basal tone of the preparation at the moment of application of atp. a smiliar biphasic action was obtained by prostaglandin (pg) e2 among the various active substances studied including acetylcholine, histamine, catecholamines ...19766718
anticholinergic activity of antipsychotic drugs in relation to their extrapyramidal effects.antipsychotic drugs were evaluated with two indices of anticholinergic activity, mydriasis in mice in vivo and antagonism of carbamylcholine-induced contractions of guinea-pig tracheal strips in vitro. the drugs from most to least potent as oral mydriatic agents were mepazine, clozapine, thioridazine, promazine and chlorpromazine. trifluoperazine, pimozide and haloperidol were inactive. these results were consistent with the hypothesis that anticholinergic activity of antipsychotic drugs is inve ...19766720
the assay of the agonist activities of n-methyl- and n-nor-homologues of morphine derivatives by the guinea-pig ileum method. 19766730
preliminary investigations of the metabolism and pharmacological activity of beta-hydroxytryptamines in mammals.beta-hydroxytryptamine and beta-hydroxy-5-hydroxytryptamine were incubated with rat liver slices and oxidative deamination was established as the main route of metabolism: in both instances the corresponding indole-3-glycollic acids and indole-3-ethane diols were the major metabolites. however, the rates of deamination of beta-hydroxylated tryptamines, as measured manometrically, were found to be much slower than those of tryptamines nonhydroxylated in the side chain. the pharmacological activit ...19766751
an in vitro method for the study of beta-receptor mediated effects on slow contracting skeletal muscle.the soleus muscle of a guinea-pig was dissected out under pentobarbitone anaesthesia and mounted on a holder in an organ bath containing krebs solution. the tendon was attached to a force transducer and subtetanic contractions were evoked by electrical field stimulation (0.5 ms pulses at 10-12 hz for 1.5 or 3 s every 22 s). the experiments were performed at 37 degrees. terbutaline, a selective agonist at beta2-adrenoceptors, reduced the force of subtetanic contractions in a dose-dependent manner ...19766753
the effect of imipramine on isolated innervated guinea pig and rat urinary bladder preparations. 19766760
the effects of metoclopramide in modifying the response of isolated guinea-pig ileum to various agonists.metoclopramide has a dual effect on intestinal smooth muscle. low concentrations of metoclopramide cause potentiation of the responses to substance p, acetylcholine, histamine and barium chloride on the guinea-pig ileum. higher concentrations produce a depression of smooth muscle responses which is characteristic of the tertiary amine local anesthetics. neural pathways are involved in the mechanism of potentiation, since the enhancement of the responses to the agonists is abolished by tetrodotox ...19766787
a tentative transmission mechanism for the twitch elicited in guinea-pig vas deferens by field stimulation.the twitch response to nerve activity in the vas deferens does not behave as if it were adrenergic since it is enhanced by adrenoceptor blockers and often inhibited by noradrenaline and other sympathomimieic amines. potassium (k+) ions have a strong reinforcing action on the twitch and easily restore it after blockade by lanthanum. the hypothesis is advanced that k+ ions have a transmitter function in the vas deferens and that k+ ions released in conjunction with the nerve stimulus may reach a c ...19756863
species and phenobarbitone-induced differences in the kinetic constants of liver microsomal harmine o-demethylation.1. the apparent kinetic constants for the o-demethylation of harmine to harmol by 10 000 g supernatant fractions from livers of mice, rats, guinea-pigs, rabbits, cats and cows have been determined. the km values were 10-39 mum and vmax 0-25 and 1-65 nmol/mg protein/min. 2. optimal conditions of incubation time and nadp requirements differed between species. in all species except cat and cow the rate of o-demethylation of harmine was linear for 5 min, but in the latter species was linear for 15 m ...19767043
regulation of tyrosine hydroxylase activity by prostaglandin e1 in guinea pig adrenal gland.the action of prostaglandin e1 on tyrosine hydroxylase activity in adrenal slices of guinea pig was studied. the activity of tyrosine hydroxylase and was decreased by the incubation of adrenal slices with prostaglandin e1 at concentrations beyond 2 mug per ml for 2 hours. the activity of tyrosine hydroxylase was stimulated by dibutyryl adenosine 3',5'-monophosphate in slices of guinea pig adrenal glands. incubation of adrenal slices wtth the combination of pge1 and dbc-amp lead to a tyrosine hyd ...19753675
further observations on the properties of serum and tissue guanase from man and some animal species. optimum ph and activation energy in the presence of 8-azaguanine.the activation energy and the optimum ph of guanine deaminase in man, the rat, guinea pig and mouse were studied using 8-azaguanine as a substrate. the serum guanase in man and in all the animal species studied differs in activation energy from the guanase of the liver. in man, moreover, the serum guanase is also different from the brain and kidney enzyme. in the rat and guinea pig the brain enzyme has thermic activation energy different from the liver and kidney enzyme. the guanase of the serum ...19767449
studies on mode of antagonism between adrenergic beta-mimetics and beta-blocking agents (i). beta-blocking action of mescaline and its order to clarify whether or not trimetoquinol (tmq) and isoproterenol (iso) interact with the same receptor, the pa2 values of propranolol (pr) and certain trimethoxybenzene derivatives were measured, using isolated guinea pig tracheal chains. each of pr, mescaline (mes) and its derivatives gave almost the same pa2 values for tmq and iso. introduction of an alkyl group into the n atom of mes increased the affinity to the receptor in the order of methyl and isopropyl as well as the structureac ...19753674
potential histamine h2-receptor antagonists. 3. methylhistamines.syntheses are described for all the mono- and some di- and trimethylhistamines. new methods are given for the known npi, ntau-, nalpha-, 2-, and 4-methylhistamines and for the novel compounds, beta-methyl-, 4,nalpha-dimethyl-, and 4,nalpha,nalpha-trimethylhistamines. agonist activities are reported for stimulation of histamine h1 (guinea-pig ileum) and h2 (rat gastric acid secretion) receptors. h2-receptor agonist activities indicate that a methyl group is more readily accommodated at the 4 and ...19767675
properties of lysosomes in guinea pig heart: subcellular distribution and in vitro stability. 19767679
inactivation of viruses in serum with binary ethyleneimine.the inactivation os six strains from three different groups of viruses with 0.001 m binary ethyleneimine at 37 c proceeded at the same rate in either bovine serum or cell culture medium. the inactivant did not impair the growth-promoting capacity of bovine serum used in cell culture, nor did it affect the antibody activity of guinea pig hyperimmune serum.19763517
effect of beta-adrenoceptor stimulators, papaverine and theophylline on guinea-pig trachea contracted by different drugs. 19767916
consumption of complement in chelated and nonchelated guinea pig serum after challenge with some viral and nonviral interferon inducers.the consumption of complement observed during the induction of interferon by various inducers may proceed via the alternate pathway. the alternate pathway requires the presence of mg ions in the medium while ca ions may be absent.19767949
inhibition by suprofen and other non-narcotic analgesic drugs of the effects of prostaglandin precursor on isolated tissues and platelets.contractions caused by slow reacting substance c(srs-c) and by arachidonic acid hydroperoxide (aap) in the guinea-pig ileum and by aap in the rat fundus were studied in the presence of suprofen and of 3 reference compounds. the dose-related inhibitions were not due to antagonism of prostaglandins. other agonists of gastrointestinal smooth muscle were not or only weakly antagonized. for the study of selective inhibition of aap-induced contractions by non-narcotic analgesics, the rat fundus is the ...19768022
general pharmacological properties of a new non-opiate antitussive: zipeprol (3024 cerm). i. action on respiratory function and acute toxicity.1-(2-methoxy-2-phenyl)-ethyl-4-(2-hydroxy-3-methoxy-3-phenyl)-propyl-iperazine-dihydrochloride (zipeprol, respilene) is a substance of non-phenanthrenic chemical structure. in the cat, it antagonised cough induced by stimulation of the superior laryngeal nerve or by direct mechanical excitation of the sensitive tracheo-bronchial receptors. the efficacy of zipeprol after enteral administration made it possible both to establish good intestinal absorption and to rank it favourably in relation to s ...19768057
isolation of intact megakaryocytes from guinea pig femoral marrow. successful harvest made possible with inhibitions of platelet aggregation; enrichment achieved with a two-step separation technique.methods have been devised to harvest megakaryocytes from guinea pig femoral marrow and to isolate them in high yield. when marrow tissue was disaggregated the megakaryocytes underwent degenerative changes characterized by the loss of cytoplasmic granules and alterations in membrane topography, similar to the changes seen in aggregating platelets. these morphologic changes were interpreted to mean that megakaryocytes possessed functional attributes of platelets. the use of agents which inhibit pl ...19763509
isolation and properties of 2 kallikreins from human saliva.two kallikreins (k-i and k-ii) were purified from mixed, parotid and submandibular human saliva. the kallikreins were separated by chromatography on cm-cellulose. the ph optima of activity were at ph 9.3 and ph 9.6-9.8; km for baee was 1.10-3m and 4.10-3m, respectively. the esterase activity of k-i and k-ii was inhibited by trasylol-like inhibitors, while the plant and synthetic inhibitors of trypsin were uneffective. in dog, rabbit and rat the hypotensive effect of k-ii and its action upon the ...19753025
immediate hypersensitivity in the guinea pig conjunctiva. ii. effect of treatment with antihistamines, steroids and disodium cromoglycate.the effects of antihistamines, steroids and disodium cromoglycate on an immediate hypersensitivity reaction in the guinea pig eye are described in terms of clinical observations, histological examinations of sections of eyes and cytological studies of material from the conjunctival surface. the use of brushes to sample the cells on the conjunctival surface is described. the effect of repeated daily challenges on the reaction is also reported.19762864
studies on the activities of peptidases from human leucocytes, and human and guinea pig alveolar macrophages (author's transl).peptidases activities were compared in human leucocytes, guinea pig and human alveolar macrophages. seversl endo- and exopeptides were characterized; some of them were active at acid ph and others at neutral and alkaline ph. leucocytes and alveolar macrophages had proteolygic activity for hemoglobin, fibrinogen, collagen and elastin. using synthetic substrates, several enzymes were characterized: arylamidase, aminopeptidase, carboxypeptidases a and b and cathepsins a and c. the enzymatic activit ...19762398
properties of a toxin from the sea anemone stoichacis helianthus, including specific binding to sphingomyelin.stoichactis helianthus toxin, a protein derived presumably from the nematocysts, was purified to homogeneity. it has a molecular weight of about 16,000, an isoelectric ph of 9.8, and it contains approximately 3.7% carbohydrate. it is powerfully hemolytic for erythrocytes derived from a variety of animal species, those of the cat being the most sensitive and those of the guinea pig the most resistant. the toxin is lytic also for rabbit blood platelets, and it destroys cultured fibroblasts but is ...19761757
proceedings: effects of sympathomimetic amines and ouabain on potassium influx in guinea-pig liver slices. 19768635
evidences for alpha excitatory action of catecholamines on the electrical activity of the guinea-pig stomach.effects of catecholamines and their inhibitors on the electrical activity of the smooth muscle of the guinea-pig stomach were studied by using pressure electrodes. the spontaneous electrical activity of antrum and corpus preparations consisted of slow waves with or without superimposed spikes. in quiescent fundus preparations, the spike activity and slow waves were generated by tea. catecholamines (noradrenaline, isoprenaline and adrenaline) suppressed or blocked the spike discharges and the gen ...19768660
studies on the mechanism of the action of morphine on the peristalsis of guinea pig ileum in situ.the influence of some drugs on the effect of morphine on the threshold pressure required to elicit peristalsis in the guinea pig ileum in situ was studied, in order to test the hypothesis that this effect of morphine is mediated by catecholamine release. tachyphylaxis to this effect of morphine was confirmed. pretreatemnt with two 8 mg/kg doses of reserpine, 24 and 48 hrs before the experiment, significantly reduced the effect of morphine on the pressure threshold. the i.v. administration of 10 ...19751686
non-adrenergic inhibition of the electrical activity of the antrum muscle fibers of the guinea-pig stomach.the changes in the electrical activity of the antrum muscle fibers of the guinea pig stomach caused by atp and its related compounds were compared with those caused by catecholamines. the antrum preparation exhibited spontaneous electrical activity and this was suppressed or inhibited by treatment with catecholamines (adrenaline, noradrenaline and isoprenaline). the inhibitory actions of catecholamines were observed in the presence of tetrodotoxin or alpha-blockers (phentolamine or phenoxybenzam ...19768859
conformationally restricted analogs of histamine h1 receptor antagonists: trans and cis-1-benzyl-3-dimethylamino-6-phenylpiperidine.the syntheses of trans- and cis-1-benzyl-3-dimethylamino-6-phenylpiperidine (1 and 2) are described. compounds 1 and 2 were found to be inhibitors to histamine, acetylcholine, and barium chloride induced contractions of the isolated guinea pig ileum. compounds 1 and 2 do not exhibit appreciable stereoselectivity in their ability to inhibit smooth muscle contractions. the cis compound 2 is a more effective inhibitor of histamine n-methyltransferase than the trans isomer 1.19761535
on the pharmacology of 9,10-dihydro-10-(1-methyl-4-piperidylidene)-9-anthrol (wa 335), a histamine and serotonin antagonist (author's transl).the substance 9,10-dihydro-10-(1-methyl-4-piperidylidene)-9-anthrol (wa 335) was examined for its antagonistic effects against histamine and serotonin, for its atropine-like properties as well as for a series of other qualities in comparison with cyproheptadine and pimethixene. the anti-histamine and anti-serotonin activities of compound wa 335 on the smooth muscle and the capillary do not only exceed that of cyproheptadine but also that of pimethixene. wa 335 shows an extremely strong binding t ...19751049
sympathomimetic-induced effects in the soleus muscle of the guinea-pig.sympathomimetic amines reduced the peak tension, time to peak and time to half-relaxation of indirectly elicited twitches of the guinea-pig soleus muscle in vivo. clonic contractions of the soleus muscle were depressed by the amines. on a molar basis salbutamol and orciprenaline were 5.12 and 80.0 times less potent than (+/-)-isoprenaline in producing these effects. results obtained with the beta-receptor antagonists propranolol, practolol and h35/25 suggest that the depression in skeletal muscl ...19769032
electrophysiologically determined quinidine-like actions of a beta-adrenergic blocking agent, 1-(7-indenyloxy)-3-isopropylaminopropane-2-ol hydrochloride (yb-2).since 1-(7-indenyloxy)-3-isopropylaminopropane-2-ol hydrochloride (yb-2) has been reported to be a potent beta-adrenergic blocking agent with antiarrhythmic effects, the electrophysiological effects of this compound on guinea-pig and canine heart muscle were examined. yb-2 was found to have typical quinidine-like actions such as decrease in rate of rise of the action potential, prolongation of refractory period and decrease in conduction velocity.19769035
specificity and inhibition of gamma-glutamyl transpeptidase in guinea pig intestines.gamma-glutamyl transpeptidase activity in guinea pig intestine was tested toward 8 monoglutamyl and 4 diglutamyl substrates. distinct differences in specificity and activity related to ontogenetic development were noted. a mixture of l-serine and borate inhibited specifically gamma-glutamyl transpeptidase activity of homogenates and accumulation of naphthylamine and 14c-substances in slices of intestine incubated with gamma-l-14c-glutamyl-alpha-naphthylamide. the same mixture, administered per o ...19769046
species differences in the conjugation of 4-hydroxy-3-methoxyphenylethanol with glucuronic acid and sulphuric acid.the biosynthesis of the glucuronide and sulphate conjugates of 4-hydroxy-3-methoxyphenylethanol was demonstrated in vitro by using the high-speed supernatant and microsomal fractions of liver respectively. these two conjugates were also produced simultaneously by using the post-mitochondrial fraction of rat, rabbit or guinea-pig liver. in contrast only the glucuronide was synthesized by human liver and only the sulphate by mouse and cat livers. neither of these conjugates was formed by the kidne ...19769078
biochemical and biophysical changes in guinea pigs after acute head injury.animal experiments were set up mainly to derive additional diagnostic data from the study of biochemical changes after acute head injury. in standardized experiments guinea pigs were subjected in groups of 20 to three identical head injuries, each of either 1.0 j or 1.5 j intensity. the trauma was likely to result in a concussion or contusion syndrome similar to that found in man; 40 animals served as controls. during the 60 min after injury observation and measurement of body functions did not ...1975749
effect of antihistamine-antiserotonin and ganglionic blocking agents upon increased capillary permeability following burn trauma.tiny (0.2% tbs), partial thickness, non-contact radiant heat burns in guinea pigs resulted, within 3 hours, in significant edema formation and protein leakage at the site of the injury. areas of skin distant to the burn also showed an increase in water content but no protein leakage. pretreatment of the animals with either chlorisondamine hydrochloride or a mixture of methysergide and chlorpheniramine significantly decreased postburn edema formation and protein leakage. liquid emulsion autoradio ...1975515
the detection of toxin production by corynebacterium diphtheriae in diagnostic vitro tests for assessing the toxigenicity of strains of c. diphtheriae using the original agar plate precipitin method of elek are unreliable. at high concentrations of antitoxin (500-1000 u/ml) multiple non-specific precipitin lines occur making interpretation difficult. increased specificity was obtained by diluting the antitoxin but this in turn caused a delay in the appearance of toxin-antitoxin lines. also, the failure of lines to appear on media enriched with unsuitable serum may lead ...19769614
soldado virus from ornithodoros (alectorobius) maritimus (ixodoidea: argasidae) infesting herring gull nests on puffin island, northern wales.three strains of soldado (sol) virus (hughes serogroup) were isolated from nymphal and adult ornithodoros (alectorobius) maritimus vermeil et marguet collected in and near nests of the herring gull, larus a. argentatus pontoppidan, on puffin island, northern wales. reciprocal complement fixation (cf) titration results demonstrated recovered virus strains to be sol virus and antigenically distinct from other hughes serogroup members. all isolates killed mice and guinea pigs, and 1-2 day old domes ...19769805
in vitro antagonism of the mediators of allergy by a benzopyrano-benzopyran carboxylic acid was tested on isolated guinea pig ileum and rat stomach strips for activity against mediators probably released after allergen antibody union. it antagonized the response produced by histamine, bradykinin, serotonin, prostaglandin e2, prostaglandin f2alpha and slow-reacting substance of anaphylaxis (srs-a). the concentrations which blocked 50% of the response were 150, 145, 92, 70, 47, and 32 mug/ml, respectively. this compound may be useful in the treatment of allergic conditions.1975336
the contribution of extraneuronal uptake to the trachea-blood vessel selectivity of beta-adrenoceptor stimulants in vitro in guinea-pigs.1 the potencies relative to isoprenaline of isoetharine, tertiary butyl noradrenaline, salbutamol, orciprenaline, me 506, rimiterol, fenoterol, carbuterol and terbutaline on isolated preparations of guinea-pig trachea and blood vessels (perfused hind limb) were determined. all the compounds were selective for trachea and selectivity values, i.e. relative potency on trachea divided by relative potency on hind limb, ranged from 2.3 to 21.4. 2 responses to isoprenaline (the reference compound), ter ...197610029
adrenoreceptors of the guinea-pig urinary bladder.1 adrenaline, noradrenaline and isoprenaline (5 mug/ml) did not affect the resting tone of the isolated urinary bladder of the guinea-pig. 2 the catecholamines (1-2 mug/ml) inhibited neuronally evoked contractions at various stimulation frequencies; the inhibition was maximum at 2 hz and minimum at 50 hz. isoprenaline produced maximum inhibition. 3 propranolol (0.5 mug/ml) completely blocked the catecholamine-induced inhibition at all the frequencies employed. the concentration-response curves o ...197610034
phospholipase a2 as a probe of phospholipid distribution in erythrocyte membranes. factors influencing the apparent specificity of the reaction.the action of snake venom phospholipases a2 in intact human erythrocytes was investigated in detail. the basis phospholipase from agkistrodon halys blomhifii was found to induce both hydrolysis of membrane phospholipids and total cell hemolysis under certain experimental conditions. the hydrolytic action of the basic enzyme was found to consist of two sequential events: (a) hydrolysis of 70% of the total cell ph osphatidylcholine without any evident hemolysis; and (b) complete hydrolysis of the ...197554
lipoperoxidation rates and drug-oxidizing enzyme activities in the liver and placenta of some mammal species during the perinatal period.lipoperoxidation and drug-metabolizing enzymes were measured in livers and placentas of different mammal species during the perinatal perios. in placentas and fetal livers of rat, rabbit and guinea-pig, cofactor-supported lipoperoxidation was negligible, as were the activities of drug-oxidizing enzymes. human fetal liver contained an intact drug-oxidizing electron transport chain, and lipoperoxidation activity was accordingly abserved. it is suggested that lesions mediated by lipoperoxidation ma ...197610178
lipid biosynthesis in liver slices of the foetal guinea pig.lipid synthesis as measured by the incorporation of acetate or 3h2o into slices of foetal liver, is much higher than in slices of adult liver and shows a peak at about two-thirds of gestation. at this time the synthesis from glucose was low and reached a peak 10 days later. the changes in the activity of atp citrate lyase, which mirrored acetate incorporation, and the effect of glucose and pyruvate on acetate corporation into lipid suggests that some of the lipid synthesis occurs via intramitoch ...19766015
changes in contractility and calcium binding of guinea pig taenia coli by treatment with enzymes which hydrolyze sialic acid.the effects of neuraminidase and phospholipase c on the contractility and the ca++ -binding of guinea pig taenia coli were investigated. potassium contracture or histamine-induced contracture of taenia coli was inhibited by treatment with neuraminidase, though acetylcholine-induced contracture was not. treatment with phospholipase c markedly inhibited the contracture induced by isotonic potassium, histamine or acetylcholine. by treatment with neuraminidase for 4 hr, about 40 mumol/100 mg wer wt ...19755622
pharmacological studies with adenine, adenosine and some phosphorylated derivatives on guinea-pig tracheal muscle.adenine, adenosine and three adenine nucleotides all caused relaxation of the guinea-pig trachea. the relaxation to the nucleotides was often preceded by a contraction. the response to adenosine and the nucleotides, but not adenine, was potentiated by dipyridamole. imidazole inhibited the response to adenine alone. propranolol has no effect on the response to any of the compounds. it is concluded that the guinea-pig trachea does not possess and a nucleotide-specific receptor as has been postulat ...197610367
influence of various substances on prostaglandin biosynthesis by guinea-pig chopped lung.guinea-pig chopped lung tissue was used to investigate the inhibitory effect of various steroidal and non-steroidal anti-inflammatory agents, antipyretics, analgesics, local anaesthetics and psychotropic drugs on mechanically induced release of prostaglandin-like material. low concentrations of non-steroidal anti-inflammatory agents inhibited synthesis, but other antipyretics and analgesics, and the local anaesthetics had little effect. thymoleptics, neuroleptics and monoamine oxidase inhibitors ...197610390
metabolic n-oxidation of atropine, hyoscine and the corresponding nor-alkaloids by guinea-pig liver microsomal preparations.incubation of guinea-pig liver microsomal preparations with atropine or hyoscine resulted in the formation of the corresponding nor-alkaloids and both isomers of atropine n-oxide from atropine and one isomer of hyoscine n-oxide from hyoscine. separate incubations of guinea-pig liver microsomal preparations with nor-atropine and nor-hyoscine yielded the corresponding hydroxylamines. the n-oxide and hydroxylamine metabolites were identified by comparison of their t.l.c. behavior and m.x. with prep ...197610391
loperamide binding to opiate receptor sites of brain and myenteric plexus.loperamide, a new antidiarrheal agent, was tested to determine whether its biological activity involves binding to opiate receptor sites. loperamide and morphine competitively inhibited 3h-naloxone binding to homogenates a guinea-pig brain and myenteric plexus. the kp values obtain in the presence of na+ were: morphine, 9.60-10(-9) m (brain), 1.66-10(-7) m (myenteric plexus); loperamide, 7.20-10(-9) m (brain), 1.33-10(-7) m (myenteric plexus); naloxone, 4.78-10(-10) m (brain), 1.27-10(-9) m (mye ...197610422
a test for antinociceptive activity of narcotic and narcotic antagonist analgesics in the guinea pig.ethylenediamine tetraacetic acid (edta) was used as a nociceptive stimulus intradermally in the guinea pig. the responses evoked by edta included vocalization, biting and scratching at the site of injection and escape behavior. nociception by edta was shown to be the result of its cation chelating activity. the suppression of edta-induced responses proved to be a rapid and effective antinociceptive test. the narcotic analgesics morphine, codeine, meperidine and methadone and the narcotic antagon ...19765596
isoproterenol antagonism of cardioselective beta adrenergic receptor blocking agents: a comparative study of human and guinea-pig cardiac and bronchial beta adrenergic receptors.pa2 values against isoproterenol were determined for a number of cardioselective and noncardioselective beta adrenergic receptor blocking agents using human and guinea-pig isolated atrial and bronchial or tracheal preparations to study possible species differences. no significant differences in pa2 values for propranolol, pindolol, ro 3-4787, acebutolol, atenolol, practolol, metoprolol, h 87/07 and tolamolol on bronchial or tracheal beta adrenergic receptors of both species were found. with resp ...197610427
the binding of complement by complexes formed between a rabbit antibody and oligosaccharides of increasing size.immune complexes formed between a homogeneous rabbit antibody to type iii pneumococcal polysaccharide and a series of oligosaccharides of varying size derived from it were prepared and tested for their ability to fix guinea pig hemolytic complement. antibody and either tetra-, hexa-, or octasaccharide formed only monomeric antibody-hapten complexes and did not show any complement binding. a dodecasaccharide and a 16-sugar residues oligomer formed dimer and trimer immune complexes. these complexe ...19765560
studies on the mode of antagonism between adrenergic beta-mimetics and beta-blocking agents (iii). functional antagonism between beta-mimetics and equations which can explain the following characteristic phenomena in the functional antagonism between isoproterenol (iso) and spasmogens in guinea-pig trachea are proposed: (1) the amplitude of relaxation of the muscle induced by iso varied depending on the concentration of a spasmogen used (histamine or carbachol). (2) the dose-response curves for the relaxation by iso shifted to the right in a parallel manner as the concentration of the spasmogen increased, and became stationary at high ...197610457
cardiac histamine receptors.current evidence pertinent to the identification of cardiac histamine receptors in the guinea pig is reviewed. pharmacological characterization has been aided by the use of selective agonists and antagonists for both types of histamine receptors. it appears that both h1 and h2 receptors mediate the cardiac effects of histamine. histamine h2 receptors mediate the positive chronotropic and ventricular inotropic effects. h1 receptors mediate the negative dromotropic effect of histamine and possibly ...19765315
cyproheptadine as an inhibitor of the effects of bradykinin.a study was made of the influence of ciproheptadin, serotonin and histamine inhibitor, on the effects of exo- and endogenous bradykinin. ciproheptadin inhibited the effect of bradykinin on a section of a guinea pig intestine in vitro, eliminated the hypotensive effect of bradykinin in rats in vivo, and also blocked the constriction of the vessels of the ear in rabbit and a fall of the blood kininogen level caused by the administration of pyrogenal.19756095
choline acetyltransferase, glutamate decarboxylase and tyrosine hydroxylase in the cochlea and cochlear nucleus of the guinea pig.activities of choline acetyltransferase (chac), glutamate decarboxylase (gad) and tyrosine hydroxylase (th), enzymes catalyzing the synthesis of acetylcholine (ach), gamma-aminobutyric acid (gaba) and catecholamines, respectively, were measured in the cochlea and cochlear nucleus of the guinea pig. chac activity in the organ of corti, third turn, was 1270 pmole ach formed/min/mg protein (chac, 1270) and was higher than in turn 4 (chac, 543). chac activity was higher when the preparation included ...19766125
experimental study of the sensitizing properties of halothane.the sensitizing properties of halothane were investigated experimentally in guinea pigs using two different techniques. the first method, derived from that of draize, included a sensitizing phase in which the product was administered by inhalation, while the second method, derived from that of magnusson and kligman, used guinea pigs sensitized to freund's adjuvant and which were sensitized to halothane administered subcutaneously. the results obtained in these two series of experiments appeared ...197610781
experimental study of conjugates of a catabolite common to halothane, enflurane and fluroxene in guinea pigs.the authors sensitized guinea pigs to a halothane catabolite, trifluoroacetic acid, combined with guinea pig albumin. they then exposed the animals to halothane. there was no correlation between the presence of humoral and cell-mediated immune reactions obtained with the catabolite and the incidence of liver necrosis.197610782
influence of adrenaline, dibenamine and dopamine on acidosis, hemoconcentration and lethality in protracted anaphylactic shock of guinea-pigs.protracted anaphylactic shock of guinea-pigs was accompanied by a marked decrease in blood ph, and an increase in hematocrit. death ensued in 58.3% of the animals within 3 hr of observation. infusion of adrenaline (20 mug/kg/min), after eliciting anaphylaxis, intensified the acidosis, and increased the lethality to 100%. pretreatment with dibenamine (5 mg/kg) reversed the effect of adrenaline. dopamine, infused in amounts of 200 mug/kg/min, acted similarly to the combination dibenamine/adrenalin ...197610865
guanylate cyclase. subcellular distribution in cardiac muscle, skeletal muscle, cerebral cortex and liver.1. guanylate cyclase of every fraction studied showed an absolute requirement for mn2+ ions for optimal activity; with mg2+ or ca2+ reaction was barely detectable. triton x-100 stimulated the particulate enzyme much more than the supernatant enzyme and solubilized the particulate-enzyme activity. 2. substantial amounts of guanylate cyclase were recovered with the washed particulate fractions of cardiac muscle (63-98%), skeletal muscle (77-93%), cerebral cortex (62-88%) and liver (60-75%) of vari ...197610890
adenylate cyclase, guanylate cyclase and cyclic nucleotide phosphodiesterases of guinea-pig cardiac sarcolemma.1. the activities of the enzymes involved in the metabolism of cyclic nucleotides were studied in sarcolemma prepared front guinea-pig heart ventricle; the enzyme activities reported here were linear under the assay conditions. 2. adenylate cyclase was maximally activated by 3mm-naf; naf increased the km for atp (from 0.042 to 0.19 mm) but decreased the ka for mg2+ (from 2.33 to 0.9 mm). in the presence of saturating mg2+ (15 mm), mn2+ enhanced adenylate cyclase, whereas co2+ was inhibitory. bet ...197610895
esterase and protease activity of purified guinea pig basophil granules. 197610900
solubilization, partial purification and radioassay for the intrinsic factor receptor from the ileal mucosa.a macromolecule which binds intrinsic factor saturated with vitamin b12 has been solubilized from the guinea-pig ileum by homogenization followed by mechanical disruption without organic solvents or detergents. this intrinsic factor 'receptor' was further purified by precipitation with 30% saturated ammonium sulphate, centrifugation at 105000 g, and filtration through sephadex g-200. failure to precipitate the receptor following centrifugation at 105000 g for 3 h and filtration of the receptor w ...197610957
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