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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
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
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
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
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
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
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
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
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
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
study of guinea pigs fed swiss chard grown on municipal sludge-amended soil. multi-element content of tissues.swiss 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
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
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
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
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
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
letter: synthesis of prostaglandins durin anaphlaxis in guinea pig lung. 19764856
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
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
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
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
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
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
further studies on the ganglionic and smooth muscle stimulating effect of potassium on the peristaltic reflex of the guinea-pig isolated ileum. 1975639
in vitro antagonism of the mediators of allergy by a benzopyrano-benzopyran carboxylic acid pr-d-92-ea.pr-d-92-ea 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
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
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
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
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
lysosomal hydrolases of the epidermis. i. glycosidases.seven 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
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
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
studies on mode of antagonism between adrenergic beta-mimetics and beta-blocking agents (i). beta-blocking action of mescaline and its derivatives.in 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
acid secretion by guinea-pig isolated stomach.an 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
action of h1 and h2 inhibitors on the response of histamine sensitive adenyly cyclase from guinea-pig mucosa.in 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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
blockade of histamine-induced contractions of guinea pig ielum by beta-haloalkylamines.in the longitudinal muscle strip of guinea pig ileum phenoxybenzamine (pob) produces a maximum parallel shift of 0.7 log units in the dose-response curve to histamine. in the presence of sodium thiosulfate in the wash fluid the parallel shift whith retention of maximum response increases to about 2 log units, and a similar value is obtained for nethyl-n-(2-bromoethyl)-1-naphthylamine. the the agent n-ethyl-n- (2-chloroethyl)benzylamine produces a significantly smaller shift of dose-response curv ...19768204
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
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
degradation of gastrin by gastric mucosal cells.specific binding of radiolabeled gastrin by gastric mucosal cells prepared from guinea pigs was detected and examined. specific cell binding of gastrin was found to be both ph and temperature dependent. maximum binding of radiolabeled gastrin by gastric mucosal cells was demonstrated at ph 7.4 and at 4 degrees c. substantial degradation of 125i-gastrin occurred during incubation with gastric mucosal cells. gastrin degradation was detected both by loss of immunological reactivity with antibodies ...19768573
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
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
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
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
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
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
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
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
the effects of acidosis and alkalosis on coronary flow and cardiac nucleotide metabolism.the changes of the coronary flows and of the cardiac nucleotide metabolism during acidosis and during alkalosis were studied in 50 perfused guinea pig hearts with and without hypoxia. at ph 7.0 the coronary flows increased, and at ph 7.8 a significant reduction of the flows took place. at 20% o2, acidosis elicited a further flow increase, whereas alkalosis inhibited the flow increase produced by hyoxia. the increases after adenosine injections and after coronary occlusions were greater during ac ...19767231
manganese-dependent nadph oxidation by granulocyte particles. the role of superoxide and the nonphysiological nature of the manganese requirement.recent work has indicated that superoxide is involved in the manganese-stimulated oxidation of nadph by crude granule preparations of guinea pig neutrophils. the characteristics of a model manganese-requiring nadph-oxidizing system that employs a defined o2-generator have now been compared to the original neutrophil-granule system. with respect to ph dependence, cyanide sensitivity, and reduced pyridine nucleotide specificity, the properties of the two systems are very similar. additional inform ...19767574
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 microsomal enzyme systems that reduce n-hydroxyphentermine.the reduction of n-hydroxyphentermine was studied in liver microsomes isolated from rat, guinea pig, and rabbit. the reduction requires a nadph-generating system and was inhibited by oxygen and carbon monoxide. in the rat, the reduction was increased by phenobarbital pretreatment. kinetic analysis of the reductase activity in rat liver microsomes suggests that the reduction of the hydroxylamine is mediated by at least two enzyme systems, one of which is a co-sensitive system inducible by phenoba ...197610142
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
properties of lysosomes in guinea pig heart: subcellular distribution and in vitro stability. 19767679
desensitization of guinea pig tracheal muscle preparation to beta-adrenergic stimulants by a preceding exposure to a high dose of catecholamines.when a given concentration of a catecholamine was applied to guinea pig tracheal preparation contracted by 20 mum histamine or by 30 mm-k+-tyrode's solution, constant relaxations were observed, if the relaxation was submaximal. when a high concentration of catecholamine, 200 times the ed50, was once applied, subsequent responses to beta-stimulants (ed80) was reduced by about 30-40%, in spite of repeated washings. the response was gradually recovered in 2 hr. thus 45 mum epinephrine and 1 mum iso ...19767695
effect of beta-adrenoceptor stimulators, papaverine and theophylline on guinea-pig trachea contracted by different drugs. 19767916
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
effect of oleic acid on the activity of soluble hexokinase from guinea pig brain. 19768193
contractile activity of the oviduct and the mesosalpinx isolated from guinea pigs in different phases of the sex cycle. effects of several pharmacological influences. 19768393
a new model for antisperm autoimmunity in guine pigs.adult outbread male guinea pigs were autoimmunized without adjuvant. homogenates were prepared with one of their own testes previously submitted "in vivo" and "in vitro" to thermal injury. animals received a single or daily repeated intradermal injection without added adjuvant, in one or different skin sites. guinea pigs daily sensitized in the same site during 30 days showed the presence of: a) dermal granuloma at the site of injection; b) several foci of typical allergic orchitis; c) delayed h ...19768395
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
sympathomimetic amines having a carbostyril nucleus.a series of new sympathomimetic amines containing an 8-hydroxycarbostyril moiety was synthesized. these compounds probably exist as resonance hybrids having two acidic hydrogen atoms in locations approximating to those of the hydroxyl groups of catechol-containing adrenergic agents. in an in vitro test, many of these compounds showed potent activity for relaxation of guinea pig tracheal smooth muscle. one of the compounds was 24 000 times more potent than isoproterenol. their actions on cardiac ...197610441
studies on the mode of antagonism between adrenergic beta-mimetics and beta-blocking agents (iii). functional antagonism between beta-mimetics and spasmogens.new 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
effect of psychotropic and anticonvulsive preparations on transport atpase in the renal tubules of the guinea pig.the effect of 4 groups of medicamentous agents, viz. neoruleptics, tricyclic antidepressants, somnifacients and antiepileptics - on the activity of the transport atpase and p-nitrophenylphosphatase from the renal tubules of the guinea pig was studied. used in high concentrations neuroleptics suppress almost completely the activity of the enzyme, but in small doses influence but little that of the p-nitrophenylphosphatase. the butyrophenone derivatives have a mild effect upon the activity of the ...19756303
immunological mechanisms in aspirin hypersensitivity. studies on the immunogenicity of free aspirin.anti-aspiryl antibodies were produced in rabbits and guinea pigs by inoculation of aspirin incorporated in complete or incomplete freund's adjuvant. these antibodies were readily detected by passive haemagglutination using rabbit erythrocytes incubated with aspirin at alkaline ph. aspiryl conjugates with ovalbumin, human gamma-globulin, bovine gamma-globulin and rabbit serum were also prepared by incubating the proteins with aspirin at alkaline ph. aspiryl conjugates prepared by this technique b ...197610712
effect of insulin on mitochondrial oxidative phosphorylation and energy charge of the perfused guinea pig liver.the effect of insulin was investigated in the isolated guinea pig liver perfused with krebs-ringer bicarbonate buffer containing red blood cells and albumin. in the mitochondria isolated from livers perfused with 10 units of insulin per hour, the phosphorylative activity with glutamate as a substrate increased to about 160 per cent of control 60 minutes after the beginning of perfusion (p less than 0.01). such an enhanced phosphorylative activity was accompanied by increases in the respiratory c ...19766601
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
physiology of the oviduct and mesosalpinx isolated from guinea pigs. influence of pharmacological factors. 19758954
nutritional deficiency, immunologic function, and disease.several experiments conducted by our group over a period of 6 years have shown that nutritional stress, especially protein and/or calorie deprivation, leads to many, often dramatic, changes in the immune responses of mice, rats, and guinea pigs. chronic protein deprivation (cpd) has been shown to create an enhancing effect on the cell-mediated immune responses of these animals. humoral responses under cpd conditions were most often found to be depressed, but sometimes were unaffected, depending ...19768988
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
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
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
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