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adrenergic agents. 4. substituted phenoxypropanolamine derivatives as potential beta-adrenergic agonists.a series of 1-(substituted phenoxy)-3-(tert-butylamino)-2-propanols in which the ring substituents were 3,4-dihydroxy (6f), 3- and 4-hydroxy (6g and 6h, respectively), 3-hydroxy-4-methylsulfonamido (6i), its 3,4-transposed isomer (6j), and 4-methylsulfonylmethyl (6k) was prepared and examined for beta-adrenergic agonist and/or antagonist properties. two of these compounds, 6f and 6j, were potent beta-adrenoreceptor agonists in in vitro tests that measure a compound's ability to relax guinea pig ...197716136
na+-k+-atpase inhibition stimulates pge release in guinea pig taenia coli.inhibition of the plasma membrane enzyme na+-k+-atpase by ouabain zero extracellular k+, or low extracellular na+, markedly augmented prostaglandin e release from the guinea pig taenia coli. data suggest this phenomenon may be linked directly to na+-k+-atpase or na+ pump activities, or changes in intracellular k+ concentration. the augmented prostaglandin e release was not due to changes in intracellular na+, ca2+, ph, or membrane potential, resulting from na+ pump inhibition. the characteristic ...197716497
the splitting of sperm heads from tails in eight mammalian species and the measurement of their sizes.ejaculated spermatozoa from man, the euopean wild boar and the bull, and spermatozoa from the cauda epididymes of the rabbit, rat, mouse, hamster and guinea pig were treated with a sonic bath, a sonic probe, trypsin with and without prior treatment with a sulphhydryl reagent, pronase and alkalis. the fragments produced were counted and sized in an accurately calibrated coulter counter, model zb industrial, before and after zaponin treatment to lyse accompanying debris and the peripheral cytoplas ...197716511
glucuronide conjugation of 6-n-propyl-2-thiouracil and other antithyroid drugs by guinea pig liver microsomes in vitro. 197716610
the effect of birth on the maturation of hepatic cytochrome(s) p-450 mono-oxygenase and tyrosine aminotransferase activities in the guinea pig.mixed coat guinea pigs delivered by cesarian section 5 days before term were compared to spontaneously delivered full-term animals with respect to the postnatal maturation of hepatic mono-oxygenase activity in vitro toward aniline and p-chloro-n-methylaniline. tyrosine aminotransferase acitivity was studied in the same preparations as a positive control for birth-related phenomena. mono-oxygenase activities toward both sustrates increased significantly in both premature and full-term animals dur ...197716670
the energy metabolism of the leukocyte. ix. changes in the concentration of the coenzymes nad, nadh, nadp, and nadph in polymorphonuclear leukocytes during phagocytosis of staphylococcus albus and due to the action of phospholipase c.the determination of the coenzymes nad+, nadh, nadp+ and nadph, by the use of a method of enzymatic cycling, demonstrates that the enzymes responsible for the stimulations found during the phagocytosis of staphylococcus albus are nadh and nadph oxidase of human leukocytes and nadph oxidase in the case of guinea pig leukocytes. the effects of serum, of the bacterial strain used and of phospholipase c are also discussed.197716747
specific metabolic pathway in vitro of pinazepam and diazepam by liver microsomal enzymes of different animal species.the metabolic pathway of pinazepam and diazepam in vitro was studied with rat, guinea pig and dog liver microsomes using a chromatographic and spectrophotometric technique. two main pathways were observed, n1-dealkylation and c3-hydroxylation. n1-dealkylation was shown to be the predominant reaction for pinazepam in all the animal species studied, while c3-hydroxylation was the major metabolic pathway for diazepam in the rat. no oxazepam was found when pinazepam and diazepam were incubated with ...197716776
amine binding sites in acyl intermediates of transglutaminases. human blood plasma enzyme (activated coagulation factor xiii) and guinea pig liver enzyme. 197716916
descending release of acetylcholine from the locally distended guinea pig ileum.the effects of local distension of the intestinal wall on the release of acetylcholine (ach) from the adjacent non-distended part were studied with the segment os isolated guinea pig ileum. local distension of the intestinal wall induced the increased release of ach in the distended part and in its anal side but not in its oral side. such aboral release of ach by local distension was abolished by tetrodotoxin or atropine in the concentrations which did not block the release in the distended part ...197717026
subcellular compartmentation of creatine kinase isoenzymes in guinea pig heart.in an attempt to determine whether a subcellular compartmentation of creatine kinase exists and if so, whether there is a different distribution of the 3 isoenzymes of ck in the cell, studies were carried out with the guinea pig heart which had been subfractionated by either isopycnic density gradient centrifugation or differential pelleting. isoenzyme analysis of ck in the isolated subcellular fractions by electrophoresis on agarose gels, revealed that the mm isoenzyme occurred in the cytosol, ...197717468
the effect of toxin ii isolated from sea anemones (anemonia sulcata) on the isolated guinea pig ileum.when the guinea-pig isolated ileum is treated with the toxin ii from anemonia sulcata, it releases not only acetylcholine but also serotonin. these transmitters are both involved in the spasmogenic action of the toxin.197717477
glucuronidation and deglucuronidation reactions in hepatic and extrahepatic tissues during perinatal development.the relative activities of uridine diphosphoglucuronyltransferase (udpgt) and beta-glucuronidase (betag) were measured during perinatal development of hepatic and extrahepatic tissues to determine the balance between glucuronidation and deglucuronidation reactions at different developmental stages. liver, lung, kidney, intestine, and placenta were studied in guinea pigs and rabbits. in general, betag activities exceeded those of udpgt in fetal tissues, whereas the converse was evident in adults. ...197717527
o-sulfonation of n-hydroxy-2-fluorenylacetamide and 7-hydroxy-n-2-fluorenylacetamide in fetal and placental tissues of humans and guinea pigs. 197717528
in vitro pharmacology of the opioid peptides, enkephalins and endorphins.in the guinea-pig ileum methionine-enkephalin, normorphine and morphine are equipotent in depressing electrically evoked contractions; leucine-enkephalin has about 25% of the activity. the mouse vas deferens is more sensitive to the enkephalins which are 30 to 60 times more potent than morphine. fragments of beta-lipotropin61-91 (beta-endorphin) having sequences up to lph76 are more potent in the mouse vas deferens than in the guinea-pig ileum but beta-endorphin is about equipotent in the two pr ...197717538
the effects of prostaglandins e1, e2, f1alpha and f2alpha on guinea-pig ileal and colonic peristalis.prostaglandins (pge1, e2, f1alpha and f2alpha) have been tested on the peristaltic reflex in isolated segments of guinea-pig ileum and colon using simultaneous recordings of fluid propulsion and longitudinal and circular muscle activity. propulsion and circular muscle peristaltic activity were increased by serosally applied pgf compounds in the ileum and pge or pgf compounds in the colon following initial contraction of the longitudinal muscle. this is consistent with a role for prostaglandins i ...197717690
further observations on an ether-o-oxidase, formerly called alkyl etherase, from liver tissue.1. the microsomal enzyme from liver previously called an "etherase" is now described more accurately as an ether-o-oxidase. it has been investigated further to free it from the membranes in aqueous solution and to try to define its physiological substrate. 2. after a variety of attempts with detergents, etc., the enzyme was obtained in impure solution from precipitation with 35-45% (nh4)2so4 solution after a short digestion at room temperature. 3. when a suitably reinforced the enzyme in solutio ...197717745
synthesis and biological evaluation of a tetrahydroisoquinoline derivative possessing selective beta2-adrenergic agonist activity.this paper reports the synthesis of 4-(3,4,5-trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline (2) and 2-(3,4-dihydroxyphenyl)-3-(3,4,5-trimethoxyphenyl)propylamine (3). the biological activity of these agents relative to that of trimetoquinol (1) in guinea pig atria and guinea pig trachea is reported. the relative activities in relaxation of guinea pig trachea is 1 greater than 2 greater than 3 while in the chronotropic response in guinea pig atria the relative order of activity is ...197717750
effects of cimetidine, a histamine h2-receptor antagonist, on various experimental gastric and duodenal ulcers.the effects of cimetidine, a new histamine h2-receptor antagonist, on the development of experimental gastric and duodenal ulcers were studied. it was found that either by the oral, intraduodenal, or intraperitoneal route this agent had a marked inhibitory activity on stress-, aspirin-, indomethacin-, or histamine-induced gastric ulcers in rats and guinea pigs. the effects of cimetidine on stress-, aspirin-, and indomethacin-induced gastric ulcers were dose-dependent in many cases. pylorus-ligat ...197718007
some aspects of the trachea-heart selectivity of rimiterol in vitro and in vivo in guinea-pigs. 197718120
purification and properties of a new testosterone 17beta-dehydrogenase (nadp+) from guinea-pig liver.as a result of studies of guinea-pig live testosterone 17beta-dehydrogenase (nadp+) (ec 1.1.1.64), a new testosterone 17beta-dehydrogenase was discovered. the new enzyme was purified to a single homogeneous protein from the 105 000 g-supernatant fraction of guinea-pig liver by (nh4)2so4 fractional precipitation and two gel-filtration stages, deae-cellulose column chromatography and hydroxyapatite column chromatography. it was characterized by many properties. the enzyme has almost the same prope ...197718133
biochemical characterization of alkaline phosphatase in guinea pig thymus.1. alkaline phosphatase (orthophosphoric-monoester phosphohydrolase (alkaline optimum), ec 3.1.3.1) in guinea pig thymus was extracted optimally in 10 mm tris - hcl buffer at ph 8.0 containing 5 g/l triton x-100. 2. alpha-glycerophosphate, beta-glycerophosphate and phenolphthalein monophosphate were hydrolyzed by thymus extract with a ph optimum at 9.8-10.0, whereas p-nitrophenylphosphate and alpha-naphthylphosphate were hydrolyzed with ph optima at 10.7-10.8 and beta-naphthylphosphate at ph 11. ...197718186
the use of functional antagonism to determine whether beta-adrenoceptor agonists must have a lower efficacy than isoprenaline to be trachea-atria selective in vitro in guinea-pigs.1 the relative efficacies of three trachea-atria selective beta-adrenoceptor agonists, fenoterol, me 506 and me 454, compared to isoprenaline, were determined on both trachea and atria of guinea-pigs. 2 on tracheal preparations the beta-adrenoceptor agonists were used as functional antagonists of carbachol and a comparison of the maximum shifts in the carbachol concentration-response line produced by each of the beta-adrenoceptor agonists provided a comparison of their efficacies. 3 on atrial pr ...197718249
telemetry of the tissue ph value under the effect of local anesthetics. preliminary report.after discussing the problems involved in in vivo ph measurements, ph telemetry is presented as a new method. long-term in vivo measurements of the ph are intended to be performed by means of a miniature transmitter implanted into the subcutaneous tissue of guinea pigs.197718331
inter-relationships between proton electrochemical gradient, adenine-nucleotide phosphorylation potential and respiration, during substrate-level and oxidative phosphorylation by mitochondria from brown adipose tissue of cold-adapted guinea-pigs. 197718347
differences in pulmonary and cardiovascular beta receptors in the guinea pig and rabbit.an in vivo preparation, in which a body plethysmograph was incorporated, was useful in monitoring the cardiopulmonary effects of pharmacological agents in the guinea pig and rabbit. isoproterenol, given 30 seconds prior to histamine challenge, reproducibly blocked histamine-induced dynamic compliance decreases and increased heart in the artificially ventilated guinea pig. these effects were used to separate the activity of beta adrenergic blockers on airway and heart muscle. dose-response data w ...197718599
a comparative study of the effects of opc-1085 and propranolol on isolated guinea pig atrium.effects of a newly synthesized beta-blocker, 5-(3-tert-butylamino-2-hydroxy) propoxy-3,4-dihydrocarbostyril (opc-1085) were compared with those of propranolol. opc-1085 had a potency about 3 times greater than that of propranolol in blocking the positive inotropic and chronotropic effects of isoprenaline on the isolated guinea pig atrium. at a concentration of over 3 x 10(-5) m opc-1085 produced negative inotropic and chronotropic effects. however, these effects were about 10 times weaker than t ...197718629
beta-adrenoceptors in the guinea pig treated with egg-albumin. 197718633
analysis of antibody response and immunoglobulins in sera of rabbits and guinea pigs immunized with coxiella burnetii.rabbit and guinea pig sera and their immunoglobulin fractions (igm and igg) were examined by complement-fixation (cf), microagglutination (ma), opsonization-phagocytosis (op) and serum protection (sp) tests at intervals after immunization with live phase i and phase ii coxiella burnetii suspensions. in general, ma antibodies, but also decreased, earlier than cf antibodies. the anamnestic immune response was higher with lower primary doses. both phase ii and phase i cf and ma antibodies as well a ...197718924
comparative toxicities of enflurane, fluroxene and nitrous oxide at subanaesthetic concentrations in laboratory animals.we compared the toxicities of subanesthetic concentrations of fluroxene, enflurane and nitrous oxide in mice, rats and guinea pigs which were in an active growth phase. fluroxene produced a greater mortality and decrement in weight gain than enflurane and nitrous oxide despite administration of far lower concentrations. enflurane, 0.1 mac, resulted in a detrimental effect on weight and early mortality in mice but not in rats or guinea pigs. nitrous oxide, 0.1 mac, resulted in only a minor effect ...197719138
studies on the glucuronidation of 7-hydroxychlorpromazine in vitro.the glucuronide of 7-hydroxychlorpromazine (cpoh), formed by incubation with hepatic microsomes and udp-u-14cglucuronic acid, was isolated by extraction into 1-butanol at ph 1 and assayed by liquid scintillation counting. although concentrations of cpoh greater than 3 x 10(-4) m stimulated its conjugation, the apparent km of the transferase in microsomes from guinea pig liver for cpoh was 9.5 x 10(-5) m. the apparent activation of glucuronyltransferase by high concentrations of cpoh was prevente ...197719219
the effective proton conductance of the inner membrane of mitochondria from brown adipose tissue. dependency on proton electrochemical potential gradient.the nucleotide-sensitive h+ (oh-) conducting pathway of mitochondria from the brown-adipose tissue of cold-adapted guinea-pigs passes an effective proton current which is directly proportional to the proton electrochemical gradient. at 23 degrees c and ph 7.0 this conductance is 16 nmol h+ - min-1 - mg-1 - mv-1. addition of 0.2 mm gdp results in a conductance which is linear and low (0.7 nmol h+ - min-1 - mg-1 - mv-1) until deltamicronh+ exceeds 220 mv. at higher values of deltamicronh+, which c ...197719250
pd2-, pa2- and pd2'-values of a series of compounds in a histaminic and a cholinergic system.(1) affinity and intrinsic activity values of 75 compounds for a histaminergic and a cholinergic system are presented. the quantitative correlations between the affinity values of 35 compounds and some physicochemical constants (van der waals volume, lipophilicity, number of hydrogen atoms on the protonated amine) are discussed. (2) absence of systematic differences between pd2 and pa2 of partial agonists supports the assumption that these values are equivalent expressions of the same affinity. ...197719265
modification of the action of pentagastrin on acid secretion by botulinum toxin.i.v botulinum toxin after 60-90 min abolished the dose-response relationship between pentagastrin and gastric acid secretion in anesthetized rats and guinea-pigs. the toxin reduced but did not abolish the acid stimulatory effect of histamine. as expected, the acid response to vagal stimulation was abolished and that to methacholine in rats was unaltered by the toxin.197719277
the effect of ion pair formation on the antimuscarinic activity of methantheline.the quaternary ammonium compound, methantheline, was found to antagonize acetylcholine induced contractions in isolated guinea pig ileum by a mechanism which did not conform to the criteria for either competitive or non-competitive inhibition. enhancement of the lipid solubility of methantheline by formation of an ion pair with trichloracetate failed to influence its cholinergic inhibitory activity. the results suggest that in the guinea pig ileum a) an intracellular site of action does not exis ...197719279
effects of alpha- and beta-adrenergic blockers on the actions of noradrenaline on body temperature in the newborn guinea-pig.the effect of na injected into the lateral cerebral ventricle on tc was blocked by alpha-adrenergic receptor blockers, but not by beta-receptor blockers, whereas the effect of systemically administered na was blocked by i.p. administered beta-receptor blockers, but not by alpha-blockers.197719282
collagenase of human skin basal cell epithelioma.collagenase of human basal cell epithelioma was purified by sequential ammonium sulfate precipitation, sephadex gel filtration and affinity chromatography on collagen-polyacrylamide gel. the collagenase, when partially purified, was found to have an approximate molecular weight of 50,000. the purified enzyme contained no caseinolytic activity. on polyacrylamide gel electrophoresis, the purified enzyme gave a single protein band. the purified collagenase cleaved native acid-soluble guinea pig ski ...197719452
metabolic oxidation of aralkyl oximes to nitro compounds by fortified 9000g liver supernatants from various species.incubation of 'amphetamine oxime' (iia, anti-benzyl methyl ketoxime) with fortified rabbit liver 9000 g supernatants gave the nitro compound (ie) and the beta-hydroxylated oxime (iic) in addition to the previously reported ketone (iib) and alcohol (ic) metabolites. formation of the products was cofactor dependent. the nitro compound was also formed using mouse, hamster and guinea-pig 9000 g liver supernatants and to a minor extent by rat liver. the oximes of 2-phenethylamine (iie) and norfenflur ...197719580
the effects of diethylcarbamazine citrate on smooth muscle.the effect of the anthelmintic drug diethylcarbamazine citrate (decc) was examined on the guinea-pig isolated ileum, rabbit duodenum, chick oesophagus, rat portal vein and pig coronary artery. decc contracted all the gastrointestinal smooth muscle preparations. the contractions were antagonized by hexamethonium and atropine but they were not affected by mepyramine or methysergide in concentrations that abolished, or markedly reduced, responses to histamine and 5-hydroxytryptamine. decc inhibited ...197719582
enhancement by physalaemin of the contractions induced by cholinomimetics in the guinea-pig ileum. 197719590
an in vivo assay for the analysis of the biological potency and structure-activity relationships of narcotics: serum testosterone depletion in the male rat.an in vivo method for the assessment of the agonistic-antagonistic activities and structure-activity relationships of the narcotics is described. the method, which is based on the depletion of serum testosterone levels by the narcotics in the male, satisfies all of the criteria necessary for a valid narcotic assay: 1) the ability of the narcotics to deplete serum testosterone levels is stereospecific; 2) naloxone competitively inhibits their effects; 3) and the relative potencies of the drugs in ...197719620
adrenergic agents. 6. synthesis and potential beta-adrenergic agonist activity of some meta-substituted p-hydroxyphenylethanolamines related to salbutamol.salbutamol, an adrenergic receptor agonist with selectivity for tracheobronchial vs. cardiac muscle, differs from the catecholamine n-tert-butylnorepinephrine in that it bears a hydroxymethyl, rather than a phenolic, group in the meta position. in a search for new bronchodilating agents with minimal cardiovascular side effects, a series of derivatives, in which this m-hydroxymethyl group is modified, was prepared. these compounds were examined for potential bronchodilator activity in an in vitro ...197719629
the alpha-action of catecholamines on the guinea-pig taenia coli in k-free and na-free solution and in the presence of ouabain. 197719746
calcium requirement for the alpha-action of catecholamines on guinea-pig taenia coli. 197719747
action of fazadine bromide in the preparation of the ductus-deferens-hypogastric nerve of the guinea pig. 197720064
studies on the antigenicity of an inactivated, aluminum hydroxide adjuvant equine influenza vaccine.an inactivated, aluminum hydroxide adjuvant equine influenza vaccine was tested in horses and guinea pigs to determine the levels of antigen that would elicit maximum serological responses. vaccine containing serial twofold increments of a/equi-1/prague and a/equi-2/miami strains of equine influenza virus was administered to random groupings of both types of test animals. the hemagglutination inhibition antibody response for each group was then measured. results in horses and guinea pigs were co ...197720211
soterenol and related compounds: molecular modifications and changes in selectivity, affinity and efficacy at beta-adrenoreceptors in guinea-pig atria and trachea. 197720258
the stimulatory effect of morphine on metabolism of naloxone to 6alpha-naloxol in the guinea pig. 197720294
the interaction of 1-(2(diarylmethoxy)ethyl)aziridines with histamine receptors in the longitudinal muscle strip of the guinea pig ileum.the time course of the onset and decline of histamine antagonism by 1-(2-(diarylmethoxy)ethyl)aziridines, compounds which could be expected to have h1-receptor alkylating properties, was investigated on the longitudinal muscle strip of the guinea pig ileum. experiments were performed with normal preparations and with muscle strips pretreated with a prostaglandin synthesis inhibitor in order to prevent spontaneous rise of muscle tone. in contrast to the previously reported observation that antihi ...197720314
long-term experiments on toleration of the ganglionic blockader hygronium.in tests set up on albino rats, guinea pigs and rabbits the chronic toxicity of hygronium--a new original ganglion blocking agent of a short-term action was studied. with its daily intraperitoneal administration for 14 days in doses of 10 and 40 mg/kg (1/10 and 1/3 dl50) the drug produces in some of the animals, chiefly in rabbits and guinea pigs receiving 40 mg/kg, readily reversible histological changes in some of their internal organs. hygronium does not cause any local irritating effect197720328
drug effects on blood pressure and heart rate in unanesthetized animals. (1). effects of beta-blocking agents (author's transl).beta-blocking actions of orally administered kö 1400 and tiprenolol, new beta-blocking agents, were studied in unanesthetized rats and dogs, using a fall of blood pressure and an increase in heart rate produced by isoproterenol as a measure of beta-receptor activation. blood pressure was recorded from the aorta of the dog and the caudal artery of rat via indwelling catheter, and heart rate of the dog was recorded by a cardiotachometer triggered by r waves of the lead ii electrocardiogram. mean r ...197720392
phenothiazine phototoxicity: toxic chlorpromazine photoproducts.the effect of preirradiated chlorpromazine (cpz) solutions has been studied in vivo in the guinea pig and in vitro in a yeast culture. with intracutaneous administration of cpz solutions preirradiated with long-wave ultraviolet radiation (uva), an inflammatory response was attained equaling the response achieved when nonirradiated solutions were injected and the skin of the animals was subsequently irradiated with uva. preirradiated cpz was not toxic to the yeast culture. during irradiation the ...197720478
adrenerigic agents. 7.1 synthesis and beta-adrenergic agonist activity of several 2-pyridylethanolamines.in a search for new selective bronchodilators, three 2-pyridylethanolamines, i.e., 2-tert-butylamino-1-(5-hydroxy-2-pyridyl)ethanol (2b), a related 6-methylsulfonylmethyl (2c), and, a 6-methyl (2d) derivative, were prepared. these compounds were examined for potential bronchodilator activity in an in vitro test for relaxation of guinea pig tracheal tissue. potential cardiac stimulant activity was evaluated in vitro by measuring changes in the rate of spontaneously beating guinea pig right atrial ...197720503
adrenergic agents. 8.1 synthesis and beta-adrenergic agonist activity of some 3-tert-butylamino-2-(substituted phenyl)-1-propanols.replacement of the benzylic hydroxyl group of n-tert-butylnorepinephrine with a hydroxymethyl substituent affords a propanolamine homologue which retains a high degree of beta-adrenergic agonist activity. as modification of the meta substituent of catecholic ethanolamines, such as n-tert-butylnorepinephrine, often provides compounds that exert a more pronounced effect in relaxing tracheobronchial smooth muscle (beta2-adrenergic agonist) than in stimulating cardiac muscle (beta1-adrenergic respon ...197720504
pharmacological studies with beta-adrenoreceptor blocking agents i. effect on the smooth muscle of the taenia coli of the guinea pig. 197720544
antimuscarinic properties of antidepressants: dibenzepin (noveril).the antimuscarinic potency of dibenzepin (noveril) was estimated by measuring (a) central in vivo effects in mice (antihypothermia and antitremor, both induced by oxotremorine), (b) peripheral in vivo activity (mydriasis caused by systemic administration of the drug), (c) the effects of dibenzepin on isolated smooth muscle from guinea pig ileum, and (d) in vitro determination of the affinity constant of dibezepine toward the muscarinic binding sites in whole mouse-brain homogenate. the data allo ...197720647
some effects of crude venom from the cones conus striatus and conus magus on isolated guinea-pig atria. 197720679
long-term cultivation of cells derived from guinea pig tongue. 197720772
catalytic formation of epsilon-(gamma-glutamyl)lysine in guinea pig liver transglutaminase. 197720879
effect of tyrosine ionization upon biological activities of angiotensin ii and two new peptide analogues.the role of the tyrosine side-chain in the smooth muscle contracting activity of angiotensin iii was investigated by determining intrinsic activities and ed50 values of 4-(3-chlorotyrosine)angiotensin ii and 4-(3-benzyltyrosine)angiotensin ii in the isolated guinea-pig ileum and rat uterus. 4-(3-chlorotyrosine)angiotensin ii activity was compared with that of angiotensin ii at different ph values, in which the ratio of their degrees of phenolic ionization varied. the results indicated that depro ...197720979
enumeration of t rosette-forming cell population in rabbit peripheral blood using human, sheep, guinea-pig, rat, mouse and chicken red blood cells under different experimental conditions.attempts were made to estimate peripheral t-lymphocytes in rabbits by their ability to form rosettes with sheep, human, guinea-pig, rat, mouse and chicken rbc. the reaction was studied under different conditions of ph and temperature. the test was also carried out in the presence or absence of glutaraldehyde. with sheep rbc, lymphocytes from 2 of the 5 rabbits studied formed rosettes to the extent of 1.5% in the system containing glutaraldehyde. these results however were not reproducible when s ...197721220
evidence from agonist and antagonist studies to suggest that the beta1-adrenoceptors subserving the positive inotropic and chronotropic responses of the heart do not belong to two separate subgroups.the positive inotropic and chronotropic responses of guinea-pig isolated left and right atria to 17 sympathomimetic amines were examined under conditions selected to control the pharmacological environment. each agonist was compared with (--)-isoprenaline as the reference by constructing dose-response curves. equiactive molar concentration ratios relative to (--)-isoprenaline were calculated at the ec50 for rate and tension responses. statistical analysis revealed that (--)-noradrenaline and (+/ ...197721238
effects of dantrolene sodium on isolated skeletal, smooth and cardiac muscle of the guinea-pig. 197721244
effect of tazolol on beta-adrenoceptors in isolated preparations of the guinea-pig and rat. 197721245
influence of pyridylisatogen tosylate on contractions produced by atp and by purinergic stimulation in the terminal ileum of the guinea-pig.2-2'pyridylisatogen tosylate (pit), which antagonizes the inhibitory action of atp in the taenia caeci, did not antagonize the excitatory effects of exogenous atp and of purinergic stimulation of the terminal guinea-pig ileum. pit (0-5--2-5 mum) potentiated the atp-induced contractions and also the contractions produced by potassium chloride, though the potentiation could not be related to the dose in every experiment. the responses to noradrenaline, adrenaline and histamine were slightly inhibi ...197721258
analysis of the beta-receptor mediated effect on slow-contracting skeletal muscle in vitro.subtetanic contractions of the guinea-pig isolated soleus, a slow-contracting skeletal muscle, were evoked by transmural field-stimulation. isoprenaline caused a dose-dependent depression of the contractions. this effect was inhibited by propranolol and h 35/25 (1-(p-tolyl-2-isopropylamino-1-propanol) but not by practolol. similar results were obtained for terbutaline. tazolol and h 80/62 (1-isopropylamino-3-(p-hydroxyphenoxy)-2-propanol (hcl), selective beta1-agonists, had no effect per se but ...197721260
synthesis of 1-substituted analogues of trimetoquinol possessing differential and selective beta-adrenergic properties.the synthesis of the 1,1-disubstituted tetrahydroisoquinoline analogues, 1-methyl-1-(3,4,5-trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (2) and 1-benzyl-1-(3,4,5-trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (3), is described. the profile of beta-adrenergic activity for these analogues was determined and compared to that of trimetoquinol (1) in isolated guinea pig atrial, tracheal, and rat adipocyte preparations. unexpected selective ...197721293
confirmation of conductance increase by adrenalin in the guinea-pig taenia coli (alpha-action). 197721402
potentiation of beta-sympathomimetics with alpha-adrenoceptor blocking drugs in guinea pig trachea and human bronchus preparations.the actions of beta-sympathomimetics alone and in various combinations with alpha-adrenoceptor blocking agents were studied in guinea pig tracheal chain and in some preparations of human bronchi taken in operations. all the alpha-adrenoceptor blockers caused 50-100% potentiation of the effects of the beta-sympathomimetics studied in both preparations, had no effects of their own in the rather low concentrations used (10(-10) --10(-6) mol/l). the results show that guinea pig and human tracheobron ...197721422
sensitization of contracted tracheal smooth muscle to beta-adrenergic spasmolysis by subthreshold doses of papaverine.in certain cases beta-adrenergic substances cause little or no relaxation of tracheal or bronchiolar smooth muscles contracted by spasmogenic mediators. this phenomenon is explained on the basis of the model of functional antagonism, with the suppositions that the spasmogenic system has a reserve and the spasmogen concentrations are much higher than the concentration which would cause a just-maximal contraction. if this is correct, the model predicts that it should be possible to restore the eff ...197721448
role of autoimmune processes in the pathogenesis of post-vaccinal lesions of the nervous system.subcutaneous sensitization of guinea pigs with -vaccine, and also an intracardiac injection of smallpox or measles vaccine induced production of brain autoantibodies, whereas subcutaneous or intradermal immunization of the animals with liver viral vaccines was not accompanied by the formation of autoantibodies and development of the pathological processes in the nervous system tissue. tthe greatest changes in the brain tissue in the form of circulatory disturbances and inflammatory-dystrophic ph ...197721500
on the presence of myocardial alpha-adrenoceptors in the atrium of the guinea pig. 197721635
phagocytic release of lysosomal enzymes from guinea pig neutrophils--regulation by corticosteroids, autonomic neurohormones and cyclic nucleotides. 197721664
effect of dihydroergotoxine on activities of beta-receptor stimulators.the effect of dihydroergotoxine (det), an alpha-receptor blocker, on the bronchodilating effect of various beta-receptor stimulators was examined using the isolated guinea-pig tracheal smooth muscle. relaxation of isolated guinea-pig tracheal smooth muscle with isoproterenol hydrochloride, salbutamol hemisulfate and clorprenaline hydrochloride, was markedly increased by continous infusion of det. this result may suggest that det, an alpha-receptor blocker, can be used together with bronchodilato ...197721668
rabbit liver transglutaminase: physical, chemical, and catalytic properties.transglutaminase (r-glutaminyl-peptide:amine alpha-glutamyl-yltransferase ec 2.3.2.13) has been purified to apparent homogeneity from extracts of rabbit liver. the enzyme is a single polypeptide chain of approximately 80 000 molecular weight containing one catalytic site per molecule. that the isolated enzyme is the rabbit counterpart of the well-characterized guinea pig liver transglutaminase is evidenced by the similarities in their amino acid compositions and in their enzymic activities towar ...197721685
action of toxins isolated from scorpion and sea anemone venoms on ileum isolated from reserpine-treated guinea pigs.we have shown that the ileum isolated from a reserpinized guinea pig does respond to toxin ii obtained from scorpion venom but does not react to anemonia sulcata toxin. we conclude that if acetylcholine is the neurotransmitter inducing pharmacological activity of scorpion toxin it is serotonin which triggers activity of anemonia sulcata toxin in ileum of a normal guinea pig.197721755
comparative metabolism of four allylic barbiturates and hexobarbital by the rat and guinea pig.a method for the extraction and identification of urinary metabolites of allylic barbiturates by gas chromatography and mass spectrometry is described. the metabolites from rat and guinea pig urine were extracted and separated into two fractions (an acidic and a nonacidic fraction) by chromatography on deae-sephadex before converted into suitable derivatives for gas phase analysis. n,n'-dimethyl derivatives were used except in cases where metabolic n-demethylation was possible, in which case n-e ...197721777
pharmacologic studies on w10,294a, a new bronchodilator.w10,294a (1,2,3,4-tetrahydro-8,9-dimethoxy-3(2-piperidinoethyl)-5h-1 benzopyrano 3,4-c pyridin-5-one dihydrochloride) is a potent antagonist of the bronchoconstriction induced by histamine, methacholine or acetylcholine. in vitro evaluation on guinea pig trachea indicated that w10,294a had both direct smooth muscle relaxant activity and modest antihistaminic properties. resistance and dynamic compliance measurements in anesthetized dogs indicated that w10,294a prevented or reversed bronchoconstr ...197721958
cause of decrease of ethylmorphine n-demethylase activity of lipid peroxidation in microsomes from the rat, guinea pig and rabbit.there were marked differences among animal species between nadph-dependent and ascorbic acid-fe++-dependent lipid peroxidation. in nadph-dependent lipid peroxidation, this activity occurred to the greatest extent in rats followed by guinea pigs and rabbits and such was much lower in rabbits than in guinea pigs. on the other hand, rabbit microsomes exhibited higher lipid peroxidation activity than guinea pigs in ascorbic acid plus fe++ or fe++-dependent lipid peroxidation although the activity wa ...197721981
dualist or pseudo-dualist interactions of mepyramine, diphenhydramine and eprozinol with histamine at h1-receptors.the types of interaction of mepyramine (m), diphenhydramin: (d) and eprozinol (e), with histamine h1-receptors of guinea pig ileal and tracheal smooth muscle, were comparatively studied in vitro. according to the concentrations used, all three substances showed an apparent dualist mechanism of action on both preparations when histamine (dihydrochloride) was used as the agonist. the competitive component of this mechanism (at low concentrations) was characterized by the following pa2 values: 9.01 ...197721982
fungal proteases and the mammalian kinin system: i. brinolase-catalyzed kinin formation and s2160 hydrolysis.brinolase, a fungal protease advocated for thrombolytic therapy, released kinin peptides from semi-purified kininogens of the human, rabbit, guinea pig, and mouse, and moreover cleaved an arginyl bond of the chromogenic peptide s2160. its kinetics demonstrated marked differences from the mammalian protease trypsin. whereas trypsin liberated 100% of the available kinin in 30 min at ph 8, brinolase generated a maximum of only 22% under optimal conditions, viz. incubation of 5 microgram/ml enzyme a ...197722111
massive occurrence of rickettsiae of the spotted fever group in fowl tampan, argas persicus, in the armenian s.s.r.fowl tampans (argas persicus) collected in oktemberyan in the armenian s.s.r. in 1974 were found to be massively infected with rickettsiae of the spotted fever (sf) group. one isolated rickettsial strain, designated armenia 9, is antigenically related to, and probably identical with, strain armenia 11 and strain b of rickettsia slovaca, isolated from dermacentor marginatus ticks. strain armenia 9 grows readily in chick embryo yolk sacs and in chick embryo cell (cec) and l-cell cultures. it cause ...197722239
some biological properties of an endotoxic lipopolysaccharide from the typhus group rickettsiae.a lipophilic thermostable lipopolysaccharide (lps) complex was isolated by phenol extraction from purified suspensions of the typhus group rickettsiae. the lps complex is antigenic and possesses some endotoxic properties such as toxicity for actinomycin d-treated mice, pyrogenicity for rabbits and guinea pigs, ability to elicit hypothermia in white rats and local schwartzman reaction and active cutaneous anaphylaxis in rabbits.197722240
investigation of the bronchoconstriction induced by beta-adrenoceptor blocking drugs in guinea-pigs and rats proceeding. 197722371
neurotransmitter-sensitive adenylate cyclase in the hypothalami of guinea-pig, rat and monkey. 197722390
ph effect on the percutaneous penetration of lignocaine hydrochloride.(1) the percutaneous penetration of lignocaine hydrochloride is affected in vitro by the ph; alkalinity increased the portion of the unionized drug which permeated through the lipoid outer skin membrane of guinea pigs. (2) the amount of lignocaine accumulated on the dermal side of the diffusion cell containing isotonic phosphate buffer (ph 7.4) was directly proportional to the initial concentration of the applied drug at the alkaline ph. (3) the dermal transfer rates of lignocaine into the isoto ...197822468
chemotactic activity of guinea pig eosinophils for the ecf-a acidic tetrapeptides, histamine, histamine metabolites, and the effect of h1- and h2-receptor antagonists.histamine and one of its major metabolites, imidazoleacetic acid, were selectively chemotactic for guinea pig eosinophils, whereas l-histidine, 1,4-methylimidazoleacetic acid, 1,4-methylhistamine and n-acetylhistamine were inactive. the response to histamine was unaffected by concentrations of eosinophils of between 30 and greater than 90% but it was abrogated by preincubation of the cells with histamine prior to assay (self-deactivation). eosinophilotaxis was also inhibited by h1-(mepyramine-) ...197722498
the mechanism of the release of prostaglandin-like activity from guinea-pig isolated ileum. 197722612
effects of pulmonary metabolites of prostaglandins e2 and f2alpha on guinea-pig respiratory tract.the effects of three pulmonary metabolites of prostaglandins e2 and f2alpha on the guinea-pig tracheal muscle in vitro and on lung resistance in vivo were investigated. prostaglandin f2alpha, 13,14-dihydro pgf2alpha and 13,14-dihydro 15-oxo pgf2alpha produced contractions on the tracheal muscle in vitro. 15-oxo pgf2alpha relaxed some tracheal preparations but stimulated others, the stimulant action having a threshold dose range some 10-25 times lower than the relaxant doses. prostaglandin f2alph ...197722623
an analysis of the inhibitory effects and of possible prostaglandins antagonism of chloroquine in the guinea-pig isolated ileum. 197722625
antidotal action of the oxime hs6 at the soman poisoned neuromuscular junction of the rat and guinea-pig. 197722626
receptors involved in inhibition of the response to acetylcholine released from the myenteric plexus of the guinea-pig ileum proceedings. 197722656
changes in muscarinic ligand binding to intestinal muscle strips produced by pre-exposure to hypotonic conditions.the extent of the binding of 3hpropylbenzilylcholine mustard (3h-prbcm) to muscarinic receptors in longitudinal muscle strips from guinea-pig small intestine is increased by nearly 50% when the strips are preexposed to distilled water before measurement of 3h-prbcm binding in krebs-henseleit solution. the apparent rate constant for 3h-prbcm-receptor complex formation is more than double that of intact strips. the curves for the inhibition of 3h-prbcm binding by methylatropinium bromide in normal ...197822721
synthesis and beta-adrenergic blocking activity of a novel class of aromatic oxime ethers.a new series of beta-adrenergic blocking amines containing an oximino-propanolic chain linked to an aromatic nucleus was synthesized. most of the derivatives are characterized by beta2-selectivity. the structure-activity relationship are discussed. one of the compounds, selected for further studies, was more active on the trachea than on the atria of guinea pig, 155 times in vitro and 26 times in vivo. in comparison, butoxamine's beta2-selectivity is 13 in vitro and only 2 in vivo. with a series ...197722751
adrenoceptor blocking agents. 2. 2-(alpha-hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists.threo- and erythro-2-(alpha-hydroxybenzyl)-3,3-dimethylaziridines (1a and 1b) and threo-2-alpha-hydroxy(2-naphthyl)methyl- and 2-alpha-hydroxy(3,4-dichlorobenzyl)-3,3-dimethylaziridines (1d and 1c) have been prepared as conformationally restricted analogues of beta-adrenoceptor blocking agents like dichloroisoproterenol (dci) and pronethalol. the aziridine analogues 1 except possibly 1c are competitive antagonists of isoproterenol-induced response on a guinea pig tracheal chain preparation and t ...197822756
isolation and enzymatic characterization of guinea pig cardiac sarcolemma.sarcolemma was isolated by fractionation of salt-extracted particles on two consecutive sucrose density gradients. salt extraction of homogenates, rather than of washed particles, was found to preserve the activities of adenylate cyclase and ouabain-sensitive (na+,-k+)-atpase in the isolated sarcolemmal membranes. purified sarcolemma contained substantial adenylate cyclase and guanylate cyclase activities that were stimulable by beta-adrenergic and muscarinic agonists, respectively. significant ...197622901
neuronal aspects of opiate dependence and tolerance in comparison to central depressants.some acute and chronic effects of opiates and of central depressants have been reviewed, in order that a comparison can be made between the actions of these drugs. special emphasis has been given to opiate-induced changes at the neuronal level, which have been studied either by the direct microelectrophoretic application of drugs to single neurones or by application of drugs to the myenteric plexus/longitudinal muscle preparation of the guinea pig ileum. available evidence suggests that chronic ...197722993
some effects of glucose concentration and anoxia on glycolysis and metabolite concentrations in the perfused liver of fetal guinea pig.effects of glucose concentration and anoxia upon the metabolite concentrations and rates of glycolysis and respiration have been investigated in the perfused liver of the fetal guinea pig. in most cases the metabolite concentrations in the perfused liver were similar to those observed in vivo. between 50 days and term there was a fall in the respiratory rate and in the concentration of atp and fructose 1,6-diphosphate and an increase in the concentration of glutamate, glycogen and glucose. reduc ...197823174
the beta-adrenoceptor stimulant properties of opc-2009 on guinea-pig isolated tracheal, right atrial and left atrial preparations.1. the beta-adrenoceptor stimulant properties of 5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxy-carbostyril hydrochloride hemihydrate (opc-2009) were compared with those of isoprenaline and salbutamol on guinea-pig isolated tissues. 2. in producing tracheal relaxation, opc-2009 was approximately 7 times more potent and salbutamol 5 times less potent than isoprenaline. both compounds were less potent than isoprenaline in increasing either the rate of beating of isolated right atria or the contract ...197723191
adenosine, theophylline, and perfusate ph in the isolated, perfused guinea pig heart. 197823224
a comparative study of the distribution of free choline in the plasma, liver, lung and kidney of the toad, tortoise, chicken and guinea-pig. 197723239
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