Abstract：
:1. The relaxant effects of Zeneca ZD7114, BRL37344 (putative beta 3-adrenoceptor agonists) and various phenylethylamine-based agonists were studied in isolated ileum of the rat where tone was increased with carbachol (0.5 microM). Agonist-induced relaxation.was measured under equilibrium conditions with alpha-, beta 1- and beta 2-adrenoceptors inhibited. 2. Relaxant responses were obtained to isoprenaline, noradrenaline, and BRL37344, although, the efficacy of this latter agent was significantly.lower than that of isoprenaline. Salbutamol caused weak relaxation (< 20%) at high concentrations (10 microM) and ZD7114 was without significant relaxant effect even at high concentrations (10 microM). 3. Relaxant responses to isoprenaline and BRL37344 were weakly antagonized by high concentrations of (+/-)-propranolol (10 and 100 microM) yielding pKB values of 5.7 with isoprenaline as the agonist and 5.5 with BRL37344 as the agonist. 4. The non-selective beta-adrenoceptor antagonist, (+/-)-alprenolol (1-100 microM) caused competitive antagonism of the relaxant responses to isoprenaline (pA2 value = 6.5). A similar pKB value was obtained when BRL37344 was used as the agonist (6.4). 5. Relaxant effects of isoprenaline and BRL37344 were also antagonized by ZD7114 (1-100 microM) yielding pA2 and pKB values of 6.3 and 6.7 respectively. 6. The low potencies of (+/-)-propranolol and (+/-)-alprenolol as antagonists of the relaxant responses to isoprenaline and BRL37344 indicate that both the agonists and antagonists employed in the current study may interact with beta 3-adrenoceptors in the rat isolated ileum. Contrary to the previous findings in guinea-pig ileum, where BRL37344 and ZD7114 were full agonists, in the current study, BRL37344 was a partial agonist and ZD7114 an antagonist at the beta 3-adrenoceptor in rat ileum.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Growcott JW,Holloway B,Green M,Wilson Cdoi
10.1111/j.1476-5381.1993.tb13972.xsubject
Has Abstractpub_date
1993-12-01 00:00:00pages
1375-80issue
4eissn
0007-1188issn
1476-5381journal_volume
110pub_type
杂志文章abstract：:1. Isolated preparations of rat anococcygeus muscle were incubated with [3H]-noradrenaline and the efflux of radioactivity induced by stimulation of intramural sympathetic nerves was used as a measure of release of transmitter noradrenaline. Isometric contractile responses were also measured. 2. Angiotensin I (0.03 mi...
journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1988.tb11657.x
更新日期：1988-10-01 00:00:00
abstract：:The effects of caffeine and procaine on noradrenergic transmission in the guinea-pig mesenteric artery were investigated by recording electrical responses of smooth muscle cells and by measuring the outflow of noradrenaline (NA) and 3,4-dihydroxyphenylglycol (DOPEG) induced by perivascular nerve stimulation. Caffeine ...
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abstract：:1. Mast cells and basophils are believed to trigger allergic reactions and anaphylaxis. They rapidly release histamine (H), a typical mediator of inflammation, in response to antigens. In the mouse, platelets contain much 5-hydroxytryptamine (5HT), an additional inflammatory mediator, while human platelets contain bot...
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journal_title：British journal of pharmacology
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journal_title：British journal of pharmacology
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abstract：:1. The kinetics of glycine-sensitive, N-methyl-D-aspartate (NMDA) receptor desensitization were investigated in cultured neurones with the patch clamp technique. 2. The degree of fast NMDA-receptor desensitization was inversely related to glycine concentration. Thus, increasing concentrations of glycine from 30 nM to ...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1993.tb13556.x
更新日期：1993-05-01 00:00:00
abstract：:A dispersed rat anterior pituitary cell system has been used to investigate the effects of cyproheptadine and metergoline on prolactin secretion. Both drugs were potent inhibitors of prolactin secretion. However, the inhibition was not antagonized by either 5-hydroxytryptamine or a variety of dopamine antagonists. We ...
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1980.tb10896.x
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abstract：:The last five years have witnessed a remarkable resurgence of interest in myocardial reperfusion injury. Reperfusion is absolutely essential to salvage ischaemic myocardium but experimental and clinical studies show that reperfusion-associated injury may mask the full benefits of prompt reperfusion in acute myocardial...
journal_title：British journal of pharmacology
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abstract：:1. The effect of a single injection of the monoamine oxidase inhibitor, tranylcypromine, administered intravenously (20 mg/kg) or into the lateral cerebral ventricle (5-10 mg), on hypothalamic and rectal temperature, has been investigated.2. Intravenous tranylcypromine causes a significant rise in body temperature, wh...
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1970.tb10594.x
更新日期：1970-05-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Excessive production of nitric oxide (NO) by inducible NO synthase (iNOS) is thought to underlie the vascular dysfunction, systemic hypotension and organ failure that characterize endotoxic shock. Plasma levels of atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP) and C-type natriu...
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pub_type： 杂志文章
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更新日期：2010-08-01 00:00:00
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pub_type： 杂志文章
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doi：10.1111/bph.12690
更新日期：2014-07-01 00:00:00
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doi：10.1038/sj.bjp.0702442
更新日期：1999-03-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1972.tb07286.x
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doi：10.1111/j.1476-5381.1992.tb14345.x
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更新日期：2015-08-01 00:00:00
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更新日期：1999-09-01 00:00:00
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更新日期：1998-10-01 00:00:00
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0702607
更新日期：1999-06-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1995.tb15040.x
更新日期：1995-08-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Resurgence in the use of chloroquine as a potential treatment for COVID-19 has seen recent cases of fatal toxicity due to unintentional overdoses. Protocols for the management of poisoning recommend diazepam, although there are uncertainties in its pharmacology and efficacy in this context. The a...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/bph.15101
更新日期：2020-11-01 00:00:00
