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. 1991 Jun;103(2):1351–1356. doi: 10.1111/j.1476-5381.1991.tb09792.x

Characterization of catecholamine-mediated relaxations in rat isolated gastric fundus: evidence for an atypical beta-adrenoceptor.

D P McLaughlin 1, A MacDonald 1
PMCID: PMC1908376  PMID: 1679358

Abstract

1. Experiments were carried out in order to characterize the receptors mediating relaxant responses to catecholamines in the rat gastric fundus. The effects of noradrenaline, isoprenaline and the 'atypical' or beta 3-adrenoceptor agonist, BRL 37344, on methacholine-induced tone were measured. Prazosin, propranolol and cyanopindolol were used as antagonists. 2. Relaxant responses to noradrenaline, in the presence of propranolol (1 microM) were antagonized in a concentration-dependent manner by prazosin (0.01 to 1 microM), although this antagonism was weak and non-competitive in nature. Relaxant responses to isoprenaline, in the presence of prazosin (0.1 microM), were antagonized only by the highest concentration of propranolol (1 microM) giving a pKB of 6.3 BRL 37344 also relaxed the rat gastric fundus in the presence of prazosin (0.1 microM), and the responses to BRL 37344 were unaffected by propranolol (1 microM). 3. Tachyphylaxis to BRL 37344 was observed, a second concentration-response curve being significantly shifted to the right. Exposure of tissues to BRL 37344 (1 microM) between concentration-response curves also caused an 11 fold rightward shift in the response to isoprenaline. 4. In the presence of prazosin (0.1 microM) and propranolol (1 microM), the rank order of potency of the agonists was: (-)-isoprenaline (1.0) greater than (-)-noradrenaline (0.39) greater than BRL 37344 (0.10). 5. Responses to BRL 37344 in the presence of prazosin (0.1 microM) and propranolol (1 microM) were antagonized by (+/-)-cyanopindolol (1 microM), with a pKB of 6.56.(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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