Characterization of β-Adrenoceptor Subtype in Bladder Smooth Muscle in Cynomolgus Monkey

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We first investigated the relaxations of the urinary bladder induced by β-adrenoceptor agonists in anesthetized cynomolgus monkeys and then employed a variety of β-adrenoceptor agonists and antagonists in vitro to identify the β-adrenoceptor subtype responsible for the relaxation (using isolated monkey detrusors). Isoprenaline reduced bladder pressure in a dose-dependent manner. Isoprenaline, noradrenaline and adrenaline each produced a concentration-dependent relaxation of isolated detrusor strips, the rank order of relaxing potencies being isoprenaline > noradrenaline > adrenaline. Subtype-selective β-adrenoceptor agonists also relaxed isolated detrusor strips, the rank order of potencies being CGP-12177 > BRL 37344 > dobutamine, salbutamol, procaterol > xamoterol. In the antagonist experiment, bupranolol (β-antagonist, 10−6 to 10−5 M) and SR 58894A (β3-antagonist, 10−7 to 10−5 M) caused a rightward shift of the concentration-relaxation curve for isoprenaline, but CGP-20712A (β1-antagonist, 10−9 to 10 −7 M) and ICI-118551 (β2-antagonist, 10−9 to 10−7 M) did not. The present functional study provides the first evidence that relaxation of the monkey detrusor by β-adrenoceptor activation is mediated via the β3-subtype.
社団法人日本薬理学会の論文
2002-01-01