Wilson C, Lincoln C
J Cardiovasc Pharmacol. 1984 Nov-Dec;6(6):1216-21.
Selective beta-adrenoceptor agonists and antagonists were used to characterize the beta-adrenoceptor subtypes in human right atrium. The activity order of selective agonists for rat, guinea pig, and rabbit atrial inotropic and chronotropic responses was consistent with the hypothesis that only beta 1-adrenoceptors mediate these responses. In human right atrium, however, the beta 2-selective agonists fenoterol and salbutamol were relatively much more active. The beta 1-selective antagonist practolol preferentially antagonized the human atrial response to noradrenaline (beta 1-selective) as opposed to fenoterol (beta 2-selective), whereas the beta 2-selective antagonist ICI 118,551 preferentially antagonized the response to fenoterol. The data indicate that the response of human right atrium to beta-adrenoceptor agonists is mediated by a mixed beta 1-plus beta 2-adrenoceptor population. The implications of these results with respect to the therapeutic uses of beta-adrenoceptor agonists are discussed.
使用选择性β-肾上腺素能受体激动剂和拮抗剂来鉴定人右心房中的β-肾上腺素能受体亚型。选择性激动剂对大鼠、豚鼠和兔心房变力性和变时性反应的活性顺序与仅β1-肾上腺素能受体介导这些反应的假说一致。然而,在人右心房中,β2-选择性激动剂非诺特罗和沙丁胺醇的活性相对高得多。β1-选择性拮抗剂普拉洛尔优先拮抗人心房对去甲肾上腺素(β1-选择性)而非非诺特罗(β2-选择性)的反应,而β2-选择性拮抗剂ICI 118,551优先拮抗对非诺特罗的反应。数据表明,人右心房对β-肾上腺素能受体激动剂的反应是由β1加β2肾上腺素能受体混合群体介导的。讨论了这些结果对β-肾上腺素能受体激动剂治疗用途的影响。