（±）-吲哚洛尔对大鼠肋子宫肌具有β2肾上腺素能受体拮抗作用而非激动作用。

(+/-)-Pindolol has beta 2-adrenoceptor antagonist but not agonist action on the costo-uterine muscle of the rat.

Pennefather J N, Hartley M L, Leedham J A

Department of Pharmacology, Monash University, Clayton, Victoria, Australia.

Clin Exp Pharmacol Physiol. 1987 Jul;14(7):581-5. doi: 10.1111/j.1440-1681.1987.tb01877.x.

Abstract

The effects of isoprenaline and (+/-)-pindolol on rat isolated costo-uterine muscle have been compared. 2. Isoprenaline produced reproducible concentration-dependent inhibition of contractions, and maximal doses (less than 0.1 mumol/l) produced mean inhibition of 87, 94 and 97% of field, carbachol and potassium-stimulated preparations, respectively. 3. (+/-)-Pindolol, when effective, produced inhibition only in concentrations greater than its pA2 value (9.87) as an antagonist of isoprenaline; mean maximal effects were less than 60% of those produced by isoprenaline. 4. It is concluded that (+/-)-pindolol is a potent antagonist, but has only variable agonist action, at the beta 2-adrenoceptors of the rat costo-uterine muscle.

摘要

比较了异丙肾上腺素和（±）-吲哚洛尔对大鼠离体肋子宫肌的作用。2. 异丙肾上腺素可产生可重复的浓度依赖性收缩抑制作用，最大剂量（小于0.1μmol/L）分别使场刺激、卡巴胆碱刺激和钾刺激的标本平均抑制87%、94%和97%。3. （±）-吲哚洛尔仅在浓度高于其作为异丙肾上腺素拮抗剂的pA2值（9.87）时才产生抑制作用；平均最大效应小于异丙肾上腺素产生的效应的60%。4. 得出结论，（±）-吲哚洛尔在大鼠肋子宫肌的β2-肾上腺素受体处是一种强效拮抗剂，但仅具有可变的激动剂作用。