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兔心脏变时性和变力性β-肾上腺素能受体的药效学差异

Pharmacodynamic differentiation of chronotropic and inotropic beta-adrenergic receptors in rabbit heart.

作者信息

Ferguson D M, Vázquez A J

出版信息

J Cardiovasc Pharmacol. 1984 Jan-Feb;6(1):151-8.

PMID:6199598
Abstract

Isolated, perfused rabbit hearts were used to identify substituted phenylethylamines selective for either chronotropic or inotropic stimulation relative to norepinephrine. Heart rate and dF/dtmax were measured; the difference in their normalized values was used as an index of selectivity. p-Octopamine (OA) showed chronotropic preference, while phenylephrine (PE) showed a significant inotropic preference. Their effects were not prevented by reserpine pretreatment, cocaine, butoxamine, or phenoxybenzamine, but were antagonized by propranolol, which suggests that OA and PE exert their selective actions directly at beta 1-receptors. These findings provide further evidence for the existence of separate chronotropic and inotropic beta-adrenergic receptors in the heart.

摘要

使用离体灌注兔心脏来鉴定相对于去甲肾上腺素对变时性或变力性刺激具有选择性的取代苯乙胺。测量心率和最大dF/dt;它们归一化值的差异用作选择性指标。对羟基去甲肾上腺素(OA)表现出变时性偏好,而去氧肾上腺素(PE)表现出显著的变力性偏好。利血平预处理、可卡因、布托沙明或酚苄明不能阻止它们的作用,但普萘洛尔可拮抗这些作用,这表明OA和PE直接在β1受体上发挥其选择性作用。这些发现为心脏中存在独立的变时性和变力性β-肾上腺素能受体提供了进一步的证据。

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