阿普洛尔和溴乙酰阿普洛尔薄荷烷是大鼠左心房β1 -肾上腺素受体的竞争性缓慢可逆拮抗剂。
Alprenolol and bromoacetylalprenololmenthane are competitive slowly reversible antagonists at the beta 1-adrenoceptors of rat left atria.
作者信息
Surman A J, Doggrell S A
机构信息
Department of Pharmacology, School of Medicine, University of Auckland, New Zealand.
出版信息
J Cardiovasc Pharmacol. 1993 Jan;21(1):35-9. doi: 10.1097/00005344-199301000-00006.
We studied the effects of alprenolol and bromoacetylalprenololmenthane (BAAM) on rat left atria. Alprenolol and BAAM at 10(-7), 3 x 10(-7), and 10(-6) M inhibited the cardiac stimulation response slightly, which is indicative of membrane-stabilizing activity independent of beta-adrenoceptor blockade. This membrane-stabilizing activity was readily reversible. Alprenolol and BAAM also caused surmountable antagonism of isoprenaline responses, and this beta 1-adrenoceptor antagonism was slowly reversible. Inhibition of the isoprenaline responses with alprenolol and BAAM at 10(-6) M was at equilibrium after 60 min, which is indicative of reversible antagonism. We conclude that alprenolol and BAAM are competitive slowly reversible beta 1-adrenoceptor antagonists on rat left atria.
我们研究了阿普洛尔和溴乙酰阿普洛尔薄荷烷（BAAM）对大鼠左心房的影响。阿普洛尔和BAAM在10⁻⁷、3×10⁻⁷和10⁻⁶ M浓度下对心脏刺激反应有轻微抑制作用，这表明其具有与β-肾上腺素受体阻断无关的膜稳定活性。这种膜稳定活性易于逆转。阿普洛尔和BAAM还引起了对异丙肾上腺素反应的可克服性拮抗作用，且这种β₁-肾上腺素受体拮抗作用逆转缓慢。在10⁻⁶ M浓度下，阿普洛尔和BAAM对异丙肾上腺素反应的抑制作用在60分钟后达到平衡，这表明是可逆性拮抗作用。我们得出结论，阿普洛尔和BAAM是大鼠左心房上具有竞争性且逆转缓慢的β₁-肾上腺素受体拮抗剂。
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