功能研究α1-adrenoceptor亚型介导性肌力影响大鼠右心室。

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米歇尔•MC总值另G, G

功能研究α1-adrenoceptor亚型介导性肌力影响大鼠右心室。

Br J杂志。1994年2月,111(2):539 - 46所示。

PubMed ID

7911719 (在PubMed

]

文摘

1。我们已经研究了α1-adrenoceptor亚型介导性肌力的影响肾上腺素在大鼠右心室和Ca2 +源用来引出这些影响。α1 a-adrenoceptor-mediated鼠输精管收缩效应,研究了在某些情况下进行比较。2。chloroethylclonidine治疗并不影响最大beta-adrenoceptor-mediated变力作用在大鼠右心室或最大α1 a-adrenoceptor-mediated鼠输精管收缩的影响;它没有改变心室异丙肾上腺素的效力,降低了效能alpha-adrenoceptor拮抗剂的输精管仅略。治疗右心室条与CdCl2显著降低静息张力和增强最大收缩能异丙肾上腺素,但不影响其效能的影响。3所示。失活的心脏α1 b-adrenoceptors chloroethylclonidine稍有增强治疗的最大影响肌肉收缩的影响完全激动剂,肾上腺素和几个部分受体激动剂。4所示。 Schild analysis of inhibition experiments with the alpha 1A-adrenoceptor-selective antagonists, 5-methyl-urapidil and (+/-)-tamsulosin, demonstrated that adrenaline causes its inotropic effects mainly via the alpha 1B-adrenoceptor subtype. Schild analysis of 5-methyl-urapidil inhibition experiments in chloroethylclonidine-treated ventricles indicated that only alpha 1A-adrenoceptors mediate the inotropic effects of adrenaline following inactivation of the alpha 1B-adrenoceptors. 5. In control ventricles the organic Ca2+ entry blocker, nitrendipine and treatment with the inorganic Ca2+ entry blocker, CdCl2 did not reduce inotropic effects of adrenaline whereas ryanodine treatment inhibited them. In contrast, nitrendipine and CdCl2 treatment had major inhibitory effects in chloroethylclonidine-treated but lacked inhibitory effects in phenoxybenzamine-treated ventricular strips. 6. We conclude that inotropic effects of adrenaline in rat heart are mediated mainly by alpha 1B-adrenoceptors via release of Ca2+ from an intracellular pool. Following inactivation of alpha 1B-adrenoceptors by chloroethylclonidine treatment, alpha lA-adrenoceptors can fully compensate and mediate inotropic effects by promoting influx of extracellular Ca2+ at least partly via voltage-operated channels.Therefore, we speculate that alpha 1B-adrenoceptors exert a tonic inhibitory effect on alpha 1A-adrenoceptors.

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药物靶点

药物	目标	类	生物	药理作用	行动
酚苄明	Alpha-1A肾上腺素能受体	蛋白质	人类	是的	拮抗剂	细节
Tamsulosin	Alpha-1B肾上腺素能受体	蛋白质	人类	未知的	拮抗剂	细节