Effects of verapamil on the binding properties of rat heart muscarinic receptors: evidence for an allosteric site.

Effects of verapamil on the binding properties of rat heart muscarinic receptors: evidence for an allosteric site.
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维拉帕米对大鼠心脏毒蕈碱受体结合特性的影响:变构位点的证据。

DOI:
10.1016/0006-291x(84)90728-9
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发表时间:
1984
影响因子:
3.1
通讯作者:
Jean Christophe
Jean Christophe
中科院分区:
生物学4区
文献类型:
--
作者:
M. Waelbroeck;P. Robberecht;P. Neef;Jean Christophe

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已知钙通道拮抗剂维拉帕米可抑制竞争性拮抗剂与大鼠心脏毒蕈碱受体的结合。目前的数据表明,该药物识别毒蕈碱受体上的两个结合位点:1)调节示踪剂解离率的变构位点和2)毒蕈碱药物结合位点。维拉帕米对变构位点的亲和力及其对毒蕈碱配体解离率的影响取决于所研究的配体。
The calcium channel antagonist verapamil is known to inhibit competitively antagonist binding to rat heart muscarinic receptors. The present data suggest that this drug recognized two binding sites on the muscarinic receptors: 1) an allosteric site modulating the tracer dissociation rates and 2) the muscarinic drug binding site. The affinity of verapamil for the allosteric site and the efficacy of its effect on muscarinic ligand dissociation rates depended on the ligand studied.
维拉帕米竞争性抑制大鼠心肌中的α1-肾上腺素能受体和毒蕈碱受体,但不抑制β-肾上腺素能受体。
DOI: 10.1097/00005344-198205000-00025
发表时间: 1982
影响因子: 3
作者:
Karliner,JS;Motulsky,HJ;Dunlap,J;Brown,JH;Insel,PA
通讯作者: Insel,PA
维拉帕米、硝苯地平和尼莫地平对心室肌钙依赖性动作电位阻断的比较研究。
DOI: --
发表时间: 1983
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
作者:
Hachisu,M;Pappano,AJ
通讯作者: Pappano,AJ