介导血管舒张的毒蕈碱受体亚型的测定。
Determination of the muscarinic receptor subtype mediating vasodilatation.
作者信息
Eglen R M, Whiting R L
出版信息
Br J Pharmacol. 1985 Jan;84(1):3-5.
Abstract
The muscarinic receptor mediating vasodilatation of the rabbit aorta and dog femoral artery has been assessed using muscarinic antagonists. With the exception of pirenzepine, the antagonist affinities were similar to those reported for the ileal receptors and dissimilar to those reported for the atrial receptors. Pirenzepine exhibited an affinity (7.54) intermediate between that reported for the CNS receptors (8.4) and that reported for the ileal receptors (6.77). This value for pirenzepine was confirmed using acetylcholine as the agonist and using the dog femoral artery as the vascular tissue. It is concluded that the muscarinic receptor profile mediating vasodilatation is not easily accommodated into the current receptor classification.
摘要
利用毒蕈碱拮抗剂对介导兔主动脉和犬股动脉血管舒张的毒蕈碱受体进行了评估。除哌仑西平外，拮抗剂亲和力与报道的回肠受体亲和力相似，与报道的心房受体亲和力不同。哌仑西平表现出的亲和力（7.54）介于报道的中枢神经系统受体亲和力（8.4）和回肠受体亲和力（6.77）之间。以乙酰胆碱为激动剂并以犬股动脉为血管组织，证实了哌仑西平的这一数值。得出的结论是，介导血管舒张的毒蕈碱受体特征不易纳入当前的受体分类。
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