钙离子通道配体对毒蕈碱型m1和m3受体上[3H]QNB结合的影响。

Effects of Ca2+ channel ligands on [3H]QNB binding at m1 and m3 muscarinic receptors.

Kwon Y W, Triggle D J

Department of Biochemical Pharmacology, School of Pharmacy, State University of New York, Buffalo 14260.

Gen Pharmacol. 1991;22(2):267-70. doi: 10.1016/0306-3623(91)90445-c.

Abstract

The effects of Ca2+ channel ligands on [3H]QNB binding in m1- or m3-transfected Chinese hamster ovary (CHO) cells have been studied. 2. The IC50 values of Ca2+ channel ligands for the inhibition of [3H]QNB binding were between 10(-6) and 10(-4) M and the rank order of potency was HOE 166 greater than McN 6186 greater than nicardipine greater than tiamdipine greater than verapamil greater than diltiazem greater than Bay K 8644 greater than nifedipine at m1 and m3 receptors. 3. The results indicate that Ca2+ channel ligands employed in this experiment do not distinguish subtypes of muscarinic receptors.

摘要

研究了钙离子通道配体对转染了m1或m3的中国仓鼠卵巢（CHO）细胞中[3H]QNB结合的影响。2. 钙离子通道配体抑制[3H]QNB结合的IC50值在10（-6）至10（-4）M之间，在m1和m3受体上的效力排序为HOE 166大于McN 6186大于尼卡地平大于替米地尔大于维拉帕米大于地尔硫卓大于Bay K 8644大于硝苯地平。3. 结果表明，本实验中使用的钙离子通道配体无法区分毒蕈碱受体亚型。