[QUINUCLIDINYL-H-3 BENZILATE BINDING TO MUSCARINIC RECEPTORS IN RAT-BRAIN - COMPARISON OF RESULTS FROM INTACT BRAIN-SLICES AND HOMOGENATES

被引:58
作者
GILBERT, RFT
HANLEY, MR
IVERSEN, LL
机构
[1] MRC Neurochemical Pharmacology Unit, Dept. of Pharmacology, Medical School, Cambridge, Hills Road
关键词
D O I
10.1111/j.1476-5381.1979.tb07850.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The binding of [3H]‐(+)‐quinuclidinyl benzilate ([3H]‐(±)‐QNB) to muscarinic sites in rat brain slice and homogenate preparations was compared. Evidence is presented in support of the view that only the (—)‐enantiomer of QNB binds with high affinity to muscarinic sites. The Kd value for [3H]‐(—)‐QNB binding in slices was eight times higher than that measured in homogenates. Similarly, the potencies of various muscarinic ligands as inhibitors of [3H]‐(—)‐QNB binding were consistently lower in slices than in homogenates. It is proposed that the results may reflect differences in the binding properties of muscarinic receptors in intact tissue slice and homogenate preparations. 1979 British Pharmacological Society
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页码:451 / 456
页数:6
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