MUSCARINIC RECEPTOR SELECTIVITIES OF 3-QUINUCLIDINYL 8-XANTHENECARBOXYLATE (QNX) IN RAT-BRAIN

被引：2

作者：

GIBSON, RE ^{[1
]}

SCHNEIDAU, TA ^{[1
]}

GITLER, M ^{[1
]}

ZEEBERG, B ^{[1
]}

REBA, RC ^{[1
]}

机构：

[1] GEORGE WASHINGTON UNIV,MED CTR,DEPT RADIOL,RADIOPHARMACEUT CHEM SECT,WASHINGTON,DC 20037

来源：

LIFE SCIENCES | 1994年 / 54卷 / 23期

关键词：

QUINUCLIDINYL XANTHENE-8-CARBOXYLATE; MUSCARINIC RECEPTOR; BRAIN;

D O I：

10.1016/0024-3205(94)90114-7

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

We have determined the binding of (R)-3-Quinuclidinyl 8-xanthenecarboxylate to muscarinic acetylcholine receptor preparations from rat cortex, hippocampus, caudate/putamen, thalamus, pens and colliculate bodies. The competition curves determined with [H-3]quinuclidinyl benzilate as the radioligand are well described by a two site model with a difference in affinity between the two sites of 12-fold. The proportions of high affinity site vary from 100% in the caudate/putamen to 0% in the pons/medulla. The selectivities are different from those measured by pirenzepine and are consistent with QNX exhibiting similar affinity for the M(1), M(3), and M(4) receptors with lower affinity for the M(2) receptor. This assignment was confirmed by determining the affinities of QNX for the cloned receptor subtypes.

引用

页码：1757 / 1765

页数：9

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