A novel muscarinic M4 receptor antagonist provides further evidence of an autoreceptor role for the muscarinic M2 receptor sub-type
A novel muscarinic M4 receptor antagonist provides further evidence of an autoreceptor role for the muscarinic M2 receptor sub-type
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DOI：
10.1016/s0014-2999(99)00607-x
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发表时间：
1999-10-21
影响因子：
5
通讯作者：
Quirion, R
中科院分区：
文献类型：
--
作者：
Kitaichi, K;Day, JC;Quirion, R
用M-2（AF-DX 384，BIBN-161）和M-4（PD 102807）受体拮抗剂研究了这两种受体亚型在大鼠海马乙酰胆碱释放调节中的作用。在体内透析研究表明，只有毒蕈碱M-2受体拮抗剂显着和浓度依赖性促进乙酰胆碱的释放。新开发的毒蕈碱M-4受体拮抗剂不能调节乙酰胆碱的释放，除非在最高浓度的测试。因此，看来在大鼠海马中作为负性自身受体的毒蕈碱受体是毒蕈碱M-2亚型，在这方面，毒蕈碱M-4受体的作用是最小的。(C)1999 Elsevier Science B. V.保留所有权利。
Muscarinic M-2 (AF-DX 384, BIBN-161) and M-4 (PD102807) receptor antagonists were used to investigate the respective roles of these two receptor sub-types in the regulation of acetylcholine release in the rat hippocampus. In vivo dialysis studies revealed that only the muscarinic M-2 receptor antagonists significantly and concentration-dependently facilitate acetylcholine release. The newly developed muscarinic M-4 receptor antagonist was unable to regulate acetylcholine release except at the highest concentration tested. It would thus appear that the muscarinic receptor acting as negative autoreceptor in the rat hippocampus is of the muscarinic M-2 sub-type, the role of the muscarinic M-4 receptor being minimal in this regard. (C) 1999 Elsevier Science B.V. All rights reserved.