AM630 antagonism of cannabinoid-stimulated [S-35]GTP gamma S binding in the mouse brain
AM630 antagonism of cannabinoid-stimulated [S-35]GTP gamma S binding in the mouse brain
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DOI：
10.1016/s0014-2999(97)00047-2
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发表时间：
1997-02-19
影响因子：
5
通讯作者：
Yamamura, HI
中科院分区：
文献类型：
--
作者：
Hosohata, Y;Quock, RM;Yamamura, HI
本研究旨在确定新型氨基烷基吲哚AM 630的作用通过研究其与大麻素受体激动剂WIN 55，212 -2（R（+）-[2，3-二氢-5-甲基-3-[（吗啉基）甲基]吡咯并[1，2，3-de]-1，4-苯并恶嗪-基]-（1-萘基）甲酮甲磺酸盐）对小鼠脑中鸟苷-5 '-O-（3-[S-35]硫代）三磷酸（[S-35]GTP γ S）结合的影响。WIN 55，212 -2刺激[S-35]GTP γ S结合，而AM 630无作用。AM 630拮抗WIN 55，212 -2诱导的[S-35]GTP γ S结合，并使WIN 55，212 -2剂量-反应曲线向右移动。这些结果清楚地表明，AM 630在大脑中发挥大麻素受体拮抗剂特性。(C)1997年Elsevier Science B.V.
This research was designed to determine the action of the novel aminoalkylindole AM630 (6-iodo-pravadoline) at the cannabinoid receptor by studying its interaction with the cannabinoid receptor agonist WIN 55,212-2 (R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazin-yl]-(1-naphthalenyl)methanone mesylate) on guanosine-5'-O-(3-[S-35]thio)triphosphate ([S-35]GTP gamma S) binding in mouse brain. WIN 55,212-2 stimulated [S-35]GTP gamma S binding, while AM630 had no effect. AM630 antagonized WIN 55,212-2-induced [S-35]GTP gamma S binding and shifted the WIN 55,212-2 dose-response curve to the right. These results clearly demonstrate that AM630 exerts cannabinoid receptor antagonist properties in the brain. (C) 1997 Elsevier Science B.V.