SR141716A是一种人源大麻素CB1受体的反向激动剂。
SR141716A is an inverse agonist at the human cannabinoid CB1 receptor.
作者信息
Landsman R S, Burkey T H, Consroe P, Roeske W R, Yamamura H I
机构信息
Department of Pharmacology, University of Arizona Health Sciences Center, Tucson 85724, USA.
出版信息
Eur J Pharmacol. 1997 Sep 3;334(1):R1-2. doi: 10.1016/s0014-2999(97)01160-6.
The effects of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4- benzoxazin-yl]-(1-napthalenyl)methanone mesylate (WIN 55,212-2) and N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazo le-carboxamide (SR141716A) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS) binding to membranes isolated from human cannabinoid CB1 receptor-transfected Chinese hamster ovary (CHO) cells were examined. WIN 55,212-2 stimulated [35S]GTPgammaS binding 76.3% above basal levels whereas SR141716A produced a 22.3% decrease in basal [35S]GTPgammaS binding. These findings demonstrate that WIN 55,212-2 is an agonist and SR141716A is an inverse agonist in this system.
研究了R(+)-[2,3-二氢-5-甲基-3-[(吗啉基)甲基]吡咯并[1,2,3-德]-1,4-苯并恶嗪基]-(1-萘基)甲磺酸盐（WIN 55,212-2）和N-哌啶基-5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-3-吡唑甲酰胺（SR141716A）对从转染人大麻素CB1受体的中国仓鼠卵巢（CHO）细胞分离的膜上鸟苷-5'-O-(3-[35S]硫代)三磷酸（[35S]GTPγS）结合的影响。WIN 55,212-2使[35S]GTPγS结合比基础水平增加76.3%，而SR141716A使基础[35S]GTPγS结合减少22.3%。这些发现表明，在该系统中WIN 55,212-2是激动剂，SR141716A是反向激动剂。
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