220051-79-6
220051-79-6 結(jié)構(gòu)式
基本信息
AR-A 000002
Benzamide, 4-(4-morpholinyl)-N-[(2R)-1,2,3,4-tetrahydro-5-methyl-8-(4-methyl-1-piperazinyl)-2-naphthalenyl]-
物理化學(xué)性質(zhì)
常見問題列表
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5-HT 1B/D Receptor 20 nM (Ki) |
5-HT 2A Receptor 339 nM (Ki) |
5-HT 1A Receptor 3070 nM (Ki) |
AR-A 2 (AR-A000002) is a selective 5-HT 1B receptor antagonist, with high affinity to guinea pig cortex 5HT 1B/1D and recombinant guinea pig 5-HT 1B receptors (K i =0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT 1D receptors (K i , 5 nM), and shows an EC 50 of 4.5 nM for the guinea pig 5-HT 1B receptor. AR-A 2 also binds to the rat cortical 5HT 1B/1D receptor (K i , 20 nM), rat cortex 5-HT 2A receptor (K i , 339 nM), rat hippocampus 5-HT 1A receptor (K i , 3070 nM). In addition, AR-A 2 also exhibits affinity for dopamine D2 (K i , 330 nM) and α1-adrenoceptors (K i , 490 nM).