AR-A 2
| 中文名称 | AR-A 2 |
|---|---|
| 中文同义词 | 化合物 T10360 |
| 英文名称 | AR-A 2 |
| 英文同义词 | Benzamide, 4-(4-morpholinyl)-N-[(2R)-1,2,3,4-tetrahydro-5-methyl-8-(4-methyl-1-piperazinyl)-2-naphthalenyl]-;AR-A 000002;AR-A 2;ARA 2,AR A 2 |
| CAS号 | 220051-79-6 |
| 分子式 | C27H36N4O2 |
| 分子量 | 448.6 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 220051-79-6.mol |
| 结构式 |  |
AR-A 2 性质
| 沸点 | 697.1±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.22±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 15.50±0.20(Predicted) |
|
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).