AR-A 2
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) |
AR-A 2 用途与合成方法
|
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).
