395679-53-5
| 中文名称 | 395679-53-5 |
|---|---|
| 中文同义词 | 化合物 T16852 |
| 英文名称 | SB-568849 |
| 英文同义词 | SB-568849;[1,1'-Biphenyl]-4-carboxamide, N-[4-[2-(diethylamino)ethoxy]-3-methoxyphenyl]-N-methyl-4'-(trifluoromethyl)-;SB 568849,SB568849 |
| CAS号 | 395679-53-5 |
| 分子式 | C28H31F3N2O3 |
| 分子量 | 500.55 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 395679-53-5.mol |
| 结构式 |  |
395679-53-5 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
MCH R1 receptor
SB-568849 is a selective SLC-1 antagonist with a pK i of 7.7 as determined in radioligand binding displacement assays; coincubation of tissue with 1 μM SB-568849 for 45 min completely inhibits the MCH induced increase in corticotropin-releasing factor (CRF) release to basal levels without causing any effect on its own. The only reported MCH receptor in the rat is SLC-1, a G protein coupled receptor found throughout the brain and periphery.
SB-568849 (Compound 15h) possesses good receptor affinity and selectivity. SB-568849 proves to be an antagonist with stability in vivo, an acceptable brain–blood ratio and oral bioavailability. SB-568849 retains affinity, demonstrates greater in vivo stability (CL b =16 mL/min/kg) and shows an acceptable brain-blood ratio of 1. SB-568849 also shows >30-fold selectivity over a wide range of monoamine receptors and is an antagonist in the FLIPR assay with a pK b of 7.7.