1135278-41-9
中文名稱
SR 59230A HCl
英文名稱
SR 59230A HCl
CAS
1135278-41-9
分子式
C21H27NO2.HCl
分子量
361.91
MOL 文件
1135278-41-9.mol
1135278-41-9 結(jié)構(gòu)式
常見問題列表
生物活性
SR59230A hydrochloride 是一種有效，選擇性的，可透過血腦屏障的 β3-腎上腺素能受體 (β3-adrenergic receptor) 拮抗劑，對 β3，β1 和 β2 受體的 IC50 分別為 40、408 和 648 nM。靶點
IC50: 40 nM (β3 receptor), 408 nM ((β1 receptor), 648 nM (β2 receptor)
體外研究
SR59230A (100 nM-50 μM; 24 hours) is able to reduce cell viability in a dose-dependent manner in Neuro-2A, BE(2)C and SK-N-BE(2) NB cell lines.
Cell Viability Assay
| Cell Line: | Three different neuroblastoma (NB) cell lines, one murine (Neuro-2A) and two human (SK-N-BE(2), BE(2)C) |
| Concentration: | 100 nM, 1 μM, 5 μM, 10 μM, and 50 μM |
| Incubation Time: | 24 hours |
| Result: | Reduced cell viability in a dose-dependent manner, with significant effect at a concentration limit over 1?μM for Neuro-2A cells and 5?μM for SK-N-BE(2) and BE(2)C). |
體內(nèi)研究
MDMA (20 mg/kg) produces a slowly developing hyperthermia, reaching a maximum increase of 1.8°C at 130 min post injection. SR59230A (0.5 mg/kg) produces a small but significant attenuation of the slowly developing hyperthermia to MDMA. SR59230A (5 mg/kg) reveals a significant and marked early hypothermic reaction to MDMA.
| Animal Model: | Male C-57BL6J wild-type mice (22-35 g) |
| Dosage: | 0.5 or 5 mg/kg |
| Administration: | Injected s.c.; administered 30 min prior to the injection s.c. of MDMA (20 mg/kg). |
| Result: | Modulated the actions of MDMA on temperature involve α1-adrenoceptor antagonism. |