174689-39-5
中文名稱
1-(2-ETHYLPHENOXY)-3-[[(1S)-1,2,3,4-TETRAHYDRO-1-NAPHTHALENYL]AMINO]-(2S)-2-PROPANOL HYDROCHLORIDE
英文名稱
1-(2-ETHYLPHENOXY)-3-[[(1S)-1,2,3,4-TETRAHYDRO-1-NAPHTHALENYL]AMINO]-(2S)-2-PROPANOL HYDROCHLORIDE
CAS
174689-39-5
分子式
C21H27NO2.C2H2O4
分子量
415.48
MOL 文件
174689-39-5.mol
更新日期
2023/03/20 15:41:31
174689-39-5 結(jié)構(gòu)式
基本信息
中文別名
化合物SR59230A(S)-1-(2-乙基苯氧基)-3-(((S)-1,2,3,4-四氫萘-1-基)氨基)丙-2-醇草酸鹽
英文別名
SR 59230ASR59230AHCl
SR 59230A HYDROCHLORIDE
SR 59230A >=98% (HPLC), powder
3-(2-ETHYLPHENOXY)-1-((1S)-1,2,3,4-TETRA-HYDRONAPHTH-1-YLAMINO)-(2S)-2-PROPANOL OXALATE
(S)-1-(2-Ethylphenoxy)-3-(((S)-1,2,3,4-tetrahydronaphthalen-1-yl)amino)propan-2-ol oxalate
3-(2-Ethylphenoxy)-1-[[(1S)-1,2,3,4-tetrahydronaphth-1-yl]amino]-(2S)-2-propanol oxalate salt
1-(2-ETHYLPHENOXY)-3-[[(1S)-1,2,3,4-TETRAHYDRO-1-NAPHTHALENYL]AMINO]-(2S)-2-PROPANOL HYDROCHLORIDE
hyperthermia,adrenoceptor,Adrenergic Receptor,adrenergic,Beta Receptor,inhibit,hypothermia,receptor,Inhibitor,SR59230A,SR-59230A
常見問題列表
生物活性
SR59230A 是一種血腦屏障穿透性的、有效的 β3-adrenergic receptor 的選擇性拮抗劑，對β3、β1和β2受體的IC50分別為40 nM、408 nM和648 nM。靶點
| Target | Value |
|
β3-adrenergic receptor
(Cell-free assay) | 40 nM |
|
β1-adrenergic receptor
(Cell-free assay) | 408 nM |
|
β2-adrenergic receptor
(Cell-free assay) | 648 nM |
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. |