372523-75-6
中文名称
(2S)-1-(6,7-DIMETHOXY-3,4-DIHYDRO-1H-ISOQUINOLIN-2-YL)-3,3-DIMETHYL-2-(PYRIDIN-4-YLMETHYLAMINO)BUTAN-1-ONE
英文名称
(2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanonehydrochloride
CAS
372523-75-6
分子式
C23H31N3O3
分子量
397.51
MOL 文件
372523-75-6.mol
更新日期
2024/05/24 11:46:36
372523-75-6 结构式
基本信息
中文别名
化合物TCS-OX2-29(2S)-2-(4-吡啶甲基氨基)-1-(6,7-二甲氧基-1,2,3,4-四氢异喹啉-2-基)-3,3-二甲基丁烷-1-酮
英文别名
TCS OX2 29TCS-OX2-29, CID 10408514
(2S)-1-(6,7-DIMETHOXY-3,4-DIHYDRO-1H-ISOQUINOLIN-2-YL)-3,3-DIMETHYL-2-(PYRIDIN-4-YLMETHYLAMINO)BUTAN-1-ONE
1-Butanone, 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-, (2S)-
(2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanonehydrochloride
物理化学性质
储存条件Keep in dark place,Inert atmosphere,2-8°C
溶解度DMSO : 25 mg/mL (62.89 mM; Need ultrasonic)Ethanol : 25 mg/mL (62.89 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
形态粉末
常见问题列表
生物活性
TCX-OX2-29是OX2R 拮抗剂，pKi=7.5。对hOX2R的选择性比hOX1R高250倍以上，IC50分别为40 nM和>10000 nM。靶点
IC50: 40 nM ( OX 2 R ); pKi: 7.5 ( OX 2 R )
体外研究
TCS-OX2-29 inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX 2 receptor.
体内研究
TCS-OX2-29 (5-10 mg/kg; intraperitoneal injection; adult male NMRI mice) treatment suppresses conditioned place preference (CPP) acquisition and expression in both naïve and dependent mice significantly.
| Animal Model: | 440 adult male NMRI mice (25-30 g) |
| Dosage: | 5 mg/kg and 10 mg/kg |
| Administration: | Intraperitoneal injection (Pharmacokinetic study) |
| Result: | Suppressed conditioned place preference (CPP) acquisition and expression in both naïve and dependent mice significantly. |