372523-75-6
中文名稱
(2S)-1-(6,7-DIMETHOXY-3,4-DIHYDRO-1H-ISOQUINOLIN-2-YL)-3,3-DIMETHYL-2-(PYRIDIN-4-YLMETHYLAMINO)BUTAN-1-ONE
英文名稱
(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
2024/12/15 19:35:15
372523-75-6 結(jié)構(gòu)式
基本信息
中文別名
化合物TCS-OX2-29(2S)-2-(4-吡啶甲基氨基)-1-(6,7-二甲氧基-1,2,3,4-四氫異喹啉-2-基)-3,3-二甲基丁烷-1-酮
英文別名
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
物理化學(xué)性質(zhì)
儲(chǔ)存條件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)
形態(tài)粉末
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
TCX-OX2-29是OX2R 拮抗劑，pKi=7.5。對(duì)hOX2R的選擇性比hOX1R高250倍以上，IC50分別為40 nM和>10000 nM。靶點(diǎn)
IC50: 40 nM ( OX 2 R ); pKi: 7.5 ( OX 2 R )
體外研究
TCS-OX2-29 inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX 2 receptor.
體內(nèi)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 na?ve 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 na?ve and dependent mice significantly. |