544450-68-2
中文名稱(chēng)
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester
英文名稱(chēng)
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester
CAS
544450-68-2
分子式
C16H16ClNO3S
分子量
337.82
MOL 文件
544450-68-2.mol
更新日期
2023/03/20 15:41:27
544450-68-2 結(jié)構(gòu)式
基本信息
中文別名
2-(4-氯苯甲酰胺基)-4-乙基-5-甲基噻吩-3-羧酸甲酯 英文別名
COR659Methyl 2-(4-chlorobenzamido)-4-ethyl-5-methylthiophene-3-carboxylate
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester
物理化學(xué)性質(zhì)
儲(chǔ)存條件4°C, away from moisture and light
溶解度DMSO: 33.33 mg/mL (98.66 mM)
形態(tài)Solid
顏色Off-white to light yellow
常見(jiàn)問(wèn)題列表
生物活性
COR659 是有效的 GABAB 的陽(yáng)性變構(gòu)調(diào)節(jié)劑 (PAM)。COR659 可緩解大鼠對(duì)酒精和巧克力的藥物成癮。體外研究
COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABA B receptor and an action at the cannabinoid CB1 receptor.
體內(nèi)研究
COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats.
COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats.
| Animal Model: | Male sP and Wistar rats. |
| Dosage: | 0, 2.5, 5 and 10 mg/kg. |
| Administration: | Intraperitoneally (administered 30 min before the start of the self-administration, reinstatement, and locomotor activity sessions.). |
| Result: |
The magnitude of the reducing effect of the compound on number oflever-responses for alcohol averaged approximately 30, 55, and 70%, in comparison to the vehicle-treated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively.
The magnitude of the reducing effect of COR659 on number of lever-responses for alcohol averaged approximately 20, 40, and 80%, in comparison to the vehicletreated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively. |