144625-51-4
中文名稱(chēng)
GR 113808;1-METHYL-1H-INDOLE-3-CARBOXYLIC ACID, [1-[2-[(METHYLSULFONYL)AMINO]ETHYL]-4-PIPERIDINYL]METHYL ESTER;1-[2-(METHYLSULFONYL)-AMINO]ETHYL-4-PIPERIDINYLMETHYL 1-METHYL-1H-INDOLE-3-CARBOXYLATE;GR 113808
英文名稱(chēng)
GR 113808
CAS
144625-51-4
分子式
C19H27N3O4S
分子量
393.5
MOL 文件
144625-51-4.mol
更新日期
2023/03/20 15:41:25
144625-51-4 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15414 英文別名
GR 1138081-[2-(METHYLSULFONYL)-AMINO]ETHYL-4-PIPERIDINYLMETHYL 1-METHYL-1H-INDOLE-3-CARBOXYLATE
1-Methyl-1H-indole-3-carboxylicacid,[1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyles
1-METHYL-1H-INDOLE-3-CARBOXYLIC ACID, [1-[2-[(METHYLSULFONYL)AMINO]ETHYL]-4-PIPERIDINYL]METHYL ESTER
1H-Indole-3-carboxylic acid, 1-methyl-, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester
GR 113808
1-METHYL-1H-INDOLE-3-CARBOXYLIC ACID, [1-[2-[(METHYLSULFONYL)AMINO]ETHYL]-4-PIPERIDINYL]METHYL ESTER
1-[2-(METHYLSULFONYL)-AMINO]ETHYL-4-PIPERIDINYLMETHYL 1-METHYL-1H-INDOLE-3-CARBOXYLATE
GR 113808
物理化學(xué)性質(zhì)
沸點(diǎn)572.3±53.0 °C(Predicted)
密度1.30±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMSO: 44 mg/mL, soluble
溶解度DMSO：44 mg/mL，可溶
酸度系數(shù)(pKa)11.22±0.40(Predicted)
形態(tài)solid
顏色white
常見(jiàn)問(wèn)題列表
生物活性
GR 113808 是一種有效且高度選擇性的 5-HT4 receptor 受體拮抗劑 (pKb= 8.8)。GR 113808 的選擇性是 5-HT1A，5-HT1B，5-HT2A，5-HT2C 和 5-HT3 受體的 300 倍。靶點(diǎn)
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5-HT 4 Receptor
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5-HT 1A Receptor
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5-HT 3 Receptor
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5-HT 2A Receptor
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5-HT 2C Receptor
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體內(nèi)研究
GR113808 (intraperitoneal injection; 1 mg/kg; 5-7 days starting 24 h after induction of colitis) shows a significant increase in the disease activity index (DAI),which includes evaluation of weight loss, stool consistency, and presence of fecal blood.
| Animal Model: | Mice |
| Dosage: | 1 mg/Kg |
| Administration: | Intraperitoneal ?injection; 1 mg/Kg; 5-7 days starting 24 h after induction of colitis |
| Result: | Blocked protective effects of tegaserod after induction of colitis. |