产品
编 号:F254614
分子式:C16H21ClN2O2
分子量:308.8
产品类型
结构图
CAS No: 207572-69-8
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产品详情
生物活性:
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.
体内研究:
Intraduodenally administered SB-203186 (0.3-3 mg/kg) to new-born Camborough piglets produced blockade of 5-HT-evoked tachycardia which was maximal after 20 min and lasted for more than 3 h with 0.3 mg/kg.SB-203186 (0.1-3mg/kg, i.v.) surmountably antagonised 5-HT-evoked tachycardia in anaesthetized Yucatan minipigs or new-born Camborough piglets with similar potency.
体外研究:
Pretreatment with SB-203186 (10 μM) enhances the 5-HT-induced contractions of the antral strips.