136174-04-4
中文名稱
136174-04-4
英文名稱
N-(1-azabicyclo(2.2.2)octan-3-yl)-2-chloro-5a,6,7,8,9,9a-hexahydrodibenzofuran-4-carboxamide
CAS
136174-04-4
分子式
C20H25ClN2O2
分子量
360.88
MOL 文件
136174-04-4.mol
136174-04-4 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12716 英文別名
N-(1-azabicyclo(2.2.2)octan-3-yl)-2-chloro-5a,6,7,8,9,9a-hexahydrodibenzofuran-4-carboxamide4-Dibenzofurancarboxamide, N-(3S)-1-azabicyclo(2.2.2)oct-3-yl-2-chloro-5A,6,7,8,9,9A-hexahydro-, (5as,9as)-
4-Dibenzofurancarboxamide, N-(3S)-1-azabicyclo[2.2.2]oct-3-yl-2-chloro-5a,6,7,8,9,9a-hexahydro-, (5aS,9aS)- (9CI)
(5As-(4(R*),5aalpha,9aalpha))-N-1-azabicyclo(2.2.2)oct-3-yl-2-chloro-5A,6,7,8,9,9A-hexahydro-4-dibenzofurancarboxamide
4-Dibenzofurancarboxamide, N-1-azabicyclo(2.2.2)oct-3-yl-2-chloro-5A,6,7,8,9,9A-hexahydro-, (5as-(4(R*),5aalpha,9aalpha))-
物理化學(xué)性質(zhì)
沸點(diǎn)462.6±45.0 °C(Predicted)
密度1.31±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)13.83±0.20(Predicted)
常見問題列表
生物活性
RG-12915 是一種選擇性的 5-HT3 拮抗劑，IC50 值為 0.16 nM。靶點(diǎn)
|
5-HT 3 Receptor 0.16 nM (IC 50 ) |
體外研究
RG 12915 is a potent and selective displacer of binding of 5-hydroxytryptamine (5-HT3) binding sites (IC 50 value = 0.16 nM), whereas failing to displace binding of ligands for the alpha-1, alpha-2 and beta adrenergic, 5-HT1 or 5-HT2 or cholinergic-muscarinic sites with IC 50 values less than 1 μM.
體內(nèi)研究
RG 12915 has a lower ED 50 value (0.004 mg/kg) for attenuating cisplatin-induced emetic episodes in the ferret. RG 12915 (1 mg/kg, p.o.) is highly protective against cisplatin-induced emesis in the dog. RG 12915 has no significant gastroprokinetic activity in the same species.