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121650-80-4

中文名稱 泮考必利
英文名稱 Pancopride
CAS 121650-80-4
分子式 C18H24ClN3O2
分子量 349.86
MOL 文件 121650-80-4.mol
121650-80-4 結(jié)構(gòu)式 121650-80-4 結(jié)構(gòu)式

基本信息

中文別名
泮考必利
英文別名
LAS 30451
Pancoprida
Pancopride
Pancopridum
Pancopridum [inn-latin]
Pancoprida [inn-spanish]
Benzamide, 4-amino-N-1-azabicyclo[2.2.2]oct-3-yl-5-chloro-2-(cyclopropylmethoxy)-

物理化學(xué)性質(zhì)

沸點(diǎn)502.3±50.0 °C(Predicted)
密度1.33±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)13.56±0.20(Predicted)

常見(jiàn)問(wèn)題列表

生物活性
Pancopride 是一種新型有效的選擇性 5-HT3 受體拮抗劑。
靶點(diǎn)

5-HT 3 Receptor

體外研究

Pancopride is a new potent and selective 5-HT 3 receptor antagonist, orally and parenterally effective against cytotoxic drug-induced emesis. Pancopride displayed high affinity (K i =0.40 nM) for [ 3 H]GR65630-labelled 5-HT 3 recognition sites in membranes from the cortex of rat brains.

體內(nèi)研究

Pancopride antagonizes 5-HT-induced bradycardia in anaesthetized rats when administered i.v. 5 min (ID 50 =0.56 μg/kg) or p.o. 60 min (ID 50 =8.7 μg/kg) before 5-HT challenge. A single oral dose (10 μg/kg) of Pancopride produced a significant inhibition of the bradycardic reflex over an 8-h period. Pancopride dose dependently inhibited the number of vomiting episodes and delayed the onset of vomiting induced by cisplatin in dogs (ID 50 =3.6 μg/kg i.v. and 7.1 μg/kg p.o.). Pancopride inhibits vomiting induced by cisplatin in dogs and is also effective in blocking mechloretamine- and dacarbazine-induced emesis lacking any antidopaminergic activity. Pancopride stimulates gastric emptying of glass beads in the rat (DE 50 =0.032 mg/kg p.o.). Pancopride (1 mg/kg i.p.) also reverses cisplatin induced slowing of gastric emptying in the rat.

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