泮考必利
| 中文名称 | 泮考必利 |
|---|---|
| 中文同义词 | 泮考必利;化合物 T16433 |
| 英文名称 | Pancopride |
| 英文同义词 | Pancopride;Pancoprida;Pancoprida [inn-spanish];Pancopridum;Pancopridum [inn-latin];Benzamide, 4-amino-N-1-azabicyclo[2.2.2]oct-3-yl-5-chloro-2-(cyclopropylmethoxy)-;LAS 30451 |
| CAS号 | 121650-80-4 |
| 分子式 | C18H24ClN3O2 |
| 分子量 | 349.86 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 121650-80-4.mol |
| 结构式 |  |
泮考必利 性质
| 沸点 | 502.3±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.33±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 13.56±0.20(Predicted) |
|
5-HT 3 Receptor
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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.
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.