Pancopride(LAS 30451) is a novel, orally available, long-acting, selective 5-HT3 receptor antagonist that blocks nitrogen mustard and dacarbazine-induced vomiting.

5-HT3 receptor:0.40 nM (Ki)

Pancopride, a new potent and selective 5-HT3 receptor antagonist, is effective orally and parenterally against cytotoxic drug-induced emesis. It exhibited high affinity (Ki=0.40 nM) for [3H]GR65630-labelled 5-HT3 recognition sites in membranes from the cortex of rat brains[2].

Pancopride, when administered i.v. 5 minutes before 5-HT challenge, antagonizes 5-HT-induced bradycardia in anaesthetized rats (ID50=0.56 μg/kg) and, when given p.o. 60 minutes before 5-HT challenge, displays similar antagonistic effects (ID50=8.7 μg/kg). A single oral dose of Pancopride (10 μg/kg) significantly inhibits the bradycardic reflex over an 8-hour period. In dogs, Pancopride dose-dependently inhibits the number of vomiting episodes and delays the onset of vomiting induced by cisplatin (ID50=3.6 μg/kg i.v. and 7.1 μg/kg p.o.)[1]. Pancopride not only inhibits vomiting induced by cisplatin in dogs but is also effective in blocking mechloretamine- and dacarbazine-induced emesis without exhibiting any antidopaminergic activity. Additionally, Pancopride stimulates gastric emptying of glass beads in rats (DE50=0.032 mg/kg p.o.). Furthermore, Pancopride (1 mg/kg i.p.) reverses cisplatin-induced slowing of gastric emptying in rats[1].