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121650-80-4 121243-20-7
137765-22-1 137765-24-3

121650-80-4

121650-80-4 structure
121650-80-4 structure
  • Name: Pancopride
  • Chemical Name: 4-amino-N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-(cyclopropylmethoxy)benzamide
  • CAS Number: 121650-80-4
  • Molecular Formula: C18H24ClN3O2
  • Molecular Weight: 349.85500
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2016-05-19 21:14:12
  • Modify Date: 2024-01-10 10:36:57
  • Pancopride is a new potent and selective 5-HT3 receptor antagonist.
Name 4-amino-N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-(cyclopropylmethoxy)benzamide
Synonyms Pancopride
N-(1-azabicyclo[2.2.2]oct-3-yl)-2-cyclopropylmethoxy-4-amino-5-chlorobenzamide
pancopride
Description Pancopride is a new potent and selective 5-HT3 receptor antagonist.
Related Catalog
Target

5-HT3 receptor[1]
In Vitro Pancopride is a new potent and selective 5-HT3 receptor antagonist, orally and parenterally effective against cytotoxic drug-induced emesis. Pancopride displayed high affinity (Ki=0.40 nM) for [3H]GR65630-labelled 5-HT3 recognition sites in membranes from the cortex of rat brains[1].
In Vivo Pancopride antagonizes 5-HT-induced bradycardia in anaesthetized rats when administered i.v. 5 min (ID50=0.56 μg/kg) or p.o. 60 min (ID50=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 (ID50=3.6 μg/kg i.v. and 7.1 μg/kg p.o.)[1]. 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 (DE50=0.032 mg/kg p.o.). Pancopride (1 mg/kg i.p.) also reverses cisplatin induced slowing of gastric emptying in the rat[2].
References

[1]. Fernández AG, et al. Pancopride, a potent and long-acting 5-HT3 receptor antagonist, is orally effective against anticancer drug-evoked emesis. Eur J Pharmacol. 1992 Nov 10;222(2-3):257-64.

[2]. Grande L, et al. Lack of effect of a 5-HT3 antagonist, pancopride, on lower oesophageal sphincter pressure in volunteers. Br J Clin Pharmacol. 1995 Oct;40(4):401-3.
Molecular Formula C18H24ClN3O2
Molecular Weight 349.85500
Exact Mass 349.15600
PSA 67.59000
LogP 3.44500
Storage condition 2-8℃

Chemsrc provides CAS#:121650-80-4 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 121650-80-4 | Chemsrc address: https://www.chemsrc.com/en/baike/1199596.html

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