Pancopride

SKU: orb1706846

Description

Pancopride (LAS 30451) is a long-acting, selective 5-HT3 receptor antagonist with oral bioavailability. It has been studied in preclinical research for the prevention of emesis induced by chemotherapeutic agents like nitrogen mustard and dacarbazine, with applications in cancer therapy-related investigations.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 121650-80-4
• MW: 349.86
• Purity: 93.64%
• Formula: C₁₈H₂₄ClN₃O₂
• SMILES: O=C(NC1CN2CCC1CC2)C=3C=C(Cl)C(N)=CC3OCC4CC4
• Target: 5-HT Receptor

Bioactivity

• Target IC50:
  5-HT3 receptor:0.40 nM (Ki)
• In Vivo:
  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.). 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.
• In Vitro:
  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.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5HT Receptor, 5HTReceptor, 5-HT3 receptor, 5-HT, Pancopride, LAS 30451, LAS30451, LAS-30451

Compound Identifiers

PubChem CID

71342