Renzapride

SKU: orb1691957

Description

Renzapride (BRL 24924) is a dual-acting small molecule functioning as a 5-HT4 receptor agonist and a 5-HT3 antagonist. It is utilized in research for constipation-predominant irritable bowel syndrome (C-IBS), with applications in both in vitro receptor studies and in vivo gastrointestinal motility models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 112727-80-7
• MW: 323.82
• Purity: 99.09%
• Formula: C₁₆H₂₂ClN₃O₂
• SMILES: COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN2CCC[C@@H]1C2
• Target: 5-HT Receptor
• Solubility: DMSO:10 mg/mL (30.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.09 mM)

Bioactivity

• Target IC50:
  5-HT4 receptor:115 nM (Ki)
• In Vivo:
  Renzapride(BRL 24924)(0.5-1 mg/kg) and another 5-HT1P antagonist, N-acetyl-5-hydroxytryptamine-5-hydroxytryptamine amide (5 mg/kg), significantly increased the rate of emptying of 51Cr-labeled liquid meals from the mouse stomach.
• In Vitro:
  Renzapride was selective for serotonergic receptors and, in particular, had high affinity for human 5-HT(3) and guinea-pig 5-HT(4) receptors (K(i) 17 and 477 nm, respectively).

Storage & Handling

• Storage: 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

BRL 24924, BRL24924, BRL-24924, 5-HT4, 5HT Receptor, 5HTReceptor, 5-HT3, Renzapride

Compound Identifiers

PubChem CID

6917985