Clobenpropit (hydrobromide)

Clobenpropit is a selective histamine H3 receptor antagonist (Ki = 0.17 nM in rat cortical membranes). Clobenpropit (0.3, 0.1, and 3 nM) reduces inhibition of electrically induced contractions in isolated guinea pig ileum longitudinal muscle by the H3 receptor agonist (R)-alpha-methylhistamine (Cay-25601). It does not inhibit histamine-induced contractions in isolated guinea pig ileum or tachycardia in isolated right atria at concentrations up to 1 µM, indicating a lack of functional antagonist activity at H1 and H2 receptors, respectively. Clobenpropit (1 and 3 mg/kg) decreases the duration of the tonic, clonic, and convulsive coma phases of electrically induced convulsions in mice, an effect that can be blocked by (R)-alpha-methylhistamine or imetit (Cay-29517). Clobenpropit (0.1 µM) also increases GABA release and inhibits NMDA-induced neurotoxicity in primary rat cortical neurons.Formal Name: N-[(4-chlorophenyl)methyl]-carbamimidothioic acid, 3-(1H-imidazol-5-yl)propyl ester, dihydrobromide. CAS Number: 145231-35-2. Synonyms: VUF 9153. Molecular Formula: C14H17ClN4S . 2HBr. Formula Weight: 470.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 30 mg/ml, Ethanol: 2.5 mg/ml, Water: 20 mg/ml. lambdamax: 221 nm. SMILES: N=C(SCCCc1cnc[nH]1)NCc1ccc(Cl)cc1. InChi Code: InChI=1S/C14H17ClN4S/c15-12-5-3-11(4-6-12)8-18-14(16)20-7-1-2-13-9-17-10-19-13/h3-6,9-10H,1-2,7-8H2,(H2,16,18)(H,17,19). InChi Key: UCAIEVHKDLMIFL-UHFFFAOYSA-N.