Antazoline (hydrochloride)

Antazoline is a histamine H1 receptor antagonist that binds to histamine H1receptors with a Ki value of 38.4 nM in cell membranes expressing human recombinant H1 receptors. Antazoline reduces histamine-induced IL-6 and IL-8 production in human conjunctival epithelial cells (IC50s = 1 and 0.652 µM, respectively). It completely prevents anaphylaxis in rabbits sensitized to egg albumin and increases survival in a guinea pig model of histamine-induced bronchospasm. Antazoline (10-30 µM) eliminates atrial fibrillation induced by acetylcholine and isoproterenol (Cay-15592) in isolated rabbit hearts by increasing the atrial effective refractory period and interatrial conduction time in a dose-dependent manner. Antazoline also binds to NMDA receptors (Ki = 13 µM) and reduces glutamate-induced toxicity in cerebellar granule cells (EC50 = 13 µM).Formal Name: 4,5-dihydro-N-phenyl-N-(phenylmethyl)-1H-imidazole-2-methanamine, monohydrochloride. CAS Number: 2508-72-7. Synonyms: 2-(N-Benzylanilinomethyl)-2-imidazoline. Molecular Formula: C17H19N3 . HCl. Formula Weight: 301.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, Ethanol: 25 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 244, 289 nm. SMILES: C1(CN(CC2=NCCN2)C3=CC=CC=C3)=CC=CC=C1.Cl. InChi Code: InChI=1S/C17H19N3.ClH/c1-3-7-15(8-4-1)13-20(14-17-18-11-12-19-17)16-9-5-2-6-10-16,/h1-10H,11-14H2,(H,18,19),1H. InChi Key: SWKDMSRRIBZZAY-UHFFFAOYSA-N.