Oxatomide

A histamine H1 receptor antagonist (Ki = 15 nM), selective for the histamine H1 receptor over mAChRs (Ki = 263 nM) but also inhibits 5-HT2 (Ki = 7 nM), inhibits histamine release induced by an anti-IgE antibody in isolated human lung fragments (IC50 = 4.5 nM), inhibits A23187-induced degranulation of RBL-2H3 mast cells, inhibits LPS-induced NO production in RAW 264.7 cells at 50 µM and fMLP- or PMA-induced superoxide production in isolated rat neutrophils, reduces histamine-induced vascular permeability in mice (ED50 = 2.9 mg/kg). Formulation: A solid. InChI: InChI=1S/C27H30N4O/c32-27-28-24-14-7-8-15-25(24)31(27)17-9-16-29-18-20-30(21-19-29)26(22-10-3-1-4-11-22)23-12-5-2-6-13-23/h1-8,10-15,26H,9,16-21H2,(H,28,32). InChIKey: BAINIUMDFURPJM-UHFFFAOYSA-N. SMILES: O=C(NC1=C2C=CC=C1)N2CCCN3CCN(CC3)C(C4=CC=CC=C4)C5=CC=CC=C5