Carebastine-d5

Carebastine-d5 is intended for use as an internal standard for the quantification of carebastine (Item No. 23076) by GC- or LC-MS. Carebastine is an active metabolite of ebastine (Item No. 15372) and a histamine H1 receptor antagonist (Ki = 75.86 nM).{24985,34756,64270} It inhibits histamine-induced contraction of isolated guinea pig trachea (IC50 = 120 nM).{64271} It also inhibits histamine release from isolated rat peritoneal mast cells and human basophils when used at concentrations ranging from 30 to 100 µM. Carebastine decreases production of chemokine (C-C motif) ligand 5 (CCL5) and CCL2 in human nasal epithelial cells isolated from patients with nasal allergies.{41052}