Carebastine-d5

Carebastine-d₅ is intended for use as an internal standard for the quantification of carebastine by GC- or LC-MS. Carebastine is an active metabolite of ebastine and a histamine H₁ receptor antagonist (K_i = 75.86 nM). It inhibits histamine-induced contraction of isolated guinea pig trachea (IC₅₀ = 120 nM). 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.

Off-White Solid

The active labelled carboxylic acid metabolite of Ebastine.

H₁ Receptor

[1] J. VINCENT. The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.[J]. British journal of clinical pharmacology, 1988, 26 5: 497-502. DOI: 10.1111/j.1365-2125.1988.tb05288.x
[2] KWANG-HYEON LIU. Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: major roles for CYP2J2 and CYP3A.[J]. Drug Metabolism and Disposition, 2006, 34 11: 1793-1797. DOI: 10.1124/dmd.106.010488
[3] SHIGERU HISHINUMA . Asp73-dependent and -independent regulation of the affinity of ligands for human histamine H1 receptors by Na+[J]. Biochemical pharmacology, 2017, 128: Pages 46-54. DOI: 10.1016/j.bcp.2016.12.021
[4] I YAKUO. [Pharmacological study of ebastine, a novel histamine H1-receptor antagonist].[J]. Folia Pharmacologica Japonica, 1994, 103 3: 121-135. DOI: 10.1254/fpj.103.121
[5] YOKO YAMAUCHI  Tatsuo S  Terumichi Fujikura. The Effect of H1 Antagonists Carebastine and Olopatadine on Histamine Induced Expression of CC Chemokines in Cultured Human Nasal Epithelial Cells[J]. Allergology International, 2007, 56 2: Pages 171-177. DOI: 10.2332/allergolint.o-06-446