Bioactivity | (R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases[1][2]. |
CAS | 147780-50-5 |
Formula | C20H22N2S |
Molar Mass | 322.47 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Jeong SH, et al. A novel and sensitive UPLC-MS/MS method to determine mequitazine in rat plasma and urine: Validation and its application to pharmacokinetic studies. Biomed Chromatogr. 2019 Oct;33(10):e4627. [2]. Nakamura K, et al. Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes. J Pharmacol Exp Ther. 1998 Feb;284(2):437-42. PMID: 9454781. |