147780-50-5
Chemical Structure
(R)-(+)-Mequitazine
- CAS No.: 147780-50-5
- Formula:C20H22N2S
- Molecular Weight:322.47
IUPAC Name: (R)-10-(quinuclidin-3-ylmethyl)-10H-phenothiazine
InChIKey: HOKDBMAJZXIPGC-MRXNPFEDSA-N
SMILES: C12=CC=CC=C1N(C[C@H]3CN4CCC3CC4)C5=C(C=CC=C5)S2
Biological Activity:
(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].
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(R)-(+)-Mequitazine | (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. |
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References
- [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. [Content Brief]
- [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. [Content Brief]
