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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[1][2].

Product Specifications

CAS Number

147780-50-5

UNSPSC

12352005

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/r-plus-mequitazine.html

Smiles

C12=CC=CC=C1N(C[C@H]3CN4CCC3CC4)C5=C(C=CC=C5)S2

Molecular Formula

C20H22N2S

Molecular Weight

322.47

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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