PeptideDB

Mequitazine-d8 hydrobromide

CAS: F: C20H15D8BrN2S W: 411.43

Mequitazine-d8 hydrobromide is deuterated labeled Mequitazine (HY-B2168). Mequitazine is a potent, and long-acting hista
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This product is for research use only, not for human use. We do not sell to patients.

Bioactivity Mequitazine-d8 hydrobromide is deuterated labeled Mequitazine (HY-B2168). Mequitazine is a potent, and long-acting histamine H1 antagonist.
Invitro 氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注,因为它可能影响药物的药代动力学和代谢谱[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Mequitazine-d8 hydrobromide 相关抗体:
In Vivo Mequitazine and clemizole antagonize the effect of histamine in guinea-pig ileum competitively. Mequitazine at 107 produces a parallel shift of the dose-response curve to acetylcholine in the rat duodenum. Mequitazine at highest concentration shows anticholinergic activity[4]. Mequitazine inhibits contractile responses to KCl, phenylephrine (PE), 5-hydroxytryptamine (5-HT), and Ca2+ in rat aorta[5]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Formula C20H15D8BrN2S
Molar Mass 411.43
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Gonnot V, et al. Expedient synthesis of mequitazine an antihistaminic drug by palladium catalyzed allylic alkylation of sodium phenothiazinate. Chem Pharm Bull (Tokyo). 2009 Nov;57(11):1300-2. [3]. El-Nakeeb MA, et a. In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates. Braz J Microbiol. 2011 Jul;42(3):980-91. [4]. Martinez-Mir I, et al. Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole. J Pharm Pharmacol. 1988 Sep;40(9):655-6. [5]. Satake N, et al. Possible mechanisms of vasoinhibitory effects of mequitazine, an antiallergic agent, on the contractions of isolated rat aorta induced by K+, phenylephrine, 5-hydroxytryptamine, and Ca2+. J Cardiovasc Pharmacol. 1994 Apr;23(4):669-73.