Mequitazine  (Synonyms: 美喹他嗪; LM-209)

Mequitazine is a potent, and long-acting histamine H₁ antagonist.

Mequitazine is a potent H₁-receptors selective antihistaminic drug widely studied and used for allergic disorders such as hay fever and urticaria^[1]. Mequitazine demonstrates significant bactericidal effects against all the tested clinical isolates including Ps. aeruginosa. Its effect against the Gram-positive isolates is more pronounced^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[3]. Mequitazine inhibits contractile responses to KCl, phenylephrine (PE), 5-hydroxytryptamine (5-HT), and Ca²⁺ in rat aorta^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

322.47

C₂₀H₂₂N₂S

29216-28-2

固体

White to off-white

美喹他嗪；甲喹吩嗪；甲噻吩嗪；玻丽玛朗

Room temperature in continental US; may vary elsewhere.

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

• [1]. 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.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. Martinez-Mir I, et al. Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole. J Pharm Pharmacol. 1988 Sep;40(9):655-6.  [Content Brief]

  [4]. 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.  [Content Brief]