1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMequitazineCat. No.: HY-B2168CAS No.: 29216-28-2Synonyms: LM-209分式: CHNS分量: 322.47作靶點(diǎn): Histamine Receptor作通路: GPCR/G Protein; Immunology/Inflammation; NeuronalSignaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-2

2、0C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 16 mg/mL (49.62 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.1011 mL 15.5053 mL 31.0106 mL5 mM 0.6202 mL 3.1011 mL 6.2021 mL10 mM 0.3101 mL 1.5505 mL 3.1011 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Mequita

3、zine種有效的，依賴性和長效的組胺H1拮抗劑。體外研究Mequitazine is a potent H1-receptors selective antihistaminic drug widely studied and used for allergicdisorders such as hay fever and urticaria 1. Mequitazine demonstrates significant bactericidal effectsagainst all the tested clinical isolates including Ps. aeruginosa.

4、Its effect against the Gram-positive isolates is1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEmore pronounced 2.體內(nèi)研究 Mequitazine and clemizole antagonize the effect of histamine in guinea-pig ileum competitively. Mequitazineat 107 produces a parallel shift of the dose-response curve to acetylchol

5、ine in the rat duodenum. Mequitazineat highest concentration shows anticholinergic activity 3. Mequitazine inhibits contractile responses to KCl,phenylephrine (PE), 5-hydroxytryptamine (5-HT), and Ca2+ in rat aorta 4.REFERENCES1. Gonnot V, et al. Expedient synthesis of mequitazine an antihistaminic

6、drug by palladium catalyzed allylic alkylation of sodiumphenothiazinate. Chem Pharm Bull (Tokyo). 2009 Nov;57(11):1300-2.2. El-Nakeeb MA, et a. In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistantclinical isolates. Braz J Microbiol. 2011

7、Jul;42(3):980-91.3. Martinez-Mir I, et al. Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole. J Pharm Pharmacol. 1988Sep;40(9):655-6.4. Satake N, et al. Possible mechanisms of vasoinhibitory effects of mequitazine, an antiallergic agent, on the contractions of isolated rataorta induced by K+, phenylephrine, 5-hydroxytryptamine, and Ca2+. J Cardiovasc Pharmacol. 1994 Apr;23(4):669-73.McePdfHeightCaution: Product has not been fully validated for medical applications.For rese