中文同义词:
美喹他嗪;甲喹吩嗪;过敏美奎锭;10-(奎宁环-3-基甲基)-10H-吩噻嗪;10-(1-氮杂双环[2.2.2]辛烷-3-基甲基)-10H-吩噻嗪;美喹他嗪 标准品;10-((1R,3S,4R)-奎宁环-3-基甲基)-10H-吩噻嗪;玻丽玛朗
英文同义词:
10-(1-Azabicyclo[2.2.2]octan-3-ylmethyl)-10H-phenothiazine;10-(Quinuclidin-3-ylmethyl)-10H-phenothiazine;MQ-A-88;10-[(1R,3R)-1-azabicyclo[2.2.2]octan-3-ylMethyl]-10H-phenothiazine;10H-Phenothiazine, 10-(1-azabicyclo[2.2.2]oct-3-ylmethyl)- (9CI);Nipolazin;NSC 303612;Phenothiazine, 10-(3-quinuclidinylmethyl)- (8CI)
相关类别:
医药原料药;噻嗪;医药原料;原料药;Heterocyclic Compounds;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals
沸点
469.4±24.0 °C(Predicted)
密度
1.1330 (rough estimate)
酸度系数(pKa)
10.43±0.33(Predicted)
CAS 数据库
29216-28-2(CAS DataBase Reference)
NIST化学物质信息
Mequitazine(29216-28-2)
简介
美喹他嗪(mequitazine)由法国Aventis公司研发，商品名为Primalan，于1976年在法国上市，目前已在20多个国家销售。美喹他嗪为选择性H1受体拮抗剂，是无中枢镇静和抗胆碱能作用的长效抗组胺药，对外周H1受体有选择性拮抗作用，能抑制肥大细胞脱颗粒，调节迷走神经紧张性，从而阻止慢性过敏症状的发展。本品尚有轻度抗胆碱能作用。临床用于常年性及季节性过敏性皮炎、急慢性荨麻疹、过敏性结膜炎、虫咬性水肿、哮喘、各种皮肤瘙痒、湿疹等。
药物代谢
美喹他嗪口服吸收快，6h达峰值，t1/2为18h。口服后38h从体内清除，不易通过血-脑脊液屏障。体内分布广，血管渗透性高。肝内代谢，经胆汁排出体外。
不良反应
偶有困倦、乏力、头痛、口干、胃肠不适、视力模糊、便秘、SGOT和SGPT升高、血小板减少等。
药物相互作用
甲喹吩嗪不能与单胺氧化酶抑制剂同用。与中枢抑制药(如中枢镇静药和镇静药)合用，可使中枢抑制作用加强。
生物活性
Mequitazine (LM-209)是histamine H1拮抗剂，可与组胺竞争性结合胃肠道、血管和呼吸道效应细胞上正常H1受体。
体外研究
Mequitazine is a potent H 1 -receptors selective antihistaminic drug widely studied and used for allergic disorders such as hay fever and urticaria. Mequitazine demonstrates significant bactericidal effects against all the tested clinical isolates including Ps. aeruginosa . Its effect against the Gram-positive isolates is more pronounced.
体内研究
Mequitazine and clemizole antagonize the effect of histamine in guinea-pig ileum competitively. Mequitazine at 10 7 produces a parallel shift of the dose-response curve to acetylcholine in the rat duodenum. Mequitazine at highest concentration shows anticholinergic activity. Mequitazine inhibits contractile responses to KCl, phenylephrine (PE), 5-hydroxytryptamine (5-HT), and Ca 2+ in rat aorta.
危险品运输编号
UN 2811 6.1/PG III
