更新于：2024-11-09

Mequitamium iodide

甲喹碘铵

更新于：2024-11-09

概要

概要

基本信息

药物类型

小分子化药

别名

Mequitazium iodide、LG 30435、LG-30435

靶点

H1 receptor x mAChRs

作用机制

H1 receptor拮抗剂(组胺H1受体拮抗剂)、mAChRs拮抗剂(毒蕈碱型乙酰胆碱受体家族拮抗剂)

治疗领域

免疫系统疾病感染耳鼻咽喉疾病+ [1]

在研适应症-

非在研适应症

哮喘鼻炎

原研机构

Laboratori Guidotti SpA

在研机构-

非在研机构

Guidotti SRLLaboratori Guidotti SpA

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C21H25IN2S

InChIKeySWVANDLDSRKJFI-UHFFFAOYSA-M

CAS号101396-42-3

关联

100 项与甲喹碘铵相关的临床结果

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100 项与甲喹碘铵相关的转化医学

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100 项与甲喹碘铵相关的专利（医药）

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项与甲喹碘铵相关的文献（医药）

2011-04-12·The Journal of pharmacy and pharmacology3区 · 医学

Mechanisms of the Antiallergic Action of N-Methylmequitazine (LG 30435)

3区 · 医学

Article

作者: Del Monte, Marco ; Subissi, Alessandro

Abstract:

LG 30435 (N-methylmequitazine) was assayed in passive lung (PLA) and cutaneous (PCA) anaphylaxis in guinea-pigs and rats. At doses from 0.3 to 3 μmol kg−1 i.v., it produced a dose-dependent inhibition of guinea-pig PLA and of rat PCA and PLA, while the parent compound was ineffective or poorly effective up to 3 μmol kg−1. An attempt was made to elucidate the mechanism of LG 30435′s action in these anaphylactic models, by means of various antagonists. It was tentatively concluded that different mechanisms are involved in the protective action of LG 30435 in each of the three models: histamine antagonism, possibly accompanied by an inhibition of the effects of peptido-leukotrienes in guinea-pig PLA; histamine antagonism in rat PCA and 5-hydroxytryptamine antagonism in rat PLA, possibly accompanied by a mast-cell stabilizing action in both cases. LG 30435 is devoid of smooth muscle relaxant effects on the airways and its demonstrated anticholinergic and anti-PAF effects do not appear to be involved in its antiallergic action.

1994-01-01·Chirality4区 · 化学

Absolute configuration and biological activity of mequitamium iodide enantiomers

4区 · 化学

Article

作者: Paolo Dapporto ; Cristina Di Bugno ; Alessandro Subissi ; Federico Arcamone ; Stefano Manzini ; Paola Paoli ; Raffaello Giorgi

Abstract:

The enantiomers of 1‐methyl‐3‐(10H‐phenothiazine‐10‐ylmethyl)‐1‐azoniabicyclo[2,2,2]octane iodide (1) were prepared by chiral chromatographic resolution of the precursor mequitazine (2). The (+)‐(S)‐enantiomer 1b is 10‐fold more potent than (−)‐(R)‐enantiomer 1a as a histamine antagonist, while the two enantiomers show the same antimuscarinic activity in vitro. The absolute configuration of the more active dextrorotatory isomer has been determined by X‐ray analysis. Conformational analysis and molecular modeling suggest that the (+)‐(S)‐enantiomer can adopt a conformation similar to that attributed to the receptor binding conformers of classical antihistamines. © 1994 Wiley‐Liss, Inc.

1992-06-01·Pulmonary pharmacology

Effect of mequitamium iodide (LG 30435) on airway microvascular leakage in the guinea-pig

Article

作者: Abelli, L. ; Manzini, S. ; Nappi, F. ; Giachetti, A. ; Subissi, A.

Intravenous administration of mequitamium iodide (LG 30435) prevented the increase of tracheobronchial vascular permeability induced either by antigen challenge or by exogenous histamine in the guinea-pig, while it was ineffective against PAF, serotonin or capsaicin. These findings indicate that mequitamium iodide selectively interferes with the effect of histamine on airway microvascular leakage, mediated by histamine H1 receptors, and is more potent than diphenhydramine, mequitazine or astemizole. Histamine receptor antagonism is likely to be major determinant of the antiallergic activity of the compound, although additional mechanisms may be involved.

100 项与甲喹碘铵相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
哮喘	临床2期	欧洲	-	-
哮喘	临床2期	法国	-	-
哮喘	临床2期	意大利	Guidotti SRL	-
哮喘	临床2期	-	Laboratori Guidotti SpA	-
鼻炎	临床2期	欧洲	-	-
鼻炎	临床2期	法国	-	-
鼻炎	临床2期	意大利	Guidotti SRL	-