LG-50643(LG-50643) - 药物靶点：mAChRs_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

mAChRs

作用机制

mAChRs拮抗剂(毒蕈碱型乙酰胆碱受体家族拮抗剂)

治疗领域

免疫系统疾病呼吸系统疾病

在研适应症-

非在研适应症

哮喘

原研机构

Laboratori Guidotti SpA

在研机构-

非在研机构

Laboratori Guidotti SpA

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C24H34INO2

InChIKeyMKEQJLITXBFUAQ-UHFFFAOYSA-M

CAS号111372-42-0

关联

100 项与 LG-50643 相关的临床结果

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100 项与 LG-50643 相关的转化医学

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100 项与 LG-50643 相关的专利（医药）

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1

项与 LG-50643 相关的文献（医药）

1994-05-01·Journal of Pharmacy and Pharmacology3区 · 医学

Selectivity of LG50643 for Postjunctional Muscarinic-receptor Subtype in the Guinea-pig Trachea

3区 · 医学

Article

作者: Renzetti, A R ; Subissi, A ; Zonta, F ; D’Agostino, G

AbstractThe effects of (±)-LG50643, a new N-quaternary tropinic ester of phenylcyclohexene carboxylic acid, endowed with a potent antimuscarinic activity, have been investigated on muscarinic receptor-mediated responses of the guinea-pig trachea to electrical field stimulation. An isolated preparation which allows the simultaneous measurement of tritiated acetylcholine release (prejunctional effect) and smooth muscle contraction (postjunctional effect) was used. The guinea-pig epithelium-deprived trachea was stimulated with 500 pulses (20 Hz, 1 ms, 9 V for 5 s, 30 s apart) in the presence of indomethacin (1 μm). Three successive pre- and postjunctional responses were observed. The potencies (– logEC50) of (±)-LG50643 for pre- and postjunctional muscarinic receptors were determined and compared with those of selective muscarinic antagonists. In addition, the affinity values of (±)-LG50643 for muscarinic-receptor subtypes were determined in radioligand binding experiments in cerebral cortex, heart and salivary glands of rat as target tissues for M1, M2 and M3 receptors, respectively. The results obtained in both functional and binding assays indicate (±)-LG50643 is a potent and selective antagonist for the M3-receptor subtype.

100 项与 LG-50643 相关的药物交易

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