Novel?7 nicotinic acetylcholine receptor modulators as potential antitussive agents

被引：1

作者：

Mazurov, Anatoly ^{[1
]}

Ho, Jenny ^{[1
]}

Low, Tiffany ^{[1
]}

Hoeng, Julia ^{[1
]}

机构：

[1] Philip Morris Int, R&D Innovat Cube, Quai Jeanrenaud 5, CH-2000 Neuchatel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2023年 / 80卷

关键词：

7 nicotinic acetylcholine receptor modulator; Antitussive effect; In vivo guinea pig model; DISCOVERY; AGONIST; PATHWAY;

D O I：

10.1016/j.bmcl.2022.129067

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of alpha 7 nicotinic acetylcholine receptor (nAChR) modulators was designed and evaluated for an-titussive activity in an in vivo guinea pig model of chemically induced cough. Compound 16 at all tested doses (9.5, 3 and 1 mg/kg) significantly (p < 0.01) reduced the cumulative number of coughs and showed similar results to a positive control (codeine at 30 mg/kg). Among three different administration routes (intraperitoneal, oral and inhalation), compound 16 exerted a significant antitussive effect in guinea pigs at an inhaled dose as low as 0.4 mg/kg (p < 0.05). alpha 7 nAChR modulators may provide a novel, non-narcotic approach to therapy in pa-tients with acute and chronic cough.

引用

页数：7

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