Description
CHF5407 is a potent, long-acting, and selective muscarinic M3 receptor antagonist.
Uses
CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity[1].
in vivo
CHF5407 (0.1, 0.3, 1 nmol/kg; intratracheally; 100 ul; sigle dose) exerted a dose-dependent and potent inhibition of ACh-induced (20 g/kg; i.v.) bronchospasm, with an ED50 value of 0.15 nmol/kg in guinea pigs (450-550 g)[1].
References
[1] G Villetti, et al. Bronchodilator activity of (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino] carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407), a potent, long-acting, and selective muscarinic M3 rec DOI:
10.1124/jpet.110.170035
![1-Azoniabicyclo[2.2.2]octane, 3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino]carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-, bromide,(3R)- Structure](https://www.chemicalbook.com/CAS/20180601/GIF/1004312-94-0.gif)
