Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist.

M5 mAChR:0.13 nM（Ki）, M3 mAChR:0.06 nM（Ki）, M1 mAChR:0.16 nM（Ki）, M4 mAChR:0.05 nM（Ki）, M2 mAChR:0.15 nM（Ki）

Mice:Age-matched male BALB/c mice (23-25 gm) are pretreated intranasally (50 μL per mouse) with vehicle (0.9% saline) or Umeclidinium bromide at intervals (0.25-48 hours) prior to methacholine challenge, and placed into individual plethysmograph chambers. Fresh air is supplied by bias flow pumps to the chambers. After baseline respiratory [enhanced pause (Penh)] values are collected, the mice received methacholine (30 mg/mL or EC80) by aerosol delivery (flow=1.6 mL/min×2 minutes). An average Penh is then calculated for 5 minutes. Penh=[(expiratory time/relaxation time)?1]×(peak expiratory flow/peak inspiratory flow), and relaxation time is the amount of time required for 70% of the tidal volume to expire. In some cases, animals are treated on multiple, consecutive days as described in the figure legends. The data are expressed as the mean±S.E.M. percent inhibition of Penh or (mean Penh value of vehicle treated group-Penh for each drug-treated animal) divided by (mean Penh value of vehicle treated group)×100%. Data are analyzed using commercially available software.

芜地溴铵, GSK573719A

DMSO: 83.3 mg/mL (163.82 mM), Sonication is recommended.

10% DMSO+90% Saline: 2 mg/mL (3.93 mM), Sonication is recommended.