ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies.
ML381 (0.2 mg/kg; i.v.; single) possesses an overall acceptable DMPK profile for pharmacodynamic studies in rat, with the exception of poor metabolic stability and a potential for amide hydrolysis in plasma; as such, ML381 is best suited to use as an in vitro/electrophysiological probe[1].