act-462206 act-462206 act-462206 is a dual orexin receptor antagonist (ic50 for ox1 = 60nm, ox2 = 11nm) which has been investigated for the treatment of insomnia. in human trials, act-462206 produced dose-dependent sedative effects and was generally well tolerated, with residual sleepiness and headache being the most common adverse events. act-462206clinical dataroutes ofadministrationoraldrug classorexin receptor antagonistlegal statuslegal status investigational identifiers iupac name (2s)-n-(3,5-dimethylphenyl)-1--2-pyrrolidinecarboxamide cas number1361321-96-1pubchem cid40924317iuphar/bps9303chemspider34500438unii64ono62p28chemblchembl3597952chemical and physical dataformulac20h24n2o4smolar mass388.48 g·mol−13d model (jsmol)interactive image smiles o=c(nc=1c=c(c=c(c1)c)c)c2n(ccc2)s(=o)(=o)c3=cc=c(oc)c=c3 inchi inchi=inchi=1s/c20h24n2o4s/c1-14-11-15(2)13-16(12-14)21-20(23)19-5-4-10-22(19)27(24,25)18-8-6-17(26-3)7-9-18/h6-9,11-13,19h,4-5,10h2,1-3h3,(h,21,23)/t19-/m0/s1key:nhpqgzobhsvtaq-ibgzpjmesa-n pharmacology in humans, the sedative effects of act-462206 began 45 minutes after oral administration, and dissipated within 8 hours - consistent with a favorable pharmacodynamic profile for the treatment of insomnia. however, the pharmacokinetic profile of act-462206 diverges significantly from what would be expected based on behavioral effects. elevated plasma concentrations of act-462206 are sustained for over 24–36 hours after administration - despite behavioral measures of sedation disappearing within 8 hours of administration.