AWD 131-138(Imepitoin)

Cas No.:	188116-07-6
Chemical Name:	Imepitoin
Synonyms:	2H-Imidazol-2-one,1-(4-chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-;AWD 131-138;3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one;AWD-131-138;Imepitoin;1-(4-CHLOROPHENYL)-4-MORPHOLINO-1H-IMIDAZOL-2(5H)-ONE;1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one;1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one;Imepitoin 1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one;2H-Imidazol-2-one, 1-(4-chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-;19V39682LI;Imepitoin [INN];Imepition;AOB2654;BCP08396;1-(4-Ch
SMILES:	ClC1C([H])=C([H])C(=C([H])C=1[H])N1C(N=C(C1([H])[H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])=O
Formula:	C13H14ClN3O2
M.Wt:	279.7222
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
In Vivo:	AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels [2]. Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model [3].
In Vitro:	AWD 131-138 dose-dependently stimulated GABA currents(Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM [1].