1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one

Name	1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one
Synonyms	IMEPITOIN Imepitoin AWD-131-138 AWD131-138 1-(4-CHLOROPHENYL)-4-MORPHOLINO-1H-IMIDAZOL-2(5H)-ONE 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one 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)- Imepitoin 1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one
CAS	188116-07-6
EINECS	200-256-5

Molecular Formula	C13H14ClN3O2
Molar Mass	279.72
Density	1.42±0.1 g/cm3(Predicted)
Melting Point	264℃ (ethanol )
Boling Point	421.8±55.0 °C(Predicted)
pKa	4.39±0.20(Predicted)
Storage Condition	2-8°C
In vitro study	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].
In vivo study	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].

Last Update：2024-01-02 23:10:35

biological activity	Imepitoin (AWD 131-138) is a low affinity partial benzodiazepine (benzodiazepine) receptor agonist with antispasmodic and antianxiety effects.
target	GABA receptor
in vitro study	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].
in vivo study	AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative dosup 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 two-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].

Last Update：2024-04-09 15:16:36

Spot supply

Product Name: 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one Visit Supplier Webpage Request for quotation
CAS: 188116-07-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

Spot supply

Wechat: 18301782025

View History

1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one Request for Quotation