AWD 131-138

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100 Gram	FOB Price: USD 1.0000

100 Gram

FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

AWD 131-138 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)-;I 188116-07-6

Quick Details

Appearance:off white powder
Application:CAS：188116-07-6； 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-
PackAge:100g,500g,1kg,25kg
ProductionCapacity:1000|Gram|Month
Storage:Dry seal
Transportation:shipping

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Details:

AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
IC50 Value:
Target: GABA receptor
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].
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].

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