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AWD 131-138

CAT: 0013-GTR19163391-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163391-01Size:200 mg
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Description
AWD 131-138 (Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models. (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 . (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 . 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.
CAS Number
188116-07-6
Product Name Alternative
ELB138 | Imepitoin
Field of Research
Metabolism Research
Purity
>98% (HPLC)
Solubility
DMSO: 10 mM
Smiles
O=C1N=C (N2CCOCC2) CN1C3=CC=C (Cl) C=C3
Molecular Formula
C13H14ClN3O2
Molecular Weight
279.72
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1- (4-Chlorophenyl) -1,5-dihydro-4- (4-morpholinyl) -2H-imidazol-2-one

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