2014年8月17日星期日

AWD 131-138(Imepitoin)|cas 188116-07-6| DC Chem|Supplier|Price|Buy  

AWD 131-138(Imepitoin)|cas 188116-07-6| DC Chem|Supplier|Price|Buy
DC Chemicals Supply: AWD 131-138(Imepitoin)|cas 188116-07-6,Purity: >98% ,Cat No. DC7071, In stock.

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AWD 131-138(Imepitoin)|cas 188116-07-6 ,Synonym: Imepitoin; AWD131-138  ,Chemical name:  ,Molecular Formula: C13H14ClN3O2 ,MW:279.72

AWD 131-138(Imepitoin), cas 188116-07-6,Purity: >98%, Best Price and quality from DC Chemicals. AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

AWD 131-138 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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