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CAS号:188116-07-6
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英文名称:1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one
分子式
C13H14ClN3O2
分子量
280
EINECS号
200-256-5
MDL
MFCD18450225
Smiles
InChIKey
乙二醇化学百科
基本信息
物化性质
安全信息
生产及用途
Imepitoin (AWD 131-138) 是低亲和力的部分苯二氮(benzodiazepine)受体激动剂,有抗痉挛和抗焦虑作用。 GABA receptor 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].
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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