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AWD 131-138
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AWD 131-138图片
CAS NO:188116-07-6
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
500mg电议
1g电议

产品介绍
AWD 131-138 (AWD 131-138) 是一种新型低亲和力部分苯二氮卓受体激动剂，在啮齿动物模型中具有有效的抗惊厥和抗焦虑特性。
Cas No.188116-07-6
别名伊匹妥英,AWD 131-138
化学名3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one
Canonical SMILESC1COCCN1C2=NC(=O)N(C2)C3=CC=C(C=C3)Cl
分子式C13H14ClN3O2
分子量279.72
溶解度DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 0.25 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AWD 131-138 is a partial agonist of benzodiazepine receptor [1].

Benzodiazepine (BZD) is a psychoactive drug and acts as positive allosteric modulators of the inhibitory neurotransmitter GABA by binding to a recognition site (BZD receptor) of the GABAA receptor chloride ionophore complex [1].

AWD 131-138 is a partial benzodiazepine receptor agonist with anticonvulsant and anxiolytic activity [1]. In Xenopus oocytes expressed recombinant γ-aminobutyric acid A (GABAA) receptors of ɑ1β2γ2, ɑ1β3γ2, ɑ2β2γ2, ɑ3β2γ2 and ɑ5β2γ2, AWD 131-138 stimulated GABA currents in a dose-dependent way and acts at the binding site for benzodiazepines. AWD 131-138 (10 μM) stimulated GABA currents up to 12-21% of the maximal stimulation achieved by diazepam [2].

In a dog seizure model, AWD 131-138 increased the pentylenetetrazole (PTZ) seizure threshold. AWD 131-138 (5 or 40 mg/kg) caused relatively mild abstinence symptoms, particularly at the lower dosage. In dogs with newly diagnosed epilepsy, AWD 131-138 significantly reduced seizure frequency and severity [3].

References:
[1].  Rundfeldt C, Loscher W. The pharmacology of imepitoin: the first partial benzodiazepine receptor agonist developed for the treatment of epilepsy. CNS Drugs, 2014, 28(1): 29-43.
[2].  Sigel E, Baur R, Netzer R, et al. The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site. Neurosci Lett, 1998, 245(2): 85-88.
[3].  Loscher W, Potschka H, Rieck S, et al. Anticonvulsant efficacy of the low-affinity partial benzodiazepine receptor agonist ELB 138 in a dog seizure model and in epileptic dogs with spontaneously recurrent seizures. Epilepsia, 2004, 45(10): 1228-1239.