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- GABA Receptor
- AWD 131-138
AWD 131-138
A partial agonist of the GABAA receptor
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
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包装价格促销价数量
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10mg￥1300.001040.00- +
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5mg￥662.00530.00- +
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25mg￥3175.002540.00- +
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50mg￥4312.003450.00- +
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500mg￥15025.0012020.00- +
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1g￥26087.0020870.00- +
- 货号: ajci6190
- CAS: 188116-07-6
- 别名: 伊匹妥英,AWD 131-138
- 分子式: C13H14ClN3O2
- 分子量: 279.72
- 纯度: ＞98%
- 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: Store at -20°C
- 库存: 现货
Background
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].
参考文献:
[1].? Rundfeldt C, L?scher 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].? L?scher 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.
