| AWD 131-138GABAA receptor agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 188116-07-6 | SDF | Download SDF |
| Chemical Name | 3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one | ||
| Canonical SMILES | C1COCCN1C2=NC(=O)N(C2)C3=CC=C(C=C3)Cl | ||
| Formula | C13H14ClN3O2 | M.Wt | 279.72 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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, Löscher 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]. Löscher 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.
