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AWD 131-138 (Synonyms: ELB138, Imepitoin)

Catalog No.GC10974

AWD 131-138 (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

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AWD 131-138 Chemical Structure

Cas No.: 188116-07-6

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10mg
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5mg
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25mg
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50mg
$360.00
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500mg
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1g
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Sample solution is provided at 25 µL, 10mM.

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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].

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.

Chemical Properties

Cas No. 188116-07-6 SDF
Synonyms ELB138, Imepitoin
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 DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 0.25 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.575 mL 17.875 mL 35.75 mL
5 mM 0.715 mL 3.575 mL 7.15 mL
10 mM 0.3575 mL 1.7875 mL 3.575 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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