A partial agonist of the GABAA receptor
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AWD 131-138

Item No. 16235

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(4-chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one
CAS Number
188116-07-6
Synonyms
  • ELB138
  • Imepitoin
Molecular Formula
C13H14ClN3O2
Formula Weight
279.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.25 mg/ml
λmax
229, 271 nm
SMILES
O=C1N(C2=CC=C(Cl)C=C2)CC(N3CCOCC3)=N1
InChi Code
InChI=1S/C13H14ClN3O2/c14-10-1-3-11(4-2-10)17-9-12(15-13(17)18)16-5-7-19-8-6-16/h1-4H,5-9H2
InChi Key
IQHYCZKIFIHTAI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $117

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    10 mg

    $218

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    25 mg

    $514

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    50 mg

    $909

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    Product Description

    AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.1 This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).1 AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.2,3,4 It has a superior pharmacokinetic profile in dogs vs. humans.3,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sigel, E., Baur, R., Netzer, R., et al. The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABAA receptor through the benzodiazepine binding site. Neurosci. Lett. 245(2), 85-88 (1998).

    2. Rundfeldt, C., Gasparic, A., and Wlaz, P. Imepitoin as novel treatment option for canine idiopathic epilepsy: Pharmacokinetics, distribution, and metabolism in dogs. J. Vet. Pharmacol. Ther. 37(5), 421-434 (2015).

    3. Rundfeldt, C., and Löscher, W. The pharmacology of imepitoin: The first partial benzodiazepine receptor agonist developed for the treatment of epilepsy. CNS Drugs 28(1), 29-43 (2014).

    4. Yasar, S., Bergman, J., Munzar, P., et al. Evaluation of the novel antiepileptic drug, AWD 131-138, for benzodiazepine-like discriminative stimulus and reinforcing effects in squirrel monkeys. Eur. J. Pharmacol. 465(3), 257-265 (2003).

    5. Patterson, E.E. Canine epilepsy: An underutilized model. ILAR J. 55(1), 182-186 (2014).