AWD 131-138

GABAA receptor agonist CAS# 188116-07-6

AWD 131-138

Catalog No. BCC4045----Order now to get a substantial discount!

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Chemical structure

AWD 131-138

3D structure

Chemical Properties of AWD 131-138

Cas No. 188116-07-6 SDF Download SDF
PubChem ID 3083511 Appearance Powder
Formula C13H14ClN3O2 M.Wt 279.72
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
Chemical Name 3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one
SMILES C1COCCN1C2=NC(=O)N(C2)C3=CC=C(C=C3)Cl
Standard InChIKey IQHYCZKIFIHTAI-UHFFFAOYSA-N
Standard InChI 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
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

AWD 131-138 Dilution Calculator

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AWD 131-138 Molarity Calculator

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Preparing Stock Solutions of AWD 131-138

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.575 mL 17.875 mL 35.75 mL 71.5001 mL 89.3751 mL
5 mM 0.715 mL 3.575 mL 7.15 mL 14.3 mL 17.875 mL
10 mM 0.3575 mL 1.7875 mL 3.575 mL 7.15 mL 8.9375 mL
50 mM 0.0715 mL 0.3575 mL 0.715 mL 1.43 mL 1.7875 mL
100 mM 0.0358 mL 0.1788 mL 0.3575 mL 0.715 mL 0.8938 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on AWD 131-138

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.

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References on AWD 131-138

Evaluation of the novel antiepileptic drug, AWD 131-138, for benzodiazepine-like discriminative stimulus and reinforcing effects in squirrel monkeys.[Pubmed:12681437]

Eur J Pharmacol. 2003 Apr 4;465(3):257-65.

AWD 131-138 [1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one], a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models, was studied in squirrel monkeys trained to discriminate intramuscular (i.m.) injections of midazolam (0.3 mg/kg) from injections of vehicle. Diazepam produced midazolam-like responding at cumulative doses of 1.0 and 3.0 mg/kg i.m. and decreased rates of responding at 3.0 mg/kg (plasma levels of about 400 ng/ml). In contrast, AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). Other monkeys were trained to intravenously (i.v.) self-administer cocaine (56.0 microg/kg/injection). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels. The failure of AWD 131-138 to produce benzodiazepine-like discriminative effects and the absence of drug self-administration behavior when substituted for cocaine suggest that its abuse liability is low.

[Identity and physicochemical properties of 1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one, AWD 131-138].[Pubmed:11446164]

Pharmazie. 2001 Jun;56(6):458-61.

The structure of the anticonvulsant 1-(4-chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazolin-2-one (Code: AWD 131-138, CAS-No.: 188116-07-6) was proved by IR, UV, 1H NMR, 13C NMR and mass spectra. AWD 131-138 is practically insoluble in a neutral aqueous medium at 20 degrees C (S approximately 0.08 g/l). The solubility of the substance in 0.1 N HCl is about 2.7 g/l. In DMF, AWD 131-138 is sparingly soluble (S approximately 28.5 g/l). The pKa-value is about 2.5. The partition coefficients P = COctanol/Cwater at 37 degrees C range from 0.7 at pH approximately 1 to about 20 at pH > or = 6.

The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.[Pubmed:9605491]

Neurosci Lett. 1998 Apr 3;245(2):85-8.

Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2 were expressed in Xenopus oocytes in a functionally active form. At all subunit combinations, AWD 131-138 dose-dependently stimulated GABA currents. At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM. One micrometer of the benzodiazepine antagonist flumazenil (Ro 15-1788) counteracted the current stimulation by 10 microM AWD 131-138, indicating that this drug acts at the binding site for benzodiazepines.

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