AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist, which has potent anticonvulsant and anxiolytic properties in rodent models. AWD 131-138 dose-dependently stimulated GABA currents (Recombinant gamma aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted to nearly 12-21% of the maximal stimulation achieved using diazepam in average. 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).
| Molecular Weight | 279.72 |
| Formula | C13H14ClN3O2 |
| CAS Number | 188116-07-6 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related GABA Receptor Products |
|---|
| CGP7930
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. |
| 5-Aminovaleric acid
5-Aminovaleric acid is a GABA receptor antagonist. |
| L-2,4-Diaminobutyric acid dihydrochloride
L-2,4-Diaminobutyric acid dihydrochloride inhibits GABA transaminase activity, resulting in elevated GABA levels, and exhibits ex vivo antitumor activity against mouse fibrosarcoma cells. In addition, L-2,4-Diaminobutyric acid dihydrochloride can be used as an internal standard for amino acid analysis. |
| 3,4,5-Trimethoxy-trans-cinnamic acid
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. |
| NCS-382 sodium
NCS-382 (sodium) is a potent GABA receptor antagonist. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
