2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：91917-65-6 Product Name：RO 15-4513 Synonyms：RO 15-4513;ethyl 8-azido-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate;8-Azido-5,6-dihydro-5-Methyl-6-oxo-4H-iMidazo[1,5-a][1,4]benzodiazepine-3-carboxylicacidethylester;Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylate;Tocriscreen Total EINEC: Molecular Formula：C15H14N6O3 Molecular Weight：326.31006193161
Target:
BZR[1]; ethanol[2];
In Vivo
Ro 15-4513 (i.p.; 3 mg/kg; 10 min before being tested) completely inhibits the ethanol-induced (1.8 g/kg) reduction in total locomotor activity and partly the reduction in rearing[2]. Ro 15-4513 (i.p.; 3 mg/kg; 15 min before administration of 1.5 g/kg ethanol) reverses ethanol-induced sedation in GABAA receptor δ subunit-deficient mice[2]. Animal Model: Male C57BL/6J mice[2] Dosage: 3 mg/kg Administration: I.p.; 10 min before being tested Result: Completely inhibited the ethanol-induced reduction in total locomotor activity and partly the reduction in rearing.
In Vitro
Ro15-4513 usually acts as a partial inverse agonist at GABAA receptors, except an agonist for α4 and α6 subunit-containing ones[3].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Bonetti EP, et al. Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol. Pharmacol Biochem Behav. 1988 Nov;31(3):733-49.
[2]. Suzdak PD, et al. Effects of Ro15-4513 and other benzodiazepine receptor inverse agonists on alcohol-inducedintoxication in the rat. J Pharmacol Exp Ther. 1988 Jun;245(3):880-6.
[3]. Linden AM, et al. Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci. 2011 Jan 20;5:3.
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