Ro15-4513

• CAT Number: I009091
• CAS Number: 91917-65-6
• Molecular Formula: C15H14N6O3
• Molecular Weight: 326.31
• Purity: ≥95%
• Synonyms: ethyl 8-azido-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
• InChI: InChI=1S/C15H14N6O3/c1-3-24-15(23)13-12-7-20(2)14(22)10-6-9(18-19-16)4-5-11(10)21(12)8-17-13/h4-6,8H,3,7H2,1-2H3
• InChIKey: CFSOJZTUTOQNIA-UHFFFAOYSA-N
• SMILES: CCOC(=O)C1=C2CN(C(=O)C3=C(N2C=N1)C=CC(=C3)N=[N+]=[N-])C

Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR)[1]. Ro15-4513 is a potent ethanol antagonist[2]. Ro15-4513 has anti-anxiety effect[3]. Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Ro15-4513 usually acts as a partial inverse agonist at GABAA receptors, except an agonist for α4 and α6 subunit-containing ones[3].
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].

Reference

[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.
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[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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