Ro 15-4513

Names

[ CAS No. ]:
91917-65-6

[ Name ]:
Ro 15-4513

[Synonym ]:
Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylate
Tocriscreen Total

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

BZR[1]; ethanol[2];

[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].

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₅H₁₄N₆O₃

[ Molecular Weight ]:
326.31000

[ Exact Mass ]:
326.11300

[ PSA ]:
114.18000

[ LogP ]:
1.96706

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Rats with different thresholds for DMCM-induced clonic convulsions differ in the sleep-time of diazepam and [(3)H]-Ro 15-4513 binding.

Epilepsy Res. 98(2-3) , 216-22, (2012)

The current study investigated the possible inherent relationship between convulsions and sleep involving the GABA(A)/benzodiazepine site complex. The aim of this study was to determine if rats with h...

Antagonism of the ethanol-like discriminative stimulus effects of ethanol, pentobarbital, and midazolam in cynomolgus monkeys reveals involvement of specific GABA(A) receptor subtypes.

J. Pharmacol. Exp. Ther. 331(1) , 142-52, (2009)

The gamma-aminobutyric acid (GABA)(A) receptors mediating the discriminative stimulus effects of ethanol were studied by comparing the potency of ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazol(1...

Modulation of diazepam-insensitive GABA(A) receptors by micromolar concentrations of thyroxine and related compounds in vitro.

Brain Res. 1490 , 1-8, (2013)

The effects of thyroxine and its related compounds on the benzodiazepine-insensitive γ-aminobutyric acid type A (GABA(A)) receptors were studied. Thyroxine at micromolar concentrations potentiated the...

Related Compounds

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