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MedKoo Cat#: 526155 | Name: Ro 15-4513
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ro 15-4513 is a partial inverse agonist of benzodiazepine receptors. It acts as a competitive antagonist, and can therefore be an antidote to the acute impairment caused by alcohol. Ro 15-4513's Ki values are 3.1 and 5.3 nM for diazepam-insensitive (DI) and diazepam-sensitive (DS) benzodiazepine receptors respectively. Ro 15-4513 displays partial agonism at DI α4- and α6-GABAA receptors.

Chemical Structure

Ro 15-4513
Ro 15-4513
CAS#91917-65-6

Theoretical Analysis

MedKoo Cat#: 526155

Name: Ro 15-4513

CAS#: 91917-65-6

Chemical Formula: C15H14N6O3

Exact Mass: 326.1127

Molecular Weight: 326.32

Elemental Analysis: C, 55.21; H, 4.32; N, 25.75; O, 14.71

Price and Availability

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10mg USD 270.00
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Synonym
Ro 15-4513; Ro 154513; Ro-15-4513.
IUPAC/Chemical Name
Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylate
InChi Key
CFSOJZTUTOQNIA-UHFFFAOYSA-N
InChi Code
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
SMILES Code
CCOC(=O)C1=C2CN(C)C(=O)C3=C(C=CC(=C3)N=[N+]=[N-])N2C=N1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO and ethanol
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO and ethanol
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Ro 15-4513 is a high affinity benzodiazepine ligand. Ki values are 3.1 and 5.3 nM for diazepam-insensitive (DI) and diazepam-sensitive (DS) benzodiazepine receptors respectively. It acts as partial inverse agonist at recombinant DS α1-, α2-, α3- and α5-GABAA receptors. Ro 15-4513 displays partial agonism at DI α4- and α6-GABAA receptors. Ro 15-4513 antagonizes several behavioral and neurochemical effects of ethanol. It is a proconvulsant and anxiogenic.
In vitro activity:
Among the ligands examined in this study, Ro 15-4513 was the only substance with a diazepam-insensitive/diazepam-sensitive potency ratio approximately 1; other substances had ratios ranging from 13 to greater than 1000. Reference: Eur J Pharmacol. 1992 Jan 14;225(1):63-8. https://pubmed.ncbi.nlm.nih.gov/1311690/
In vivo activity:
This study found that Ro 15-4513 abolished the sedative effect of ethanol by an action on γ2 subunit-dependent benzodiazepine sites. Reference: Front Neurosci. 2011 Jan 20;5:3. https://pubmed.ncbi.nlm.nih.gov/21270945/
Solvent mg/mL mM
Solubility
Ethanol 1.6 5.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 326.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Wong G, Skolnick P. High affinity ligands for 'diazepam-insensitive' benzodiazepine receptors. Eur J Pharmacol. 1992 Jan 14;225(1):63-8. doi: 10.1016/0922-4106(92)90040-3. PMID: 1311690. 2. Leggio GM, Di Marco R, Gulisano W, D'Ascenzo M, Torrisi SA, Geraci F, Lavanco G, Dahl K, Giurdanella G, Castorina A, Aitta-Aho T, Aceto G, Bucolo C, Puzzo D, Grassi C, Korpi ER, Drago F, Salomone S. Dopaminergic-GABAergic interplay and alcohol binge drinking. Pharmacol Res. 2019 Mar;141:384-391. doi: 10.1016/j.phrs.2019.01.022. Epub 2019 Jan 12. PMID: 30648615. 3. Linden AM, Schmitt U, Leppä E, Wulff P, Wisden W, Lüddens H, Korpi ER. Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci. 2011 Jan 20;5:3. doi: 10.3389/fnins.2011.00003. PMID: 21270945; PMCID: PMC3026482.
In vitro protocol:
1. Wong G, Skolnick P. High affinity ligands for 'diazepam-insensitive' benzodiazepine receptors. Eur J Pharmacol. 1992 Jan 14;225(1):63-8. doi: 10.1016/0922-4106(92)90040-3. PMID: 1311690.
In vivo protocol:
1. Leggio GM, Di Marco R, Gulisano W, D'Ascenzo M, Torrisi SA, Geraci F, Lavanco G, Dahl K, Giurdanella G, Castorina A, Aitta-Aho T, Aceto G, Bucolo C, Puzzo D, Grassi C, Korpi ER, Drago F, Salomone S. Dopaminergic-GABAergic interplay and alcohol binge drinking. Pharmacol Res. 2019 Mar;141:384-391. doi: 10.1016/j.phrs.2019.01.022. Epub 2019 Jan 12. PMID: 30648615. 2. Linden AM, Schmitt U, Leppä E, Wulff P, Wisden W, Lüddens H, Korpi ER. Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci. 2011 Jan 20;5:3. doi: 10.3389/fnins.2011.00003. PMID: 21270945; PMCID: PMC3026482.
1: Lister RG, Nutt DJ. RO 15-4513 and its interaction with ethanol. Adv Alcohol Subst Abuse. 1988;7(3-4):119-23. doi: 10.1300/J251v07n03_19. PMID: 2851930. 2: Linden AM, Schmitt U, Leppä E, Wulff P, Wisden W, Lüddens H, Korpi ER. Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci. 2011 Jan 20;5:3. doi: 10.3389/fnins.2011.00003. PMID: 21270945; PMCID: PMC3026482. 3: Wong G, Skolnick P. Ro 15-4513 binding to GABAA receptors: subunit composition determines ligand efficacy. Pharmacol Biochem Behav. 1992 May;42(1):107-10. doi: 10.1016/0091-3057(92)90454-n. PMID: 1326771. 4: Corda MG, Giorgi O, Longoni B, Biggio G. Ro 15-4513, a partial inverse agonist for benzodiazepine recognition sites, has proconflict and proconvulsant effects in the rat. Eur J Pharmacol. 1989 Jan 17;159(3):233-9. doi: 10.1016/0014-2999(89)90153-2. PMID: 2537736. 5: Belzung C, Misslin R, Vogel E. Does RO 15-4513 reverse the anxiolytic effects of ethanol by its intrinsic properties? Pharmacol Biochem Behav. 1988 Aug;30(4):867-70. doi: 10.1016/0091-3057(88)90112-8. PMID: 2906436. 6: Korpi ER, Uusi-Oukari M. Cerebellar GABAA receptors and alcohol-related behaviors: focus on diazepam-insensitive [3H]Ro 15-4513 binding. Adv Biochem Psychopharmacol. 1992;47:289-99. PMID: 1324578. 7: Buczek Y, Tomkins DM, Lê AD, Sellers EM. Opposite effects of Ro 15-4513 on acquisition and maintenance of ethanol drinking behavior in male Wistar rats. Alcohol Clin Exp Res. 1997 Dec;21(9):1667-75. PMID: 9438528. 8: Koob GF, Percy L, Britton KT. The effects of Ro 15-4513 on the behavioral actions of ethanol in an operant reaction time task and a conflict test. Pharmacol Biochem Behav. 1988 Nov;31(3):757-60. doi: 10.1016/0091-3057(88)90261-4. PMID: 3251257. 9: Nutt DJ, Lister RG, Rusche D, Bonetti EP, Reese RE, Rufener R. RO 15-4513 does not protect rats against the lethal effects of ethanol. Eur J Pharmacol. 1988 Jun 22;151(1):127-9. doi: 10.1016/0014-2999(88)90701-7. PMID: 3416920. 10: Halldin C, Farde L, Litton JE, Hall H, Sedvall G. [11C]Ro 15-4513, a ligand for visualization of benzodiazepine receptor binding. Preparation, autoradiography and positron emission tomography. Psychopharmacology (Berl). 1992;108(1-2):16-22. doi: 10.1007/BF02245279. PMID: 1329130. 11: Turner DM, Sapp DW, Olsen RW. The benzodiazepine/alcohol antagonist Ro 15-4513: binding to a GABAA receptor subtype that is insensitive to diazepam. J Pharmacol Exp Ther. 1991 Jun;257(3):1236-42. PMID: 1646328. 12: Jeffreys RD, Pournaghash S, Glowa JR, Riley AL. The effects of Ro 15-4513 on ethanol-induced taste aversions. Pharmacol Biochem Behav. 1990 Apr;35(4):803-6. doi: 10.1016/0091-3057(90)90362-l. PMID: 2345759. 13: Shelton KL, Grant KA. Effects of naltrexone and Ro 15-4513 on a multiple schedule of ethanol and Tang self-administration. Alcohol Clin Exp Res. 2001 Nov;25(11):1576-85. PMID: 11707632. 14: Pringle AK, Gardner CR, Walker RJ. Different functional effect of Ro 15-4513 and Ro 19-4603 on synaptic responses of Purkinje cells in the rat cerebellar slice. Brain Res. 1994 Dec 5;665(2):222-8. doi: 10.1016/0006-8993(94)91341-2. PMID: 7895057. 15: Hiltunen AJ, Järbe TU. Effects of Ro 15-4513, alone or in combination with ethanol, Ro 15-1788, diazepam, and pentobarbital on instrumental behaviors of rats. Pharmacol Biochem Behav. 1988 Nov;31(3):597-603. doi: 10.1016/0091-3057(88)90236-5. PMID: 3150785. 16: Wood AL, Healey PA, Menéndez JA, Verne SL, Atrens DM. The intrinsic and interactive effects of RO 15-4513 and ethanol on locomotor activity, body temperature, and blood glucose concentration. Life Sci. 1989;45(16):1467-73. doi: 10.1016/0024-3205(89)90037-4. PMID: 2811603. 17: Risinger FO, Malott DH, Riley AL, Cunningham CL. Effect of Ro 15-4513 on ethanol-induced conditioned place preference. Pharmacol Biochem Behav. 1992 Sep;43(1):97-102. doi: 10.1016/0091-3057(92)90644-u. PMID: 1409822. 18: Yutrzenka GJ, Stone T, Anderson S. Ro 15-4513 alteration of pentobarbital dependence. Pharmacol Biochem Behav. 1996 Nov;55(3):379-86. doi: 10.1016/s0091-3057(96)00107-4. PMID: 8951979. 19: Prunell M, Escorihuela RM, Fernández-Teruel A, Núñez JF, Tobeña A. Differential interactions between ethanol and Ro 15-4513 on two anxiety tests in rats. Pharmacol Biochem Behav. 1994 Jan;47(1):147-51. doi: 10.1016/0091-3057(94)90124-4. PMID: 8115416. 20: Bonetti EP, Burkard WP, Gabl M, Hunkeler W, Lorez HP, Martin JR, Moehler H, Osterrieder W, Pieri L, Polc P, et al. Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol. Pharmacol Biochem Behav. 1988 Nov;31(3):733-49. doi: 10.1016/0091-3057(88)90259-6. PMID: 2855118.