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MedKoo Cat#: 584329 | Name: Ocinaplon
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Description:

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

Ocinaplon appears to be a well-tolerated and effective treatment for GAD. Ocinaplon produces a rapid onset of anxiolytic action absent the side effects (e.g., dizziness, sedation) typically reported following anxiolytic doses of benzodiazepines.

Chemical Structure

Ocinaplon
Ocinaplon
CAS#96604-21-6

Theoretical Analysis

MedKoo Cat#: 584329

Name: Ocinaplon

CAS#: 96604-21-6

Chemical Formula: C17H11N5O

Exact Mass: 301.0964

Molecular Weight: 301.31

Elemental Analysis: C, 67.77; H, 3.68; N, 23.24; O, 5.31

Price and Availability

Size Price Availability Quantity
10mg USD 425.00
50mg USD 1,450.00
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Related CAS #
No Data
Synonym
Ocinaplon; CL 273,547; CL 273547; DOV 273,547
IUPAC/Chemical Name
Methanone, 2-pyri(dinyl(7-(4-pyridinyl)pyrazolo(1,5-a)pyrimidin-3-yl)-
InChi Key
OQJFBUOFGHPMSR-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H11N5O/c23-16(14-3-1-2-7-19-14)13-11-21-22-15(6-10-20-17(13)22)12-4-8-18-9-5-12/h1-11H
SMILES Code
O=C(C1=NC=CC=C1)C2=C3N=CC=C(C4=CC=NC=C4)N3N=C2
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
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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:
Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 3.0 10.00
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 301.31 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:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: Hammouda MM, Gaffer HE, Elattar KM. Insights into the medicinal chemistry of heterocycles integrated with a pyrazolo[1,5-a]pyrimidine scaffold. RSC Med Chem. 2022 Sep 8;13(10):1150-1196. doi: 10.1039/d2md00192f. PMID: 36325400; PMCID: PMC9580358. 2: Abdallah AEM, Elgemeie GH. New Route to the Synthesis of Novel Pyrazolo[1,5-a]pyrimidines and Evaluation of their Antimicrobial Activity as RNA Polymerase Inhibitors. Med Chem. 2022;18(9):926-948. doi: 10.2174/1573406418666220302092414. PMID: 35236270. 3: Skolnick P. Anxioselective anxiolytics: on a quest for the Holy Grail. Trends Pharmacol Sci. 2012 Nov;33(11):611-20. doi: 10.1016/j.tips.2012.08.003. Epub 2012 Sep 14. PMID: 22981367; PMCID: PMC3482271. 4: Vinkers CH, Olivier B, Hanania T, Min W, Schreiber R, Hopkins SC, Campbell U, Paterson N. Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2-73 in rats trained to discriminate chlordiazepoxide or zolpidem. Eur J Pharmacol. 2011 Oct 1;668(1-2):190-3. doi: 10.1016/j.ejphar.2011.06.054. Epub 2011 Jul 8. PMID: 21762686. 5: Iosifescu DV. GABA-A receptor modulators: can they offer any improvement over benzodiazepines in the treatment of anxiety disorders? CNS Neurosci Ther. 2010 Apr;16(2):61-2. doi: 10.1111/j.1755-5949.2009.00127.x. PMID: 20415836; PMCID: PMC6493848. 6: Czobor P, Skolnick P, Beer B, Lippa A. A multicenter, placebo-controlled, double-blind, randomized study of efficacy and safety of ocinaplon (DOV 273,547) in generalized anxiety disorder. CNS Neurosci Ther. 2010 Apr;16(2):63-75. doi: 10.1111/j.1755-5949.2009.00109.x. Epub 2009 Dec 22. PMID: 20041911; PMCID: PMC6493815. 7: Berezhnoy D, Gravielle MC, Downing S, Kostakis E, Basile AS, Skolnick P, Gibbs TT, Farb DH. Pharmacological Properties of DOV 315,090, an ocinaplon metabolite. BMC Pharmacol. 2008 Jun 13;8:11. doi: 10.1186/1471-2210-8-11. PMID: 18554397; PMCID: PMC2529273. 8: Mirza NR, Rodgers RJ, Mathiasen LS. Comparative cue generalization profiles of L-838, 417, SL651498, zolpidem, CL218,872, ocinaplon, bretazenil, zopiclone, and various benzodiazepines in chlordiazepoxide and zolpidem drug discrimination. J Pharmacol Exp Ther. 2006 Mar;316(3):1291-9. doi: 10.1124/jpet.105.094003. Epub 2005 Dec 8. PMID: 16339395. 9: Atack JR. The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Expert Opin Investig Drugs. 2005 May;14(5):601-18. doi: 10.1517/13543784.14.5.601. PMID: 15926867. 10: Lippa A, Czobor P, Stark J, Beer B, Kostakis E, Gravielle M, Bandyopadhyay S, Russek SJ, Gibbs TT, Farb DH, Skolnick P. Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator. Proc Natl Acad Sci U S A. 2005 May 17;102(20):7380-5. doi: 10.1073/pnas.0502579102. Epub 2005 May 3. PMID: 15870187; PMCID: PMC1129138. 11: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2004 Jan-Feb;26(1):53-84. PMID: 14988742. 12: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Dec;25(10):831-55. PMID: 14735233. 13: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506. PMID: 12949633. 14: Atack JR. Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):213-32. doi: 10.2174/1568007033482841. PMID: 12871032.

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