Ocinaplon
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Hodoodo CAT#: H584329

CAS#: 96604-21-6

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

Chemical Structure

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Ocinaplon
CAS# 96604-21-6
Instruction

Theoretical Analysis

Hodoodo Cat#: H584329
Name: Ocinaplon
CAS#: 96604-21-6
Chemical Formula: C17H11N5O
Exact Mass: 301.10
Molecular Weight: 301.309
Elemental Analysis: C, 67.77; H, 3.68; N, 23.24; O, 5.31

Price and Availability

Size Price Availability Quantity
10mg USD 425 2 Weeks
50mg USD 1450 2 Weeks
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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:

Biological target:
In vitro activity:
In vivo activity:

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:
In vitro protocol:
In vivo protocol:

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1: 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. PubMed PMID: 18554397; PubMed Central PMCID: PMC2529273.

2: 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. PubMed PMID: 20041911.

3: 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. Epub 2005 May 3. PubMed PMID: 15870187; PubMed Central PMCID: PMC1129138.

4: 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. PubMed PMID: 20415836.

5: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Dec;25(10):831-55. PubMed PMID: 14735233.

6: 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. PubMed PMID: 21762686.

7: 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. Epub 2005 Dec 8. PubMed PMID: 16339395.

8: 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. Review. PubMed PMID: 12871032.

9: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506. PubMed PMID: 12949633.

10: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2004 Jan-Feb;26(1):53-84. Review. PubMed PMID: 14988742.

11: 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. Review. PubMed PMID: 15926867.

12: 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. Review. PubMed PMID: 22981367; PubMed Central PMCID: PMC3482271.