Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H11N5O |
Molecular Weight | 301.3021 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C(C1=C2N=CC=C(N2N=C1)C3=CC=NC=C3)C4=NC=CC=C4
InChI
InChIKey=OQJFBUOFGHPMSR-UHFFFAOYSA-N
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
Molecular Formula | C17H11N5O |
Molecular Weight | 301.3021 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/15870187Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800001407
https://en.wikipedia.org/wiki/Ocinaplon
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15870187
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800001407
https://en.wikipedia.org/wiki/Ocinaplon
Ocinaplon is anxiolytic in rodents and primates, including humans, with a magnitude of effect comparable to benzodiazepines. It was evaluated to treat Generalised anxiety disorder. The mechanism of action by which ocinaplon produces its anxiolytic effects is by allosteric modulating of GABA-A receptors. The serious adverse event detected in the ocinaplon group was icterus following transaminase elevations. Due to liver complications that occurred in Phase III, development of ocinaplon is discontinued.
Originator
Approval Year
PubMed
Title | Date | PubMed |
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Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. | 2003 Aug |
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Gateways to clinical trials. | 2003 Jul-Aug |
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Gateways to clinical trials. | 2004 Jan-Feb |
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GABA-A receptor modulators: can they offer any improvement over benzodiazepines in the treatment of anxiety disorders? | 2010 Apr |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20041911
90 mg three times a day
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15870187
Ocinaplon was ≈3-fold more potent in inhibiting [3H]flunitrazepam binding to rat cerebellum than cortex (IC50 values of 1.2 μM and 3.8 μM, respectively, with Hill coefficients 0.9 and 0.7 in cerebellum and cortex, respectively).
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:37:20 GMT 2023
by
admin
on
Fri Dec 15 15:37:20 GMT 2023
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Record UNII |
2H6KVC5E76
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Record Status |
Validated (UNII)
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Record Version |
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C28197
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SUB09398MIG
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OCINAPLON
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2H6KVC5E76
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C501948
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96604-21-6
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Related Record | Type | Details | ||
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TARGET->POSITIVE ALLOSTERIC MODULATOR (PAM) |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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