Ocinaplon

Ocinaplon: Ocinaplon

Systematic (IUPAC) name

pyridin-2-yl-(7-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-3-yl)methanone

Clinical data

Pregnancy cat. ?

Legal status ?

Identifiers

CAS number 96604-21-6

ATC code None

PubChem CID 216456

ChemSpider 187602^Y

UNII 2H6KVC5E76^Y

KEGG D02617^Y

Chemical data

Formula C₁₇H₁₁N₅O

Mol. mass 301.302 g/mol

SMILES eMolecules & PubChem

InChI

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^Y
Key:OQJFBUOFGHPMSR-UHFFFAOYSA-N^Y

Y(what is this?) (verify)

Ocinaplon is an anxiolytic drug in the pyrazolopyrimidine family of drugs. Other pyrazolopyrimidine drugs include zaleplon and indiplon.

Ocinaplon has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and relatively little sedative or amnestic effect.^[1]

Mechanism of action

The mechanism of action by which ocinaplon produces its anxiolytic effects is by modulating GABA_A receptors,^[2] although ocinaplon is more subtype-selective than most benzodiazepines.^[3]

Availability

Development of ocinaplon is discontinued due to liver complications that occurred in one of the Phase III subjects.^[4] However new compounds are under preclinical pipeline.^[5]

References

^ 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.

^ 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.

^ 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.

^ DOV Pharmaceuticals discontinues development of ocinaplon for GAD [Anxiety Insights]

^ www.dovpharm.com/sub_page/products_body.html

v · d · eAnxiolytics (N05B)

GABA_A PAMs

Benzodiazepine

Adinazolam • Alprazolam • Bretazenil • Bromazepam • Camazepam • Chlordiazepoxide • Clobazam • Clonazepam • Clorazepate • Clotiazepam • Cloxazolam • Diazepam • Ethyl Loflazepate • Etizolam • Fludiazepam • Halazepam • Imidazenil • Ketazolam • Lorazepam • Medazepam • Nordazepam • Oxazepam • Pinazepam • Prazepam

Carbamates

Emylcamate • Mebutamate • Meprobamate (Carisoprodol, Tybamate) • Phenprobamate • Procymate

Nonbenzodiazepines

Abecarnil • Adipiplon • Alpidem • CGS-8216 • CGS-9896 • CGS-13767 • CGS-20625 • Divaplon • ELB-139 • Fasiplon • GBLD-345 • Gedocarnil • L-838,417 • NS-2664 • NS-2710 • Ocinaplon • Pagoclone • Panadiplon • Pipequaline • RWJ-51204 • SB-205,384 • SL-651,498 • Taniplon • TP-003 • TP-13 • TPA-023 • Y-23684 • ZK-93423

Pyrazolopyridines

Cartazolate • Etazolate • ICI-190,622 • Tracazolate

Others

Chlormezanone • Ethanol (Alcohol) • Etifoxine • Kavalactones (Kava Kava) • Skullcap • Valerenic Acid (Valerian)

α₂δ VDCC Blockers
Gabapentin • Pregabalin

5-HT_1A Agonists
Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Oxaflozane

H₁ Antagonists
Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine

CRH₁ Antagonists
Antalarmin • CP-154,526 • Pexacerfont • Pivagabine

NK₂ Antagonists
GR-159,897 • Saredutant

MCH₁ antagonists
ATC-0175 • SNAP-94847

mGluR₂_/₃ Agonists
Eglumegad

mGluR5 NAMs
Fenobam

TSPO agonists
DAA-1097 • DAA-1106 • Emapunil • FGIN-127 • FGIN-143

σ₁ agonists
Afobazole • Opipramol

Others
Benzoctamine • Carbetocin • Demoxytocin • Mephenoxalone • Mepiprazole • Oxanamide • Oxytocin • Promoxolane • Tofisopam • Trimetozine • WAY-267,464

^#WHO-EM. ^‡Withdrawn from market. Clinical trials: ^†Phase III. ^§Never to phase III

M: PSO/PSI

mepr

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc(eval/thrp), drug(N5A/5B/5C/6A/6B/6D)

Categories:
Pyrazolopyrimidines
Sedatives
Pyridines
Ketones

Ocinaplon

Systematic (IUPAC) name
pyridin-2-yl-(7-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-3-yl)methanone
Clinical data
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	96604-21-6
ATC code	None
PubChem	CID 216456
ChemSpider	187602^Y
UNII	2H6KVC5E76^Y
KEGG	D02617^Y
Chemical data
Formula	C₁₇H₁₁N₅O
Mol. mass	301.302 g/mol
SMILES	eMolecules & PubChem
InChI 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^Y Key:OQJFBUOFGHPMSR-UHFFFAOYSA-N^Y
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Ocinaplon

Mechanism of action

Availability

References

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Ocinaplon

Mechanism of action

Availability

References

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