Difference between revisions of "Gepirone"
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Latest revision as of 09:50, 28 August 2010
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Systematic (IUPAC) name | |
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4,4-dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione | |
Clinical data | |
Routes of administration | Oral |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Biological half-life | 2-3 hours |
Identifiers | |
CAS Number | 83928-76-1 |
ATC code | N06AX19 (WHO) |
PubChem | CID 55191 |
Chemical data | |
Formula | C19H29N5O2 |
Molar mass | 359.46586 g/mol[[Script error: No such module "String".]] |
Gepirone (Ariza, Variza; BMY-13,805, ORG-13,011) is a psychoactive drug and research chemical of the piperazine and azapirone chemical classes. It is currently under clinical development in an extended release form as an anxiolytic and antidepressant agent. Pharmacologically, gepirone acts as a selective 5-HT1A receptor partial agonist.
Gepirone was originally developed by Bristol-Myers Squibb, but was out-licensed to Fabre-Kramer in 1993. The U.S. Food and Drug Administration (FDA) rejected approval for gepirone in 2004. It was submitted for the preregistration (NDA) phase again in May 2007 after adding additional information from clinical trials as the FDA required in 2004. However, in 2007 it once again failed to convince the FDA of its qualities for treating anxiety and depression. Fabre-Kramer and GlaxoSmithKline are evaluating the response from the FDA to determine appropriate next steps.[1]
Ormaza, V. A.; 1986, ES 8606333 .
See also
References
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GABAA PAMs |
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α2δ VDCC Blockers | |||||||||||
5-HT1A Agonists | |||||||||||
H1 Antagonists | Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine | ||||||||||
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NK2 Antagonists | |||||||||||
MCH1 antagonists | |||||||||||
mGluR2/3 Agonists | |||||||||||
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TSPO agonists | |||||||||||
σ1 agonists | |||||||||||
Others | Benzoctamine • Carbetocin • Demoxytocin • Mephenoxalone • Mepiprazole • Oxanamide • Oxytocin • Promoxolane • Tofisopam • Trimetozine • WAY-267,464 | ||||||||||
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Simple piperazines (no additional rings) | |
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Phenylpiperazines | Acaprazine • Antrafenine • Aripiprazole • Batoprazine • Bifeprunox • BRL-15,572 • Ciprofloxacin • CSP-2503 • Dapiprazole • DCPP • DMPP • Dropropizine • EGIS-12,233 • Elopiprazole • Eltoprazine • Enpiprazole • Ensaculin • Etoperidone • Flesinoxan • Flibanserin • Fluprazine • Itraconazole • Ketoconazole • Levodropropizine • Lorpiprazole • mCPP • MeOPP • Mepiprazole • Naftopidil • Naphthylpiperazine • Nefazodone • Niaprazine • Oxypertine • Pardoprunox • pCPP • pFPP • Posaconazole • PRX-00023 • S-14,506 • S-14,671 • S-15,535 • SB-258,585 • SB-271,046 • SB-357,134 • SB-399,885 • Sonepiprazole • TFMPP • Tolpiprazole • Trazodone • Urapidil • Vesnarinone • Vilazodone • WAY-100,135 • WAY-100,635 |
Benzylpiperazines | 2C-B-BZP • Befuraline • Bifeprunox • Buclizine • BZP • Chlorbenzoxamine • DBZP • Fipexide • Imatinib • MBZP • MDBZP • Meclozine • Piberaline • Piribedil • Trimetazidine • Vesnarinone |
Diphenylalkylpiperazines (benzhydrylalkylpiperazines) | Almitrine • Amperozide • BRL-15,572 • Buclizine • BW373U86 • Cetirizine • Chlorbenzoxamine • Chlorcyclizine • Cinnarizine • Clocinizine • Cyclizine • DBL-583 • Diphenylmethylpiperazine • Dotarizine • DPI-221 • DPI-287 • DPI-3290 • GBR-12,783 • GBR-12,935 • GBR-13,069 • GBR-13,098 • GBR-13,119 • Hydroxyzine • Lidoflazine • Manidipine • Meclozine • Oxatomide • SNC-80 • Vanoxerine |
Pyrimidinylpiperazines | Buspirone • Dasatinib • Eptapirone • Gepirone • Ipsapirone • Piribedil • Pyrimidinylpiperazine • Revospirone • Tandospirone • Tirilazad • Trimazosin • Umespirone • Zalospirone |
Pyridinylpiperazines | |
Benzo(iso)thiazolylpiperazines | |
Tricyclics (piperazine attached via side chain) | |
Others | 6-Nitroquipazine • Azimilide • Cinepazet • Cyclohexylpiperazine • Hexocyclium • Indinavir • JNJ-7777120 • Lodenafil • Mirodenafil • PB-28 • Quipazine • Ranolazine • SA-4503 • Sildenafil • Tadalafil • Vardenafil • VUF-6002 • Zipeprol |
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- Anxiolytics
- Piperazines
- Pyrimidines
- Azapirones
- Glutarimides
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