Vabicaserin

From Self-sufficiency
Jump to: navigation, search
Vabicaserin
File:Vabicaserin.png
Systematic (IUPAC) name
(9aR,12aS)-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
Clinical data
Routes of
administration		 Oral
Legal status
Legal status
  • Uncontrolled
Identifiers
CAS Number 620948-34-7
ATC code none
PubChem CID 11658860
Chemical data
Formula C15H21ClN2
Molar mass 264.79 g/mol[[Script error: No such module "String".]]
Script error: No such module "TemplatePar".Expression error: Unexpected < operator.

Vabicaserin (SCA-136) was a novel antipsychotic and anorectic under development by Wyeth.[1] As of 2010 it is no longer in clinical trials for the treatment of psychosis.[1][2] It was also under investigation as an antidepressant but this indication appears to have been dropped as well.[3]

Vabicaserin acts as a selective 5-HT2C receptor full agonist (Ki = 3 nM; EC50 = 8 nM; IA = 100% (relative to 5-HT)) and 5-HT2B receptor antagonist (IC50 = 29 nM).[4][5][6] It is also a very weak antagonist at the 5-HT2A receptor (IC50 = 1,650 nM), though this action is not clinically significant.[4] By activating 5-HT2C receptors, vabicaserin inhibits dopamine release in the mesolimbic pathway, likely underlying its efficacy in alleviating positive symptoms of schizophrenia, and increases acetylcholine and glutamate levels in the prefrontal cortex, suggesting benefits against cognitive symptoms as well.[7][6]

See also

References

Cite error: Invalid <references> tag; parameter "group" is allowed only.

Use <references />, or <references group="..." />


Antipsychotics (neuroleptics) (N05A)
Typical
Benzamides: Levosulpiride • Nemonapride • Sulpiride • Sultopride • Tiapride • Veralipride; Butyrophenones: Azaperone • Benperidol • Bromperidol • Droperidol • Fluanisone • Haloperidol • Lenperone • Moperone • Pipamperone • Spiperone • Timiperone • Trifluperidol; Diphenylbutylpiperidines: Clopimozide • Fluspirilene • Penfluridol • Pimozide; Phenothiazines: Acepromazine • Acetophenazine • Butaperazine • Carphenazine • Chloracizine • Chlorproethazine • Chlorpromazine • Cyamemazine • Dixyrazine • Fluacizine • Fluphenazine • Levomepromazine/Methotrimeprazine • Mesoridazine • Perazine • Periciazine • Perphenazine • Piperacetazine • Pipotiazine • Prochlorperazine • Promazine • Promethazine • Propiomazine • Sulforidazine • Thiethylperazine • Thiopropazate • Thioproperazine • Thioridazine • Trifluoperazine • Triflupromazine; Thioxanthenes: Chlorprothixene • Clopenthixol • Flupentixol • Thiothixene • Zuclopenthixol; Tricyclics: Amoxapine • Butaclamol • Fluotracen • Loxapine • Metitepine/Methiothepin • Octoclothiepin • Trimipramine; Others: Prothipendyl
Atypical
Others

M: PSO/PSI

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

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

Central
4-Methylamphetamine • Amfecloral • Amfepentorex • Amfepramone • Aminorex • Amphetamine • Amphetaminil • Atomoxetine • Benfluorex • Benzphetamine • Bupropion • Cathine • Cathinone • Chlorphentermine • Ciclazindol • Clobenzorex • Cloforex • Clominorex • Clortermine • Dexfenfluramine • Dextroamphetamine • Dextromethamphetamine • Dexmethylphenidate • Difemetorex • Dimethylcathinone • Diphemethoxidine • Ephedrine • Ephedra • Ethylamphetamine • Etolorex • Fenbutrazate • Fencamfamine • Fenethylline • Fenfluramine • Fenproporex • Fludorex • Fluminorex • Furfenorex • Indanorex • Khat • Levopropylhexedrine • Lisdexamfetamine • Manifaxine • Mazindol • Mefenorex • Methamphetamine • Methylphenidate • Pemoline • Pentorex (Phenpentermine) • Phendimetrazine • Phenethylamine • Phenmetrazine • Phentermine • Phenylpropanolamine • Pipradrol • Prolintane • Propylhexedrine • Pseudoephedrine • Pyrovalerone • Radafaxine • Reboxetine • Setazindol • Sibutramine • Synephrine • Tesofensine • Viloxazine • Xylopropamine • Zylofuramine
Others
Peripheral

M: NUT

cof, enz

drug(A8/11/12)

  1. ↑ 1.0 1.1 "Search of: vabicaserin - List Results - ClinicalTrials.gov". 
  2. ↑ "Enzyme Inhibition in Drug Discovery ... - Google Books". 
  3. ↑ Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 0-470-51979-7. 
  4. ↑ 4.0 4.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  5. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  6. ↑ 6.0 6.1 "ECNP-2007 CIS". 
  7. ↑ Stahl's essential psychopharmacology: neuroscientific basis and practical applications. Cambridge, UK: Cambridge University Press. 2008. ISBN 0-521-85702-3. 
Retrieved from "http://ssf.f15ijp.com/wiki/index.php?title=Vabicaserin&oldid=23894"