Movatterモバイル変換

[0]ホーム
URL:

Jump to content
WikipediaThe Free Encyclopedia
Search

Vabicaserin

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Vabicaserin
Clinical data
Routes of
administration		By mouth
ATC code
  • None
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • (9aR,12aS)-4,5,6,7,9,9a,10,11,12,12a-Decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC15H21ClN2
Molar mass264.80 g·mol−1
3D model (JSmol)
  • C1C[C@H]2CN3CCNCC4=C3C(=CC=C4)[C@H]2C1
  • InChI=1S/C15H20N2/c1-3-11-9-16-7-8-17-10-12-4-2-5-13(12)14(6-1)15(11)17/h1,3,6,12-13,16H,2,4-5,7-10H2/t12-,13-/m0/s1 ☒N
  • Key:NPTIPEQJIDTVKR-STQMWFEESA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Vabicaserin (codenamedSCA-136) was a novelantipsychotic andanorectic under development byWyeth.[1] As of 2010 it is no longer inclinical trials for the treatment ofpsychosis.[1][2] It was also under investigation as anantidepressant but this indication appears to have been dropped as well.[3]

Vabicaserin acts as aselective5-HT2C receptorfull agonist (Ki = 3 nM; EC50 = 8 nM; IA = 100% (relative to5-HT)) and5-HT2B receptorantagonist (IC50 = 29 nM).[4][5][6] It is also a very weak antagonist at the5-HT2A receptor (IC50 = 1,650 nM), though this action is not clinically significant.[4] By activating 5-HT2C receptors, vabicaserin inhibitsdopamine release in themesolimbic pathway, likely underlying its efficacy in alleviatingpositive symptoms ofschizophrenia, and increasesacetylcholine andglutamate levels in theprefrontal cortex, suggesting benefits againstcognitive symptoms as well.[6][7][8]

See also

[edit]

References

[edit]
  1. ^ab"Search of: vabicaserin - List Results".ClinicalTrials.gov.
  2. ^Lu C, Li AP (26 January 2010).Enzyme Inhibition in Drug Discovery ... John Wiley & Sons.ISBN 9780470538944 – via Google Books.
  3. ^Kelly J (2010).Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley.ISBN 978-0-470-51979-0.
  4. ^abRosenzweig-Lipson S, Dunlop J, Marquis KL (November 2007). "5-HT2C receptor agonists as an innovative approach for psychiatric disorders".Drug News & Perspectives.20 (9):565–571.doi:10.1358/dnp.2007.20.9.1162244.PMID 18176661.
  5. ^Tong Z, Chandrasekaran A, DeMaio W, Jordan R, Li H, Moore R, et al. (April 2010). "Species differences in the formation of vabicaserin carbamoyl glucuronide".Drug Metabolism and Disposition.38 (4):581–590.doi:10.1124/dmd.109.028639.PMID 20032194.S2CID 793693.
  6. ^abRosenzweig-Lipson S, Beyer CE, Hughes Z, Lin Q, Zhang MY, Grauer S, et al."Vabicaserin: effects of a novel 5HT2C agonist on medial prefrontal cortex neurotransmission, cognition and sensorimotor gating".The Journal of the European College of Neuropsychopharmacology.17 (Supplement 4): S484.doi:10.1016/S0924-977X(07)70740-X.S2CID 54245668. Archived fromthe original on 4 March 2012.
  7. ^Stahl SM, ed. (2008).Stahl's essential psychopharmacology: neuroscientific basis and practical applications. Cambridge, UK: Cambridge University Press. p. 447.ISBN 978-0-521-85702-4.
  8. ^Albert JS (2012). Wood MW (ed.).Targets and Emerging Therapies for Schizophrenia (3rd ed.). Hoboken, New Jersey: John Wiley & Sons, Inc.ISBN 9781118309384.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Retrieved from "https://en.wikipedia.org/w/index.php?title=Vabicaserin&oldid=1254283439"
Categories:
Hidden categories:
[8]ページ先頭
©2009-2025 Movatter.jp