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ORG-12962

From Wikipedia, the free encyclopedia
(Redirected fromOrg 12962)
Chemical compound
Pharmaceutical compound
ORG-12962
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • 1-(5-trifluoromethyl-6-chloropyridin-2-yl)piperazine
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC10H11ClF3N3
Molar mass265.66 g·mol−1
3D model (JSmol)
  • C2CNCCN2c(nc1Cl)ccc1C(F)(F)F
  • InChI=1S/C10H11ClF3N3/c11-9-7(10(12,13)14)1-2-8(16-9)17-5-3-15-4-6-17/h1-2,15H,3-6H2 checkY
  • Key:QZYYPQAYSFBKPW-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

ORG-12962 is apyridinylpiperazinedrug developed byOrganon, which acts as apotent andselectiveagonist for the5-HT2receptor family, with highestaffinity at5-HT2C and lowest at5-HT2B subtypes.[1] It was developed as a potential anti-anxiety drug, but was discontinued from human trials after tests in a public speaking challenge showed that its anti-anxiety effects were accompanied by side effects such as dizziness and a "spacey" feeling, which were attributed to poor selectivityin vivo over thehallucinogenic5-HT2Areceptor.[2]

See also

[edit]

References

[edit]
  1. ^Porter RH, Benwell KR, Lamb H, Malcolm CS, Allen NH, Revell DF, Adams DR, Sheardown MJ (September 1999)."Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells".British Journal of Pharmacology.128 (1):13–20.doi:10.1038/sj.bjp.0702751.PMC 1571597.PMID 10498829.
  2. ^Monck NJ, Kennett GA (2008). "5-HT2C ligands: recent progress".Progress in Medicinal Chemistry.46:281–390.doi:10.1016/S0079-6468(07)00006-9.ISBN 9780444530189.PMID 18381128.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Simple piperazines
(no additional rings)
Phenylpiperazines
Benzylpiperazines
Diphenylalkylpiperazines
(benzhydrylalkylpiperazines)
Pyrimidinylpiperazines
Pyridinylpiperazines
Benzo(iso)thiazolylpiperazines
Tricyclics
(piperazine attached via side chain)
Others/Uncategorized


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