ORG-12962
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • 1-(5-trifluoromethyl-6-chloropyridin-2-yl)piperazine
CAS Number
PubChem CID
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 a pyridinylpiperazine drug developed by Organon, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity at 5-HT2C and lowest at 5-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 selectivity in vivo over the hallucinogenic 5-HT2A receptor.[2]

See also

References

  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.


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