Preladenant

Preladenant
Clinical data
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
IUPAC name
  • 2-(2-Furanyl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.210.813
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Chemical and physical data
FormulaC25H29N9O3
Molar mass503.567 g·mol−1
3D model (JSmol)
SMILES
  • COCCOc(cc4)ccc4N(CC3)CCN3CCn(c2nc1N)ncc2c(n5)n1nc5-c6occc6
InChI
  • InChI=1S/C25H29N9O3/c1-35-15-16-36-19-6-4-18(5-7-19)32-11-8-31(9-12-32)10-13-33-23-20(17-27-33)24-28-22(21-3-2-14-37-21)30-34(24)25(26)29-23/h2-7,14,17H,8-13,15-16H2,1H3,(H2,26,29) ☒N
  • Key:DTYWJKSSUANMHD-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Preladenant (SCH 420814) was a drug that was developed by Schering-Plough which acted as a potent and selective antagonist at the adenosine A2A receptor. It was being researched as a potential treatment for Parkinson's disease.[1] Positive results were reported in Phase II clinical trials in humans,[2] but it did not prove itself to be more effective than a placebo during Phase III trials, and so was discontinued in May 2013.[3]

References

  1. Hodgson RA, Bertorelli R, Varty GB, Lachowicz JE, Forlani A, Fredduzzi S, Cohen-Williams ME, Higgins GA, Impagnatiello F, Nicolussi E, Parra LE, Foster C, Zhai Y, Neustadt BR, Stamford AW, Parker EM, Reggiani A, Hunter JC (March 2009). "Characterization of the Potent and Highly Selective A2A Receptor Antagonists Preladenant and SCH 412348 in Rodent Models of Movement Disorders and Depression". The Journal of Pharmacology and Experimental Therapeutics. 330 (1): 294–303. doi:10.1124/jpet.108.149617. PMID 19332567. S2CID 22033475.
  2. Hauser, R. A.; Cantillon, M.; Pourcher, E.; Micheli, F.; Mok, V.; Onofrj, M.; Huyck, S.; Wolski, K. (2011). "Preladenant in patients with Parkinson's disease and motor fluctuations: a phase 2, double-blind, randomised trial". The Lancet Neurology. 10 (3): 221–229. doi:10.1016/S1474-4422(11)70012-6. PMID 21315654. S2CID 39226234.
  3. http://bigstory.ap.org/article/merck-ends-development-parkinsons-disease-drug


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