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	377727-87-2 ;
PubChem CID	10117987;
IUPHAR/BPS	5614;
ChemSpider	8293510 ;
UNII	950O97NUPO;
KEGG	D09717;
CompTox Dashboard (EPA)	DTXSID90191219 ;
ECHA InfoCard	100.210.813
Chemical and physical data
Formula	C25H29N9O3
Molar mass	503.567 g·mol−1
3D model (JSmol)	Interactive image;
	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) ; Key:DTYWJKSSUANMHD-UHFFFAOYSA-N ;
	(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 A_2A 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

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.
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.
http://bigstory.ap.org/article/merck-ends-development-parkinsons-disease-drug

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[pmid19332567-1] 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.

[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.

[3] ttp://bigstory.ap.org/article/merck-ends-development-parkinsons-disease-drug