Preladenant

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Preladenant

Systematic (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
Clinical data
Legal status	Investigational
Routes	Oral
Identifiers
CAS number	377727-87-2^N
ATC code	None
PubChem	CID 10117987
UNII	950O97NUPO^N
Chemical data
Formula	C₂₅H₂₉N₉O₃
Mol. mass	503.555 g/mol
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
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

Adenosinergics

Receptor
ligands

Agonists	2-(1-Hexynyl)-N-methyladenosine 2-Cl-IB-MECA 2'-MeCCPA 5'-N-ethylcarboxamidoadenosine ATL-146e BAY 60–6583 CCPA CGS-21680 CP-532,903 GR 79236 LUF-5835 LUF-5845 N⁶-Cyclopentyladenosine Regadenoson SDZ WAG 994 UK-432,097

Antagonists	8-Phenyl-1,3-dipropylxanthine Acefylline Aminophylline Bamifylline Caffeine CGS-15943 8-Chlorotheophylline CPX CVT-6883 Dimethazan DPCPX Fenethylline Istradefylline KF-26777 MRE3008F20 MRS-1220 MRS-1334 MRS-1706 MRS-1754 MRS-3777 Paraxanthine Pentoxifylline Preladenant Propentofylline PSB-10 PSB-11 PSB 36 PSB-603 PSB-788 PSB-1115 Rolofylline SCH-442,416 SCH-58261 Theobromine Theophylline VUF-5574 ZM-241,385

Reuptake
inhibitors

Plasmalemmal

ENT inhibitors	Dilazep Dipyridamole Hexobendine Pentoxifylline Propentofylline Barbiturates Ethanol Benzodiazepines

Vesicular

VNT inhibitors

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