Preladenant
Chemical compound
- none
- Investigational
- 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
- 377727-87-2
N
- 10117987
- 5614
- 8293510 N
- 950O97NUPO
- D09717
- DTXSID90191219
- Interactive image
- 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-NN
N
Y (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
- ^ Hodgson RA, Bertorelli R, Varty GB, Lachowicz JE, Forlani A, Fredduzzi S, et al. (July 2009). "Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] 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.
- ^ Hauser RA, Cantillon M, Pourcher E, Micheli F, Mok V, Onofrj M, et al. (March 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.
- ^ "Merck ends development of Parkinson's disease drug". The Big Story. Associated Press. 23 May 2013. Archived from the original on 2013-06-16. Retrieved 2013-05-23.
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Purine receptor modulators
(ligands)
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| P1 (adenosine) |
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| P2 (nucleotide) |
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(blockers)
| CNTsTooltip Concentrative nucleoside transporters |
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| ENTsTooltip Equilibrative nucleoside transporters | |
| PMATTooltip Plasma membrane monoamine transporter |
(inhibitors)
| XOTooltip Xanthine oxidase | |
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| Others |
See also: Receptor/signaling modulators
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