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 ;
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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, 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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[pmid19332567-1] 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.

[2] 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.

[3] "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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