10207. Istradefylline

Nomenclature

CAS number: 155270-99-8
8-[(1E)-2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione; (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methylxanthine; KW-6002.
C20H24N4O4; mol wt 384.43.
C 62.49%, H 6.29%, N 14.57%, O 16.65%.

Description and references

Selective adenosine A2A receptor antagonist. Prepn: F. Suzuki et al., EP 590919; eidem, US 5484920 (1994, 1996 both to Kyowa). Improved prepn: J. Hockemeyer et al., J. Org. Chem. 69, 3308 (2004) DOI PubMed. Receptor binding study: L. K. Harper et al., Pharmacol. Biochem. Behav. 83, 114 (2006) DOI PubMed. Neuroprotective effects in MPTP-treated mice: M. Pierri et al., Neuropharmacology 48, 517 (2005) DOI PubMed. Clinical experience as dual therapy with levadopa: W. Bara-Jimenez et al., Neurology 61, 293 (2003) PubMed; as monotherapy in advanced Parkinson's disease: R. A. Hauser et al., ibid. 297 PubMed. Review of development and clinical experience: P. Jenner, Expert Opin. Invest. Drugs 14, 729-738 (2005) DOI PubMed.

Chemical structure

Properties

Pale yellow needles from isopropanol, mp 190.4-191.3°.

Therapeutic Category

Antiparkinsonian.

Keywords

Antiparkinsonian