In vitro pharmacological profile of the A2A receptor antagonist istradefylline

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 386, Issue 11, 2013, Pages 963-972

  Saki, Mayumi ^a   Yamada, Koji ^a   Koshimura, Etsuko ^a   Sasaki, Katsutoshi ^a   Kanda, Tomoyuki ^a  

^a KYOWA HAKKO KOGYO CO LTD   (Japan)

Author keywords

Adenosine A2A receptor; Istradefylline; KW 6002; Parkinson's disease

Indexed keywords

2 [4 (2 CARBOXYETHYL)PHENETHYLAMINO]ADENOSINE 5' (N ETHYLCARBOXAMIDE); 8 CYCLOPENTYL 1,3 DIPROPYLXANTHINE; ADENOSINE A1 RECEPTOR; ADENOSINE A2A RECEPTOR; ADENOSINE A2A RECEPTOR AGONIST; ADENOSINE A2A RECEPTOR ANTAGONIST; ADENOSINE A2B RECEPTOR; ADENOSINE A3 RECEPTOR; AMINE OXIDASE (FLAVIN CONTAINING) ISOENZYME A; AMINE OXIDASE (FLAVIN CONTAINING) ISOENZYME B; CATECHOL METHYLTRANSFERASE; CYCLIC AMP; DOPAMINE RECEPTOR; IODINE 125; ISTRADEFYLLINE; RADIOLIGAND; TRITIUM;

ARTICLE; CALLITRICHINAE; CELL CULTURE; CONCENTRATION RESPONSE; DOG; DOPAMINE METABOLISM; DRUG RECEPTOR BINDING; DRUG TARGETING; ENZYME KINETICS; HUMAN; ISOTOPE LABELING; LIGAND BINDING; MOUSE; NEUROLOGIC DISEASE; NEUROTRANSMISSION; NONHUMAN; PARKINSON DISEASE; RAT; SUBSTANTIA NIGRA;

ADENOSINE A2 RECEPTOR ANTAGONISTS; ANIMALS; ANTIPARKINSON AGENTS; BRAIN; CALLITHRIX; CELL MEMBRANE; DOGS; DOPAMINE; GUINEA PIGS; HUMANS; MICE; PC12 CELLS; PURINES; RADIOLIGAND ASSAY; RATS; RECEPTORS, PURINERGIC P1; RECOMBINANT PROTEINS;

EID: 84885953512     PISSN: 00281298     EISSN: 14321912     Source Type: Journal    
DOI: 10.1007/s00210-013-0897-5     Document Type: Article

References (41)

1. Aoyama S, Kase H, Borrelli E (2000) Rescue of locomotor impairment in dopamine D2 receptor-deficient mice by an adenosine A2A receptor antagonist. J Neurosci 20(15):5848-5852
2. 2A adenosine receptor antagonists in the therapy of Parkinson's disease. Pharmacol Ther 132(3):280-299
3. Arunlakshana O, Schild HO (1959) Some quantitative uses of drug antagonists. Br J Pharmacol Chemother 14(1):48-58
4. Augood SJ, Emson PC (1994) Adenosine A2a receptor mRNA is expressed by enkephalin cells but not by somatostatin cells in rat striatum: a co-expression study. Brain Res Mol Brain Res 22(1-4):204-210
5. 2A receptor antagonist treatment of Parkinson's disease. Neurology 61(3):293-296
6. 3H]SCH58261 to coronary artery membranes. Circ Res 79(6):1153-1160
7. 2a antagonist SYN115 in Parkinson disease. J Neurosci 30(48):16284-16292
8. Boswell-Smith V, Spina D, Page CP (2006) Phosphodiesterase inhibitors. Br J Pharmacol 147(Suppl 1):S252-S257
9. 2A receptor antagonists. Neurology 61(11 Suppl 6):S62-S68
10. Ciruela F, Albergaria C, Soriano A, Cuffi L, Carbonell L, Sanchez S, Gandia J, Fernandez-Duenas V (2010) Adenosine receptors interacting proteins (ARIPs): behind the biology of adenosine signaling. Biochim Biophys Acta 1798(1):9-20
11. DeLong MR (1990) Primate models of movement disorders of basal ganglia origin. Trends Neurosci. 13(7):281-285. Hayashi N, Kinemuchi H, Kamijo K (1981) Effect of tris (hydroxymethyl) aminomethane on amine oxidase activity in dog brain, liver and serum and in human placenta. Jpn J Pharmacol. 31(5):737-746.
12. 2A receptor antagonist istradefylline in advanced PD. Neurology 61(3):297-303
13. Hayashi N, Kinemuchi H, Kamijo K. (1981) Effect of tris (hydroxymethyl) aminomethane on amine oxidase activity in dog brain, liver and serum and in human placenta. Jpn J Pharmacol. 31(5):737-46
14. Hettinger BD, Lee A, Linden J, Rosin DL (2001) Ultrastructural localization of adenosine A2A receptors suggests multiple cellular sites for modulation of GABAergic neurons in rat striatum. J Comp Neurol 431(3):331-346
15. 2A adenosine receptors from rat striatum and rat pheochromocytoma PC12 cells: characterization with radioligand binding and by activation of adenylate cyclase. Mol Pharmacol 41(2):352-359
16. 2A receptor antagonist, is active in primate models of movement disorders. Exp Neurol 225(2):384-390
17. Huynh T (2011) The Parkinson's disease market. Nat Rev Drug Discov 10(8):571-572
18. 2A receptor antagonist, for the treatment of Parkinson's disease. Expert Opin Investig Drugs 14(6):729-738
19. 2A antagonists, and Parkinson's disease. Parkinsonism Relat Disord 15(6):406-413
20. 2A antagonist: a novel antiparkinsonian agent that does not provoke dyskinesia in parkinsonian monkeys. Ann Neurol 43(4):507-513
21. 2A antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Exp Neurol 162(2):321-327
22. 2A receptor. J Physiol 508(Pt 1):95-107
23. 2A receptor antagonist istradefylline (KW-6002) reduces "off" time in Parkinson's disease: a double-blind, randomized, multicenter clinical trial (6002-US-005). Ann Neurol 63(3):295-302
24. Liu R, Guo X, Park Y, Huang X, Sinha R, Freedman ND, Hollenbeck AR, Blair A, Chen H (2012) Caffeine intake, smoking, and risk of Parkinson disease in men and women. Am J Epidemiol 175(11):1200-1207
25. Mizuno Y, Hasegawa K, Kondo T, Kuno S, Yamamoto M, Japanese Istradefylline Study Group (2010) Clinical efficacy of istradefylline (KW-6002) in Parkinson's disease: a randomized, controlled study. Mov Disord 25(10):1437-1443
26. 2A receptor antagonism and dyskinesia in Parkinson's disease. Park Dis 2012:1-8
27. 2A antagonists. Neurology 61(11 Suppl 6):S44-S48
28. 2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4- triazolo[1,5-c]pyrimidines. Bioorg Med Chem Lett 17(5):1376-1380
29. Nikodejevic B, Senoh S, Daly JW, Creveling CR (1970) Catechol-O- methyltransferase. II. A new class of inhibitors of catechol-O- methyltransferase; 3,5-dihydroxy-4-methoxybenzoic acid and related compounds. J Pharmacol Exp Ther 174(1):83-93
30. Obeso JA, Rodriguez MC, DeLong MR (1997) Basal ganglia pathophysiology. Crit Review Adv Neurol 74:3-18
31. Olah ME, Stiles GL (1995) Adenosine receptor subtypes: characterization and therapeutic regulation. Annu Rev Pharmacol Toxicol 35:581-606
32. Olanow CW (2004) The scientific basis for the current treatment of Parkinson's disease. Annu Rev Med 55:41-60
33. Olanow CW, Koller WC (1998) An algorithm (decision tree) for the management of Parkinson's disease: treatment guidelines. American Academy of Neurology. Neurology 50(3 Suppl 3):S1-S57
34. 2A receptor antagonists. Bioorg Med Chem 11(7):1299-1310
35. Pollack AE, Harrison MB, Wooten GF, Fink JS (1993) Differential localization of A2a adenosine receptor mRNA with D1 and D2 dopamine receptor mRNA in striatal output pathways following a selective lesion of striatonigral neurons. Brain Res 631(1):161-166
36. Postuma RB, Lang AE, Munhoz RP, Charland K, Pelletier A, Moscovich M, Filla L, Zanatta D, Rios Romenets S, Altman R, Chuang R, Shah B (2012) Caffeine for treatment of Parkinson disease: a randomized controlled trial. Neurology 79(7):651-658
37. Sebastiao AM, Ribeiro JA (2000) Fine-tuning neuromodulation by adenosine. Trends Pharmacol Sci 21(9):341-346
38. 2 antagonists. J Med Chem 35(12):2342-2345
39. 2A antagonists with potent anti-cataleptic activity. Bioorg Med Chem Lett 7(18):2349-2352
40. 2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berlin) 147(1):90-95
41. Stacy M, Silver D, Mendis T, Sutton J, Mori A, Chaikin P, Sussman NM (2008) A 12-week, placebo-controlled study (6002-US-006) of istradefylline in Parkinson disease. Neurology 70(23):2233-2240