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Chemical Compound Review

Istradefylline     8-[(E)-2-(3,4- dimethoxyphenyl)ethenyl]- 1,3...

Synonyms: AC1NSJVH, Nouriast (TN), CHEMBL431770, SureCN633262, cc-324, ...
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Disease relevance of Istradefylline


Psychiatry related information on Istradefylline

  • RESULTS: Increasing doses of KW-6002 resulted in faster reaction times and an increase in the number of anticipatory responses [4].

High impact information on Istradefylline


Chemical compound and disease context of Istradefylline

  • RESULTS: KW-6002 administered alone produced a dose-dependent antiparkinsonian response that reached the level of efficacy of L-dopa/benserazide but was less likely to reproduce dyskinesias in these animals [5].
  • OBJECTIVE: This study examined the behavioural effects of systemic administration of the adenosine A(2A) antagonist KW-6002 in a cued reaction time task in the rat [4].
  • However, despite producing an enhanced antiparkinsonian response KW-6002 did not exacerbate L-DOPA-induced dyskinesia in MPTP-treated common marmosets previously primed to exhibit dyskinesia by prior exposure to L-DOPA [7].
  • Combined use of the adenosine A(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 [7].
  • METHODS: We evaluated the efficacy and potency of KW-6002 and other reference compounds in the selective adenosine A2A receptor agonist 2-[p-(2-carboxyethyl)phenethylamino]-5'-N-ethylcarboxamidoadenosin e (CGS 21680)-, haloperidol- or reserpine-induced catalepsy models [2].

Biological context of Istradefylline

  • The dimerization product of MSX-2 was a moderately potent nonselective A(1) and A(2A) antagonist (K(i)(A(1)) = 273 nM, K(i) (A(2A)) = 175 nM) while the dimer of the related compound KW-6002 was inactive at A(1) and only weakly active at A(2A) adenosine receptors (K(i) = 1.57 microM) [8].
  • On the other hand, KW-6002 did not alter the decreased gene expression of PPT in 6-OHDA-treated rats [9].

Anatomical context of Istradefylline


Gene context of Istradefylline

  • Consistently, the adenosine A2A receptor blockers SCH 58261 (1 - 10 mg kg(-1), i.p.) and KW 6002 (0.1 - 10 mg kg(-1), p.o.) reduced the total immobility time in the tail suspension test [12].
  • Combination of KW-6002 with the selective dopamine D2 receptor agonist quinpirole or the D1 receptor agonist SKF80723 produced an additive improvement in motor disability [7].
  • The results of these studies suggest that MAO-B inhibition may contribute to the neuroprotective potential of A(2A) receptor antagonists such as KW-6002 and open the possibility of designing dual targeting drugs that may have enhanced therapeutic potential in the treatment of PD [13].

Analytical, diagnostic and therapeutic context of Istradefylline


  1. Adenosine A2A antagonist: a novel antiparkinsonian agent that does not provoke dyskinesia in parkinsonian monkeys. Kanda, T., Jackson, M.J., Smith, L.A., Pearce, R.K., Nakamura, J., Kase, H., Kuwana, Y., Jenner, P. Ann. Neurol. (1998) [Pubmed]
  2. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Shiozaki, S., Ichikawa, S., Nakamura, J., Kitamura, S., Yamada, K., Kuwana, Y. Psychopharmacology (Berl.) (1999) [Pubmed]
  3. KW-6002 protects from MPTP induced dopaminergic toxicity in the mouse. Pierri, M., Vaudano, E., Sager, T., Englund, U. Neuropharmacology (2005) [Pubmed]
  4. The effect of the adenosine A(2A) antagonist KW-6002 on motor and motivational processes in the rat. O'Neill, M., Brown, V.J. Psychopharmacology (Berl.) (2006) [Pubmed]
  5. Antiparkinsonian effect of a new selective adenosine A2A receptor antagonist in MPTP-treated monkeys. Grondin, R., Bédard, P.J., Hadj Tahar, A., Grégoire, L., Mori, A., Kase, H. Neurology (1999) [Pubmed]
  6. Cellular and behavioural effects of the adenosine A2a receptor antagonist KW-6002 in a rat model of l-DOPA-induced dyskinesia. Lundblad, M., Vaudano, E., Cenci, M.A. J. Neurochem. (2003) [Pubmed]
  7. Combined use of the adenosine A(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. Kanda, T., Jackson, M.J., Smith, L.A., Pearce, R.K., Nakamura, J., Kase, H., Kuwana, Y., Jenner, P. Exp. Neurol. (2000) [Pubmed]
  8. Multigram-scale syntheses, stability, and photoreactions of A2A adenosine receptor antagonists with 8-styrylxanthine structure: potential drugs for Parkinson's disease. Hockemeyer, J., Burbiel, J.C., Müller, C.E. J. Org. Chem. (2004) [Pubmed]
  9. Distribution of adenosine A(2A) receptor antagonist KW-6002 and its effect on gene expression in the rat brain. Aoyama, S., Koga, K., Mori, A., Miyaji, H., Sekine, S., Kase, H., Uchimura, T., Kobayashi, H., Kuwana, Y. Brain Res. (2002) [Pubmed]
  10. Pharmacological validation of a mouse model of l-DOPA-induced dyskinesia. Lundblad, M., Usiello, A., Carta, M., Håkansson, K., Fisone, G., Cenci, M.A. Exp. Neurol. (2005) [Pubmed]
  11. Adenosine A(2A) receptor-mediated modulation of GABA and glutamate release in the output regions of the basal ganglia in a rodent model of Parkinson's disease. Ochi, M., Shiozaki, S., Kase, H. Neuroscience (2004) [Pubmed]
  12. Adenosine A2A receptor antagonists are potential antidepressants: evidence based on pharmacology and A2A receptor knockout mice. El Yacoubi, M., Ledent, C., Parmentier, M., Bertorelli, R., Ongini, E., Costentin, J., Vaugeois, J.M. Br. J. Pharmacol. (2001) [Pubmed]
  13. Inhibition of monoamine oxidase B by selective adenosine A2A receptor antagonists. Petzer, J.P., Steyn, S., Castagnoli, K.P., Chen, J.F., Schwarzschild, M.A., Van der Schyf, C.J., Castagnoli, N. Bioorg. Med. Chem. (2003) [Pubmed]
  14. Adenosine A2A receptor antagonists for Parkinson's disease: rationale, therapeutic potential and clinical experience. Hauser, R.A., Schwarzschild, M.A. Drugs & aging. (2005) [Pubmed]
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