Adenosine Receptors and Parkinson's Disease by Hiroshi Kase

By Hiroshi Kase

This publication is the 1st definitive evaluation on adenosine receptor antagonists and their software to the therapy of Parkinson's ailment. The impression of those novel non-dopamine medicinal drugs on vitro and in vivo platforms sincerely indicates their strength for the remedy of this debilitating illness. This ebook covers how the Parkinson's disorder antagonist drug, A2A, has been researched, constructed, and validated. it really is an important e-book for researchers drawn to the basal ganglia, purine biology, and Parkinson's ailment. Key positive aspects* Discusses the invention and improvement of a unique non-dopaminomimetic agent for Parkinson's illness* offers the 1st definitive evaluation of adenosine antagonists and their position within the therapy of Parkinson's sickness* offers a brand new mechanism of motion of adenosine A2A receptor antagonists in motor functionProposes a speculation of adenosine A2A receptor functionality within the striatum* entire evaluate of adenosine, its receptor subtypes, their antagonists/agonists from biochemistry, molecular biology, medicinal chemistry, body structure, pharmacology, and neurochemistry viewpoints

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W. (1986). Analogs of caffeine: antagonists with selectivity for A2 adenosine receptors. Life Sci 39, 743-750. A. (1992). Adenosine A1 and A2 receptors: structure-function relationships. Med Res Rev 12, 423-471. H. (1991). Photoisomerization dynamics of stilbenes. Chem Rev 91, 415-436. 48 J. , Stone, G. , and Cash, WD. (1987). Biochemical characterization of the triazoloquinazoline, CGS15943, a novel nonxanthine adenosine antagonist. J Pharm Exp Ther 241,414-420. , and Karasawa, A. (1994). Diuretic effects of KW-3902, a novel adenosine Al-receptor antagonist, in various models of acute renal failure in rats.

1981). However, these methylxanthines are nonselective antagonists and have weak affinity for both A1 and A2A receptors. Therefore, the role of receptor subtypes in the behavioral effects associated with methylxanthines has been unclear because of the lack of selective adenosine A2Aantagonists. Evidence has been accumulated to show that adenosine A2Areceptors have a profound influence on motor function (Ongini and Fredholm, 1996). , 1994). In contrast, the cataleptic response is not affected by an A1 antagonist (KFM-19).

T. (1986). Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors. J Med Chem 29, 1305-1308. , Gatta, E, and Ongini, E. (1994). Effects of the new A2 adenosine receptor antagonist 8FB-PTP, an 8-substituted pyrazolo-triazolo-pyridine, on in vivo. BrJ Pharmacol 112, 659-665. , and Suzuki, E (1996). Theoretical structure-activity studies of adenosine A1 ligands: requirements for receptor affinity. Bioorg Med Chem 4, 923-924. B. (1989). J Pharmacol Exp Ther 249, 31-37.

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