By Hiroshi Kase
This e-book is the 1st definitive evaluate on adenosine receptor antagonists and their software to the remedy of Parkinson's illness. The influence of those novel non-dopamine medications on vitro and in vivo structures sincerely indicates their power for the therapy of this debilitating affliction. This booklet covers how the Parkinson's affliction antagonist drug, A2A, has been researched, built, and proven. it's an important publication for researchers attracted to the basal ganglia, purine biology, and Parkinson's sickness. Key positive factors* Discusses the invention and improvement of a singular non-dopaminomimetic agent for Parkinson's sickness* offers the 1st definitive evaluate of adenosine antagonists and their function within the remedy of Parkinson's ailment* provides 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 assessment of adenosine, its receptor subtypes, their antagonists/agonists from biochemistry, molecular biology, medicinal chemistry, body structure, pharmacology, and neurochemistry viewpoints
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Additional info for Adenosine Receptors and Parkinson's Disease
Structure-activity relationships of 8-cycloalkyl-l,3-dipropylxanthines as antagonists of adenosine receptors. J Med Chem 33, 1906-1910. G. (1996). In vivo characterization of ZM 241385, a selective adenosine A2Areceptor antagonist. EurJ Pharmaco1301,107-113. S. (1993). The diuretic action of 8-cyclopentyl-l,3dipropylxanthine, a selective A1 adenosine receptor antagonist. BrJ Pharmacol 109, 271-277. , and Karasawa, A. (1993). Diuretic effects of KW-3902 (8-(noradamantan-3-yl)-l,3-dipropylxanthine), a novel adenosine A1 receptor antagonist, in conscious dogs.
KF17837 also ameliorated the cataleptic response produced by the dopamine D2 antagonist (halopefidol). , 1991). , 1996; see Chapters 6 and 7). To establish the precise relationships of. , 1997). Two or three substitution of the phenyl moiety with methoxy or methyl at 2,3,4-, 3,4,5- and 3,4-position favored in vivo activity. Derivatives with mono substitution or a simple phenyl group showed weak activity. Surprisingly, diethyl substitution at the 1- and 3position dramatically potentiated the activity without exception presumably due to increased oral bioavailability.
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. Jpn J Pharmacol 64, 281-288. , and Dionisotti, S. (1996). The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2A adenosine receptor antagonist. J Pharmacol Exp Ther 276, 398-404. , 1996).
Adenosine Receptors and Parkinson's Disease by Hiroshi Kase