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 remedy of Parkinson's sickness. The influence of those novel non-dopamine medicinal drugs on vitro and in vivo structures sincerely indicates their strength for the remedy of this debilitating illness. This ebook covers how the Parkinson's affliction antagonist drug, A2A, has been researched, built, and confirmed. it's a vital ebook for researchers drawn to the basal ganglia, purine biology, and Parkinson's illness. Key positive aspects* 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 position within the therapy of Parkinson's disorder* 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 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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1994). In contrast, the cataleptic response is not affected by an A1 antagonist (KFM-19). 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.

A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants. J Med Chem 33, 2240-2254. -J. (1991). Striatal restricted adenosine A2 receptor (RDC8) is expressed by enkephalin but not by substance P neurons: an in situ hybridization histochemistry study. J Neurochem 57, 1062-1067. , and Kuhn, EJ. (1991). Selective A1 antagonists for treatment of cognitive deficits. Nucleosides Nucleotides 10, 1067-1076. W. (1989). Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.

J Med Chem 37, 2970-2975. B. (1980). Are methylxanthine effects due to antagonism of endogenous adenosine? Trends Pharmacol Sci 1,129-132. W. (1987). Evidence that a novel 8-phenyl-substituted xanthine derivative is a cardioselective adenosine receptor antagonist in vivo. J Cardiovasc Pharmacol 9, 396-400. , and Williams, M. (1994). Nomenclature and classification of purinoceptors. Pharmacol Rev 46, 143-156. , and Ongini, E. (1996). (E)-l-(Heterocyclyl or cyclohexyl)-2-[ 1,3,7-trisubstituted(xanthin-8-yl)]ethenes as A2Aadenosine receptor antagonists.

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