By Hiroshi Kase
This publication is the 1st definitive evaluation on adenosine receptor antagonists and their program to the therapy of Parkinson's sickness. The influence of those novel non-dopamine medicines on vitro and in vivo platforms basically indicates their strength for the remedy of this debilitating affliction. This booklet covers how the Parkinson's disorder antagonist drug, A2A, has been researched, built, and demonstrated. it's an important e-book for researchers attracted to the basal ganglia, purine biology, and Parkinson's sickness. Key beneficial properties* Discusses the invention and improvement of a singular non-dopaminomimetic agent for Parkinson's illness* presents the 1st definitive evaluation of adenosine antagonists and their function within the remedy of Parkinson's disorder* 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 review 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
Separate promoters in the human A1 adenosine receptor gene direct the synthesis of distinct messenger RNAs that regulate receptor abundance. Mol Pharmacol, 48 (1995) 957-980. 46. , Molecular cloning and characterization of a rat Al-adenosine receptor that is widely expressed in brain and spinal cord. Mol Endocrinol, 5 (1991) 1037-1048. 47. , Adenosine A2A receptor antagonists as new agents for the treatment of Parkinson's disease. Trends Pharmacol Sci, 18 (1997) 338- 344. 48. , and Zhou, E, Immunohistochemical detection of A1 adenosine receptors in rat brain with emphasis on localization in the hippocampal formation, cerebral cortex, cerebellum and basal ganglia.
1990). These findings suggest that selective activation of a central population of A1 receptors, presumably in the hippocampus, impairs retention of a passive avoidance, possibly via an influence on hippocampal excitability. , 1993). , 1993). These results suggest that adenosine A1 antagonists may have therapeutic potential for the treatment of cognitive deficits in humans. , 1991), have also been reported. III. A2A A D E N O S I N E R E C E P T O R A N T A G O N I S T S A. , 1995). , 1986). , 1989).
1996). The role of adenosine AzA receptors in regulating GABAergic synaptic transmission in striatal medium spiny neurons. J Neurosci 16, 605-611. , Suzuki, E, and Sandoval-Ramirez, J. (1997b). Synthesis and structure-activity relationships of 3,7-dimethyl-1propargylxanthine derivatives, A2A-selective adenosine receptor antagonists. J Med Chem 40 4396 -4405. W. (1993). Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.
Adenosine Receptors and Parkinson's Disease by Hiroshi Kase