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| Contributors | |
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| Preface | |
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| Introductory Remarks: Adenosine A[subscript 2A] Receptor Antagonists: A Novel Approach to the Treatment of Parkinson's Disease | |
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| A View of the Action of Adenosine in the Striatum | |
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| Adenosine A[subscript 2A] Receptor Functions in Normal and Disease States | |
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| New Aspects of Adenosine A[subscript 2A] Receptor Function | |
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| Intracellular Signal Transduction of Presynaptic A[subscript 2A] Receptors in the Striatum | |
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| Adenosine A[subscript 2A] Function in the Parkinsonian State | |
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| Adenosine and Dopamine Receptors | |
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| L-Dopa-induced Dyskinesias and A[subscript 2A] Receptors | |
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| References | |
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| Localization of Adenosine Receptors in Brain and Periphery | |
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| Adenosine | |
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| Receptor Subtypes | |
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| Adenosine A[subscript 1] Receptors | |
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| Adeonsine A[subscript 2A] Receptors | |
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| Adenosine A[subscript 2B] Receptors | |
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| Adenosine A[subscript 3] Receptors | |
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| Summary | |
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| References | |
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| Medicinal Chemistry of Adenosine Receptors in Brain and Periphery | |
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| Introduction | |
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| A[subscript 1] Adenosine Receptor Antagonists | |
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| Structure--Activity Relationships | |
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| Pharmacology of A[subscript 1] Receptor Antagonists | |
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| A[subscript 2A] Adenosine Receptor Antagonists | |
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| Structure--Activity Relationship | |
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| Photoisomerization of 8-Styrylxanthines | |
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| Pharmacology of A[subscript 2A] Receptor Antagonists | |
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| Conclusion | |
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| References | |
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| Overview of the Physiology and Pharmacology of Adenosine in the Peripheral System | |
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| Metabolism, Receptors, and Modulation of Adenosine | |
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| Peripheral Nervous System | |
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| Cardiovascular System | |
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| Renal Effects | |
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| Respiratory and Pulmonary System | |
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| Gastrointestinal System | |
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| Inflammation and Immune System | |
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| Endocrine and Exocrine Effects | |
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| Concluding Remarks | |
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| References | |
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| Biochemical Characterization of Adenosine Agonists and Antagonists | |
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| Introduction | |
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| Ligands for Adenosine Receptor Subtypes | |
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| Binding Characterization of Adenosine Receptor Ligands | |
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| Signal Transduction | |
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| A[subscript 1] Receptor | |
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| A[subscript 2A] Receptor | |
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| A[subscript 2B] Receptor | |
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| A[subscript 3] Receptor | |
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| Biochemical Basis of the Use of A[subscript 2A] Antagonists in Parkinson's Disease | |
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| Conclusion | |
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| References | |
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| Physiology of Adenosine Receptors in the Striatum | |
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| Introduction | |
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| Striatal Cell Subtypes | |
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| The Striatal Medium Spiny Neurons | |
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| A[subscript 2A] Receptor-Mediated Suppression of Gabaergic Transmission onto Medium Spiny Neurons | |
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| A[subscript 2A] Receptor Suppression of IPSPs and IPSCs in Medium Spiny Neurons | |
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| Presynaptic A[subscript 2A] Receptor Modulation | |
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| Physiological Significance of A[subscript 2A] Receptor Modulation of Gabaergic Synaptic Transmission in Medium Spiny Neurons | |
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| Adenosine Receptor Modulation of Glutamatergic Synaptic Transmission in the Striatum | |
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| Influence of Adenosine Receptor Activation on Membrane Properties of Medium Spiny Neurons | |
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| Antiparkinsonian Effects of A[subscript 2A] Receptor Antagonists | |
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| Conclusion | |
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| References | |
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| Regulation of Neurotransmitter Release in Basal Ganglia by Adenosine Receptor Agonists and Antagonists in Vitro and in Vivo | |
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| Introduction | |
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| Methodology | |
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| The Adenosine A[subscript 1] Receptor in the Basal Ganglia | |
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| Localization of the A[subscript 1] Receptor | |
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| Mechanism of Action of the Adenosine A[subscript 1] Receptor | |
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| A[subscript 1] Receptor Modulation of ACh Release | |
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| A[subscript 1] Receptor Modulation of GABA Release | |
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| A[subscript 1] Receptor Modulation of Dopamine Release | |
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| A[subscript 1] Receptor Modulation of Glutamate Release | |
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| The Adenosine A[subscript 2] Receptors in the Basal Ganglia | |
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| Localization of the A[subscript 2] Receptors | |
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| Mechanism of Action of the A[subscript 2] Receptors | |
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| A[subscript 2A] Receptor Modulation of ACh Release | |
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| A[subscript 2A] Receptor Modulation of GABA Release | |
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| A[subscript 2] Receptor Modulation of Dopamine Release | |
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| A[subscript 2] Receptor Modulation of Glutamate Release | |
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| Relevance of the A[subscript 2A] Receptor to the Therapy of Parkinson's Disease | |
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| References | |
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| Control of Gene Expression in Basal Ganglia by Adenosine Receptors | |
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| Introduction | |
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| Neuropeptide Gene Expression | |
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| Immediate Early Gene Expression | |
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| Effect of CGS15943A on Proenkephalin mRNA Levels in Dopamine-Depleted Striatum | |
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| Effect of A[subscript 2] and A[subscript 1] Adenosine Receptor Antagonism on Levels of Striatal Peptide Gene Expression | |
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| Discussion | |
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| Effect of CGS15943A in Unilaterally Lesioned Rat Striatum | |
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| Effect of KF17837 in Striatum of Rats Treated with Eticlopride | |
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| References | |
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| Knockout Mice in the Study of Dopaminergic Diseases | |
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| Introduction | |
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| D[subscript 2]-like Receptors | |
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| Dopamine D[subscript 2] Receptor | |
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| Two Isoforms of D[subscript 2] Receptor | |
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| D[subscript 3] Receptor | |
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| D[subscript 4] Receptor | |
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| D[subscript 1]-like Receptors | |
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| D[subscript 1] Receptor | |
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| D[subscript 5] Receptor | |
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| Dopamine D[subscript 1] and D[subscript 2] Receptor Interactions in Basal Ganglia | |
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| Dopamine and Adenosine | |
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| D[subscript 2] Receptor-Deficient Mice | |
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| Adenosine A[subscript 2A] Receptor-Deficient Mice | |
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| Animal Models of Neuropathologies: D[subscript 2] Receptor-Deficient Mice and Parkinson's Disease | |
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| References | |
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| Effects of Adenosine Receptors | |
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| Introduction | |
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| The Role of Adenosine A[subscript 1] Receptor in the CNS in Cognition | |
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| Distribution of Adenosine A[subscript 1] Receptor in CNS | |
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| Cognition | |
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| Role of Adenosine A[subscript 2A] Receptor in CNS | |
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| Distribution of A[subscript 2A] Receptor in CNS | |
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| Behavioral Phenotype in A[subscript 2A] Receptor KO Mice | |
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| Sleep | |
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| Adenosine A[subscript 2A] Receptor and Motor Function | |
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| Conclusion | |
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| Methods | |
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| Spontaneous Electroencephalogram | |
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| Internal Capsule Lesion | |
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| Locomotor Activity | |
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| Data Analysis and Statistics | |
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| Acknowledgments | |
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| References | |
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| Actions of Adenosine Antagonists in Primate Model of Parkinson's Disease | |
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| Introduction | |
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| Action of MPTP on Motor Behavior in Common Marmosets | |
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| Effects of Adenosine Receptor Ligands on Motor Dysfunction in MPTP-Treated Common Marmosets | |
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| Adenosine A[subscript 1] Receptor Antagonist DPCPX | |
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| Adenosine A[subscript 2A] Receptor Antagonist KW-6002 | |
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| Adenosine A[subscript 2A] Receptor Agonist APEC | |
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| Effect of Adenosine A[subscript 2A] Receptor Antagonist KW-6002 on L-Dopa-induced Dyskinesias | |
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| Effect of Chronic Administration of Adenosine A[subscript 2A] Receptor Antagonist KW-6002 | |
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| Comparison of the Antiparkinsonian Activity of L-Dopa and A[subscript 2A] Antagonist KW-6002 | |
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| Conclusion | |
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| Acknowledgments | |
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| References | |
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| Selective Adenosine A[subscript 2A] Receptor Antagonism as an Alternative Therapy for Parkinson's Disease | |
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| Introduction | |
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| Materials and Methods | |
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| Animals | |
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| Drug Treatments | |
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| Motor Assessment | |
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| Statistical Analysis | |
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| Results | |
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| Locomotion | |
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| Improvement in Disability and Dyskinesias | |
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| Discussion | |
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| Conclusion | |
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| References | |
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| Neurobiology of Adenosine Receptors | |
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| Introduction | |
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| Adenosine in the Basal Ganglia | |
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| Effects of Caffeine or Other Methylxanthines on Parkinson's Disease | |
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| Effects of Caffeine or Other Methylxanthines on Essential Tremor | |
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| Effects of Caffeine or Other Methylxanthines on Other Movement Disorders | |
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| Levels of Adenosine and Other Nucleosides in Neurological Disorders | |
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| Effects of Xanthines or L-Dopa on Other Neurological Disorders | |
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| References | |
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| The Relevance of Adenosine A[subscript 2A] Antagonists to the Treatment of Parkinson's Disease: Concluding Remarks | |
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| Introduction | |
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| Striatal Output Pathways and Parkinson's Disease | |
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| Alterations in Striatal Output Pathways Following the Occurrence of Dyskinesia | |
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| Final Comments | |
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| Acknowledgments | |
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| References | |
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| Index | |