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Vol. 51, Issue 1, 83-133, March 1999
Section of Molecular Neuropharmacology (B.B.F., J.H.), Department
of Physiology and Pharmacology, Karolinska Institutet, Stockholm,
Sweden; Behavioural Biology Laboratory (K.B.), Swiss Federal Institute
of Technology, Zürich, Switzerland; INSERM U 398 (A.N.),
Faculté de Médecine, Strasbourg Cedex, France; Department
of Psychopharmacology (E.E.Z.), Valdman Institute of Pharmacology,
Pavlov Medical University, St. Petersburg, Russia
I. Introduction
II. Consumption and Metabolism of Caffeine
A. Sources of Caffeine
B. Caffeine Absorption, Distribution, and Pharmacokinetics
C. Caffeine Metabolism
III. Molecular and Cellular Action of Caffeine in the Brain
A. Fundamental Biochemical Actions
B. Adenosine Levels in Brain and Other Tissues
C. Adenosine Acts on Several Types of G-Protein-Coupled Receptors
1. Receptor Subtypes.
2. Receptor Distribution.
D. Caffeine Affects Transmitter Release and Neuronal Firing Rates
via Actions on Adenosine A1 Receptors
E. Caffeine Effects on Dopaminergic Transmission Are Exerted Mainly
via Actions on Adenosine A2A Receptors
F. Identifying the Neuronal Substrates For Caffeine by Examining
Changes in Immediate Early Genes
High Dose Effects
G. Low Doses of Caffeine Selectively Decrease the Activity of
Striatopallidal Neurons in the Striatum and Their Counterparts in the
Nucleus Accumbens
IV. Actions of Caffeine on Brain Functions and Behavior
A. Activation of Dopaminergic Transmission and Effects on Motor
Behavior
B. Caffeine and Mood
C. Effects of Caffeine in the Cortex and HippocampusInformation
Processing and Performance
D. Effects on Sleep
E. Effects of Caffeine on Cerebral Blood Flow and Metabolism
F. Other Effects
V. Addiction and Drug Dependence
A. Definitions
B. On the Neuronal and Molecular Basis of Drug Reinforcement and
Addiction
VI. Caffeine Withdrawal and Relief of Abstinence Symptoms by
Caffeine
A. Animal Studies on Caffeine Withdrawal
B. Human Studies
C. Effect of Caffeine on Withdrawal Symptoms
VII. Tolerance to the Effects of Caffeine
A. Cardiovascular Effects
B. Effects on Sleep
C. Effects on Mood
D. Other Central Effects
E. Differences between Acute and Long-Term AdministrationEffect
Inversion
VIII. Caffeine Discrimination and Dose Adjustment in Animals and
Humans
A. Caffeine Discrimination in Animals
B. Caffeine Discrimination in humans
C. Dose Adjustment
IX. Reinforcing Effects of Caffeine
A. Reinforcement in Animals
1. Intravenous and Oral Self-Administration.
2. Reinforcing Effects of Caffeine: Place Conditioning.
B. Reinforcement in Humans
X. Possible Reinforcing Effects of Coffee, Independent of Caffeine
Content
XI. Comparisons with Known Addictive Compounds and Interactions
between Caffeine and Addictive Drugs
A. General Considerations
B. Interactions between Caffeine and Cocaine or Amphetamine
C. Interactions between Caffeine and Ethanol
D. Interactions between Caffeine and Nicotine
XII. Possible Harmful Effects of Caffeine at the Individual or
Social Level
Abuse or Misuse
XIII. Conclusions
Acknowledgments
References
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