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Vol. 51, Issue 4, 745-781, December 1999

International Union of Pharmacology. XXI. Structure, Distribution, and Functions of Cholecystokinin Receptors

Florence Noble, Stephen A. Wank, Jacqueline N. Crawley, Jacques Bradwejn, Kim B. Seroogy, Michel Hamon and Bernard P. Roques1

Institut National de la Santé et de la Recherche Médicale U266, Centre National de la Recherche Scientifique UMR 8600, Université René Descartes, Paris, France (B.P.R., F.N.); Royal Ottawa Hospital, University of Ottawa, Ottawa, Ontario, Canada (J.B.); Section on Behavioral Neuropharmacology, Experimental Therapeutics Branch, National Institute of Mental Health, Bethesda, Maryland (J.N.C.); National Institutes of Health, Digestive Diseases Branch, Bethesda, Maryland (S.A.W.); Department of Anatomy and Neurobiology, Chandler Medical Center, University of Kentucky, Lexington, Kentucky (K.B.S.); and Institut National de la Santé et de la Recherche Médicale U288, Faculté de Médecine Pitié-Salpêtrière, Paris, France (M.H.)

I. Introduction
II. Characterization of Cholecystokinin (CCK) Receptors
    A. CCK1 (CCK-A) Receptors
        1. CCK1 Receptor Clones.
        2. Antagonists of CCK1 Receptors.
        3. Agonists of CCK1 Receptors.
    B. CCK2 (CCK-B) Receptors
        1. CCK2 Receptor Clones.
        2. Gastrin Receptors Are CCK2 Receptors.
        3. Antagonists of CCK2 Receptors.
        4. Agonists of CCK2 Receptors.
III. Molecular Biology of CCK Receptors
    A. CCK Receptor Gene Structure
    B. Chromosomal Localization of CCK Receptor Genes
    C. Animal Models without Detectable Levels of CCK Receptors
IV. Receptor Structure/Function Studies
    A. Signal Transduction
        1. CCK1 Receptors.
        2. CCK2 Receptors.
    B. Ligand-Receptor Interaction
        1. Agonists.
        2. Antagonists.
        C. Receptor Regulation.
V. Radioligands and Binding Assays: Heterogeneity of CCK1 and CCK2 Receptors
    A. Radioligands at CCK1 Receptors
    B. Radioligands at CCK2 Receptors
    C. Heterogeneity of CCK2 Receptor-Binding Sites
VI. Distribution of CCK Receptors
    A. Distribution in Central Nervous System
        1. CCK1 Receptors.
        2. CCK2 Receptors.
        3. Regulation of CCK Receptors.
    B. Distribution in Gastrointestinal and Other Systems
VII. Physiological Implications of CCK Receptors
    A. Peripheral Functions
    B. Central Functions
        1. CCK in Panic Attacks and Anxiety.
        2. CCK and Schizophrenia.
        3. CCK and Depression.
        4. CCK and Memory Processes.
        5. Interactions between CCK and Enkephalin
Systems.
VIII. Conclusion
Acknowledgments
References


1 Address for correspondence: Prof. Bernard P. Roques, INSERM U266, Centre National de la Recherche Scientifique UMR 8600, Université René Descartes, 4, Avenue de l'Observatoire, 75270 Paris Cedex 06, France. E-mail: roques{at}pharmacie.univ-paris5.fr


0031-6997/99/5104-0745$03.00/0
PHARMACOLOGICAL REVIEWS
Copyright © 1999 by The American Society for Pharmacology and Experimental Therapeutics



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