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Vol. 50, Issue 2, 291-314, June 1998
-Aminobutyric AcidA Receptors: Classification on
the Basis of Subunit Structure and Receptor Function
Molecular Neurobiology Unit (E.A.B.), Royal Free Hospital
School of Medicine, London, England;
Neuroscience Discovery (P.S.),
Lilly Research Laboratories, Indianapolis, Indiana;
Department of
Pharmacology (R.W.O.), U.C.L.A. School of Medicine, Los Angeles,
California;
Institute of Pharmacology (H.M.), ETH and University of
Zurich, Zurich, Switzerland;
Department of Biochemical Psychiatry
(W.S.), University of Vienna, Vienna, Austria;
Department of
Experimental Biology (G.B.), University of Cagliari, Cagliari,
Italy;
Pharmaceutical Division (C.B.), Schering A.G., Berlin,
Germany;
Department of Pharmacology, University of Alberta
(A.N.B.), Edmonton, Canada;
Synthélabo Recherche (L.E.R.S.)
(S.Z.L.), Bagneux, France
I. Introduction
A. Earlier Classifications of 
-Aminobutyric Acid Receptors
1. -Aminobutyric acidA and -aminobutyric
acidB receptors.
2. -Aminobutyric acidC receptors.
3. Benzodiazepine receptors.
4. Excitatory -aminobutyric acidA receptors.
B. Conclusion on -Aminobutyric Acid Receptor Types
II. Approaches to the Classification of the
-Aminobutyric AcidA Receptors
A. Transductional Criteria
B. Operational Criteria
C. Structural Criteria
III. The Structures of the -Aminobutyric AcidA
Receptors
A. The Repertoire of Subunit Types
B. The Subunit Number per Receptor Molecule
C. The Subunit Isoforms in One Receptor
D. Possibilities for Subunit Stoichiometry
IV. Principles of the Classification
A. Application of Selectivities at the Binding Site for
Benzodiazepines and Their Functional Analogs
1. The choice of a classification system.
2. Benzodiazepine-responsive -aminobutyric acid receptor
subtypes.
3. Notation.
B. Advantages and Possible Modification of the Classification
C. Nomenclature for the Site Binding Benzodiazepines and Modulators
with Similar Activity
D. Benzodiazepine Insensitivity
V. Chromosomal Localization of -Aminobutyric AcidA
Receptor Genes
VI. Other Binding Sites in Relation to the Receptor Classification
A. Other Modulatory Sites
B. The -Aminobutyric Acid Recognition Site
VII. Conclusions
Acknowledgments
References
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C. Leroy, P. Poisbeau, A. F. Keller, and A. Nehlig Pharmacological |
