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Vol. 49, Issue 3, 253-278, September 1997
Department of Physiology and Pharmacology (S.J.H.), Medical School,
Queen's Medical Centre, Nottingham, England;
Department of Chemistry
(C.R.G.), University College London, Christopher Ingold Laboratories,
London, England;
Department of Pharmacochemistry (H.T.),
Leiden/Amsterdam Center for Drug Research, Vrije Universiteit,
Amsterdam, The Netherlands;
Unité de Neurobiologie (J.C.S.),
Paris, France;
James Black Foundation (N.P.S.), King's College School
of Medicine and Dentistry, Dulwich, London, England;
Department of
Pharmacology (J.M.Y), University of Cambridge, Cambridge;
Freie
Universität Berlin (W.S.), Institut für Pharmazie I, Berlin
(Dahlem), Germany;
Department of Pharmacology (R.L.), Cornell
University Medical College, New York;
Department of Physiology
(H.L.H.), Heinrich Heine University, Düsseldorf, Germany
I. Introduction and Historical Perspective
II. Histamine H1-Receptor
A. Distribution and Function
B. H1-Selective Ligands
C. Receptor Structure
D. Signal Transduction Mechanisms
III. Histamine H2-Receptor
A. Distribution and Function
B. H2-Selective Ligands
C. Receptor Structure
D. Signal Transduction Mechanisms
IV. Histamine H3-Receptor
A. Distribution and Function
B. H3-Receptor Selective
Ligands
C. Receptor Structure
D. Signal Transduction Mechanisms
V. Other Responses to Histamine
A. Potentiation of Responses to N-Methyl-D-Aspartate
B. A Role as an Intracellular Messenger?
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||||
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||||
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||||
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