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Vol. 50, Issue 4, 723-757, December 1998
Department of Pharmacology II, Faculty of Medicine, Osaka
University, Osaka, Japan
I. Introduction
II. Functional Analysis of G Protein-Mediated Activation of
Muscarinic K+ Channels in Cardiac Atrial Myocytes
A. Time-Dependent Response of the Whole-Cell Muscarinic
K+ Current to Acetylcholine
1. The G protein cyclic reaction mediating the receptor-to-channel
signal transmission.
2. Activation phase.
3. The phase of short-term desensitization.
4. Deactivation of the response of the muscarinic K+
channel.
B. Quantitative Analysis of G Protein-Mediated Activation of the
Muscarinic K+ Channel
1. Single-channel characteristics of the muscarinic K+
channel.
2. Positive cooperative effect of GTP on muscarinic K+
channel activity.
3. Spectral analysis of the muscarinic K+ channel
currents in the presence of different concentrations of intracellular
GTP.
4. A possible mechanism for the G protein-mediated increase in the
functional numbers of muscarinic K+ channels.
C. Modulation of G Protein-Mediated Activation of the Muscarinic
K+ Channel
III. Molecular Analysis of G Protein-Gated K+ Channels
A. Cloning of Inwardly Rectifying K+ Channels
B. Subunits of G Protein-Gated K+ Channels
C. Tissue Distribution of GIRK Subunits
1. Peripheral tissues.
2. Central nervous system.
D. Expression of G Protein-Gated K+ Channels
E. Tetrameric Structure
F. Molecular Mechanism Underlying G Protein Activation of G
Protein-Gated K+ Channels
1. Interaction between G protein 
subunits and subunits of G
protein-gated K+ channels.
2. Mechanism underlying G protein 
subunitinduced
activation of G protein-gated K+ channels.
3. Interaction between subunits of G protein-gated K+
channels, G
proteins, and membrane agonist
receptors.
4. Possible mechanisms underlying specific signal transduction in
the receptor/G protein/G protein-gated K+ channel
system.
IV. Voltage-Dependent Properties of G Protein-Gated K+
Channels
A. Inwardly-Rectifying K+ Channels
1. Voltage-dependent change in inwardly rectifying K+
channel activity.
2. Mg2+ and polyamine block.
3. Mg2+/polyamine block sites in the inwardly
rectifying K+ channel pore.
B. Inward Rectification of G Protein-Gated K+ Channels
1. Inward rectification of the muscarinic K+
channel.
2. Mg2+/polyamine block of G protein-gated
K+ channels.
3. The Mg2+/polyamine-binding sites in G protein-gated
K+ channels.
4. Slow relaxation of G protein-gated K+ channels
containing GIRK1.
V. Pharmacological Properties of G Protein-Gated K+
Channels
VI. Localization of the G Protein-Gated K+ Channel in
Different Organs
A. Cardiac Atrial Myocytes
B. Neurons
1. Differential cellular and subcellular distribution of GIRK
subunits.
2. Functional significance of differential subcellular distribution
of GIRK subunits.
C. Endocrine Cells
VII. Weaver Mutant Mice and the GIRK2 Gene
VIII. Conclusions
Acknowledgments
References
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