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Voltage‐dependence of the human dopamine D 2 receptor
Author(s) -
Sahlholm Kristoffer,
Nilsson Johanna,
Marcellino Daniel,
Fuxe Kjell,
Århem Peter
Publication year - 2008
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/syn.20509
Subject(s) - g protein coupled inwardly rectifying potassium channel , d1 like receptor , dopamine receptor , dopamine , neuroscience , neurotransmitter receptor , chemistry , receptor , quinpirole , neurotransmitter , dopamine receptor d1 , biophysics , synaptic plasticity , d2 like receptor , dopamine receptor d2 , microbiology and biotechnology , biology , g protein , biochemistry
The dopamine D 2 receptor plays a critical role in activity‐dependent synaptic plasticity in the striatum, and regulates the transitions between different states of electrical activity. The D 2 receptor is the main target for antipsychotics, and its affinity towards dopamine has been shown to be increased in psychotic patients. Recently, voltage‐sensitivity has been reported for the ligand binding and G protein‐coupling properties of some neurotransmitter receptors, raising the question whether the D 2 receptor is also regulated by voltage. Our present electrophysiology data from Xenopus oocytes indicate that the D 2 receptor is indeed voltage‐sensitive. Comparing concentration–response relationships for the activation of G protein‐coupled inward rectifier potassium (GIRK) channels via D 2 receptor stimulation by quinpirole or dopamine at −80 and at +40 mV revealed rightward shifts upon depolarisation of nearly tenfold, for both agonists. Our results are likely to bear relevance to the function of the D 2 receptor in gating synaptic input and in regulating plasticity. Synapse 62:476–480, 2008. © 2008 Wiley‐Liss, Inc.