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J. Biol. Chem., Vol. 276, Issue 25, 22621-22629, June 22, 2001
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From the School of Animal and Microbial Sciences, University of
Reading, Whiteknights, Reading RG6 6AJ, United Kingdom
We have examined the binding of two radioligands
([3H]spiperone and [3H]raclopride) to
D2 dopamine receptors expressed in Chinese hamster ovary cells. In saturation binding experiments in the presence of sodium ions, both radioligands labeled a similar number of sites,
whereas in the absence of sodium ions [3H]raclopride
labeled about half the number of sites labeled by [3H]spiperone. In competition experiments in the absence
of sodium ions, however, raclopride was able to inhibit
[3H]spiperone binding fully. In saturation analyses with
[3H]spiperone in the absence of sodium ions raclopride
exerted noncompetitive effects, decreasing the number of sites labeled
by the radioligand. These data are interpreted in terms of a
model where the receptor exists as a dimer, and in the absence of
sodium ions, raclopride exerts negative cooperativity across the dimer
both for its own binding and the binding of spiperone. A model of the
receptor has been produced that provides a good description of the
experimental phenomena described here.
Dopamine D2 Receptor Dimer Formation
EVIDENCE FROM LIGAND BINDING*
*
This work was supported by the Wellcome Trust and the
University of Reading.The costs of publication of this
article were defrayed in part by the
payment of page charges. The article
must therefore be hereby marked
"advertisement" in
accordance with 18 U.S.C. Section
1734 solely to indicate this fact.
To whom correspondence should be addressed: School of Animal and
Microbial Sciences, University of Reading, Whiteknights, Reading RG6
6AJ, United Kingdom.
Copyright © 2001 by The American Society for Biochemistry and Molecular Biology, Inc.
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