The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor.
Eur J Pharmacol, 1996/10/24;314(1-2):229-33.
Heuillet E[1], Petitet F, Mignani S, Malleron JL, Lavayre J, Néliat G, Doble A, Blanchard JC
Affiliations
PMID: 8957240
Impact factor: 5.195
Abstract
The dopamine D4 receptor is a potential target for novel antipsychotic drugs. Most available compounds with affinity for the dopamine D4 receptor also bind to dopamine D2 receptors. This report describe the affinity of the 5-HT2A receptor antagonist RP 62203 (fananserin) for the human dopamine D4 receptor. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D4 receptors with a Ki of 2.93 nM. This compares with an affinity (Ki) of 0.37 nM for the rat 5-HT2A receptor and of 726 mM for the rat dopamine D2 receptor. [3H]Fananserin can be used to label the recombinant dopamine D4 receptor expressed in Chinese hamster ovary cells with a KD of 0.725 nM. Fananserin is, thus, the first compound to be reported that distinguishes between dopamine D4 and D2 receptors.
MeSH terms
Animals; Binding, Competitive; CHO Cells; Cricetinae; Cyclic S-Oxides; Humans; Male; Naphthalenes; Rats; Rats, Sprague-Dawley; Receptor, Serotonin, 5-HT2A; Receptors, Dopamine D2; Receptors, Dopamine D4; Receptors, Serotonin; Serotonin Antagonists
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