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.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Heuillet E,Petitet F,Mignani S,Malleron JL,Lavayre J,Néliat G,Doble A,Blanchard JCdoi
10.1016/s0014-2999(96)00554-7subject
Has Abstractpub_date
1996-10-24 00:00:00pages
229-33issue
1-2eissn
0014-2999issn
1879-0712pii
S0014-2999(96)00554-7journal_volume
314pub_type
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