[3H](+)S 14297: a novel, selective radioligand at cloned human dopamine D3 receptors.
The selective dopamine D3 receptor antagonist [3H](+)S 14297 ((+)-[7-(N,N-dipropylamino)-5,6,7,8-tetrahydro-naphtho(2,3b)dihydro,2,3- furane]), labelled to high specific activity (145 Ci/mmol), bound to cloned human dopamine D3 receptors but displayed negligible binding to cloned human D2 receptors. [3H](+)S 14297 exhibited rapid association and dissociation, high affinity saturable binding (Kd = 7.0 nM) and a competition binding profile highly correlated with that of [125I]iodosulpride (r = 0.98).
Newman-Tancredi
A
A
Department of Psychopharmacology, Institut de Recherches Servier, Paris, France.
Audinot
V
V
Jacques
V
V
Peglion
J L
JL
Millan
M J
MJ
D015081:2-Naphthylamine / Q000031:analogs & derivatives* / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive; D016466:CHO Cells; D006224:Cricetinae; D015259:Dopamine Agents / Q000378:metabolism; D005663:Furans / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050637:Receptors, Dopamine D3; D013469:Sulpiride / Q000031:analogs & derivatives / Q000378:metabolism; D014162:Transfection; D014316:Tritium
C493593:DRD3 protein, human; D015259:Dopamine Agents; D005663:Furans; D008024:Ligands; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; C045105:iodosulpride; D014316:Tritium; C090812:7-(N,N-dipropylamino)-5,6,7,8-tetrahydronaphtho(2,3-b)dihydro-2,3-furan; D013469:Sulpiride; D015081:2-Naphthylamine