Phenylpiperazinylmethylindolecarboxylates and derivatives as selective D(4)-ligands.
Novel phenylpiperazinylmethylindolecarboxylates were synthesized for evaluation as potential D(4)-ligands. Test compounds showed high affinity for the human dopamine D(4) receptor and great selectivity over the other receptor subtypes. Intrinsic effects of indole derivatives, which indicated most promising binding properties, were investigated in a mitogenesis assay.
Moll
Annette
A
Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Schuhstrasse 19, D-91052, Erlangen, Germany.
Hübner
Harald
H
Gmeiner
Peter
P
Troschütz
Reinhard
R
D000818:Animals; D016466:CHO Cells; D002417:Cattle; D006224:Cricetinae; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D008024:Ligands; D015394:Molecular Structure; D011485:Protein Binding; D011954:Receptors, Dopamine / Q000235:genetics / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000235:genetics / Q000378:metabolism*; D050638:Receptors, Dopamine D4; D013379:Substrate Specificity
C493599:DRD4 protein, human; D007211:Indoles; D008024:Ligands; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D050638:Receptors, Dopamine D4