Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.
A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity.
Grundt
Peter
P
Medicinal Chemistry, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA.
Husband
Sarah Little Jane
SL
Luedtke
Robert R
RR
Taylor
Michelle
M
Newman
Amy Hauck
AH
D002460:Cell Line; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D008024:Ligands; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011485:Protein Binding; D017448:Receptors, Dopamine D2 / Q000187:drug effects* / Q000235:genetics; D013329:Structure-Activity Relationship; D014162:Transfection
D018492:Dopamine Antagonists; D007211:Indoles; D008024:Ligands; D010880:Piperidines; D017448:Receptors, Dopamine D2; C104750:3-(4-(4-chlorophenyl-4-hydroxypiperidino)methyl)indole