Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.
A series of dopamine D(4) antagonists was synthesized and evaluated as potential candidates for development as positron emission tomography (PET) radioligands. All new compounds display high affinity and selectivity for the D(4) receptors and compounds 5b, 5d, and 5e were identified as candidates for radioligand development.
Huang
Y
Y
Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA. hh285@columbia.edu
Kegeles
L S
LS
Bae
S
S
Hwang
D
D
Roth
B L
BL
Savage
J E
JE
Laruelle
M
M
D001665:Binding Sites; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D050638:Receptors, Dopamine D4; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism; D014055:Tomography, Emission-Computed / Q000379:methods
C099630:3-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo(2,3-b)pyridine; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D011725:Pyridines; D011758:Pyrroles; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D050638:Receptors, Dopamine D4