期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 14, 页码 5291-5300出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.05.052
关键词
Dopamine; D-2 receptor; Indoles; Benzofurans; Benzothiophenes
资金
- National Institutes of Health [MH081281, DA023957]
A series of indole, 7-azaindole, benzofuran, and benzothiophene compounds have been prepared and evaluated for affinity at D2-like dopamine receptors. These compounds share structural elements with the classical D2-like dopamine receptor antagonists haloperidol, N-methylspiperone and benperidol. Two new compounds, 4-(4-iodophenyl)-1-((4-methoxy-1H-indol-3-yl) methyl) piperidin-4-ol (6) and 4-(4-iodophenyl)-1-((5-methoxy-1H-indol-3-yl) methyl) piperidin-4-ol (7), were found to have high affinity to and selectivity for D2 versus D3 receptors. Changing the aromatic ring system from an indole to other heteroaromatic ring systems reduced the D2 binding affinity and the D2 versus D3 selectivity. (C) 2010 Elsevier Ltd. All rights reserved.
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