Title of article
Discovery of selective dopamine D4 receptor antagonists: 1-Aryloxy-3-(4-aryloxypiperidinyl)-2-propanols
Author/Authors
Jon L. Wright، نويسنده , , Tracy F. Gregory، نويسنده , , Thomas G. Heffner، نويسنده , , Robert G. MacKenzie، نويسنده , , Thomas A. Pugsley، نويسنده , , Seth Vander Meulen، نويسنده , , Lawrence D. Wise، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1997
Pages
4
From page
1377
To page
1380
Abstract
High volume screening identified 3-(4-benzylpiperidinyl)-1-naphthoxy-2-propanol as a selective dopamine D4 receptor ligand. A systematic structure-activity study revealed that the benzyl group could be replaced with phenoxy and the naphthalene with phenyl to improve potency almost tenfold. The (R) enantiomer of this compound had a D4 affinity of 2 nM and was over 100-fold weaker at dopamine D2 and D3 receptors.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1997
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
788773
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