Bioorganic and Medicinal Chemistry Letters p. 1377 - 1380 (1997)
Update date:2022-08-12
Topics:
Wright, Jon L.
Gregory, Tracy F.
Heffher, Thomas G.
MacKenzie, Robert G.
Pugsley, Thomas A.
Vander Meulen, Seth
Wise, Lawrence D.
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.
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