Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR

Peter Grundt, Sarah Little Jane Husband, Robert R. Luedtke, Michelle Taylor, Amy Hauck Newman

Research output: Contribution to journalArticlepeer-review

29 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)745-749
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number3
DOIs
StatePublished - Feb 1 2007

Bibliographical note

Funding Information:
The research reported herein was supported by funds from the NIDA Intramural Research Program and 1 DA 13584. P.G. was supported by a National Institutes of Health (NIH) Visiting Fellowship. S.L.J.H. was supported by a NIH summer IRTA fellowship.

Keywords

  • Dopamine D2 receptor antagonists

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