2. Academic Validation
  3. Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR

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

  • Bioorg Med Chem Lett. 2007 Feb 1;17(3):745-9. doi: 10.1016/j.bmcl.2006.10.076.
Peter Grundt 1,  Sarah Little Jane Husband,  Robert R Luedtke,  Michelle Taylor,  Amy Hauck Newman
Affiliations

Affiliation

  • 1 Medicinal Chemistry, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA.
PMID: 17095222 DOI: 10.1016/j.bmcl.2006.10.076
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.

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