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

Medicinal Chemistry, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA.
Bioorganic & Medicinal Chemistry Letters (Impact Factor: 2.34). 03/2007; 17(3):745-9. DOI: 10.1016/j.bmcl.2006.10.076
Source: PubMed

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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