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.
Bibliographical noteFunding 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.
- Dopamine D2 receptor antagonists