Further Characterization of Structural Requirements for Ligands at the Dopamine D2 and D3 Receptor:  Exploring the Thiophene Moiety

Autor: Dijkstra, D., Rodenhuis, N., Vermeulen, E. S., Pugsley, T. A., Wise, L. D., Wikstrom, H. V.
Zdroj: Journal of Medicinal Chemistry; July 2002, Vol. 45 Issue: 14 p3022-3031, 10p
Abstrakt: The present study describes the synthesis and in vitro pharmacology of a novel series of dopaminergic agents in which the classical phenylethylamine pharmacophore is replaced by a thienylethylamine moiety. In general, the novel compounds showed a moderate affinity for the dopamine (DA) D2 and D3 receptors. When the thienylethylamine moiety is fixed in a rigid system, the affinity for the DA receptor is significantly increased. However, in the tricyclic hexahydrothianaphthoxazine structure, the affinity for the DA receptors is diminished.
Databáze: Supplemental Index