Design, Synthesis, and Evaluation of Indolebutylamines as a Novel Class of Selective Dopamine D3 Receptor Ligands

and displays excellent selectivity overthe dopamine 1 receptor and dopamine 2 receptor.Investigation based on structural information indicatesthat site S182 located in extracellular loop 2 mayaccount for high selectivity of compounds. Interactionmodels of the dopamine 3 receptor-11q complex andstructure-activity relationships were discussed by inte-grating all available experimental and computationaldata with the eventual aim to discover potent and selec-tive ligands to dopamine 3 receptor.Key words: dopamine 3 receptor, indolebutylamine, pharma-cophore model, selectivity, structure-activity relationshipReceived 22 November 2012, revised 17 April 2013 andaccepted for publication 26 April 2013