Synthesis of novel 4-aryl-1,2,3,4-tetrahydroisoquinolines as probes for dopamine receptor ligands.

Gianfabio Giorgioni, Dario Ambrosini, Giovanni Filippo Palmieri, Barbara Costa, Antonio Di Stefano, Claudia Martini

School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy. gianfabio.giorgioni@unicam.it

Medicinal chemistry (Shāriqah (United Arab Emirates)) 2012 Jul

filter terms:

Dopamine (DA) agonists, bearing catechol or phenol rings, are endowed with low oral bioavailability and short effect duration. In this report, the synthesis of novel differently substituted 4-(3-pyridyl)-1,2,3,4-tetrahydroisoquinolines and (1,2,3,4-tetrahydroisoquinolin-4-yl)phenylmethanols as potential non phenolic and non catecholic DA receptor ligands is reported. The new compounds, evaluated by binding tests on cerebral striatal membranes, bound to DA receptors with moderate affinity. Anyhow, they may represent a starting point to develop new DA ligands endowed with better pharmacokinetic and metabolic properties.

Citation

Gianfabio Giorgioni, Dario Ambrosini, Giovanni Filippo Palmieri, Barbara Costa, Antonio Di Stefano, Claudia Martini. Synthesis of novel 4-aryl-1,2,3,4-tetrahydroisoquinolines as probes for dopamine receptor ligands. Medicinal chemistry (Shāriqah (United Arab Emirates)). 2012 Jul;8(4):699-704