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Synthesis of Novel 4-Aryl-1,2,3,4-tetrahydroisoquinolines as Probes for Dopamine Receptor Ligands

[ Vol. 8 , Issue. 4 ]

Author(s):

Gianfabio Giorgioni, Dario Ambrosini, Giovanni Filippo Palmieri, Barbara Costa, Antonio Di Stefano and Claudia Martini   Pages 699 - 704 ( 6 )

Abstract:


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.

Keywords:

Binding tests, cross-coupling reactions, D1-like receptors, D2-like receptors, dopamine ligands, structure activity relationships, tetrahydroisoquinoline, pharmacokinetic, cerebral striatal membranes, phenylmethanols

Affiliation:

School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, via S. Agostino 1 62032 Camerino Italy.



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