title: Synthesis of novel 4-aryl-1,2,3,4-tetrahydroisoquinolines as probes for dopamine receptor ligands.
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.
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy. gianfabio.giorgioni@unicam.it
authors.forename: Gianfabio
authors.initials: G
authors.lastname: Giorgioni
authors.forename: Dario
authors.initials: D
authors.lastname: Ambrosini
authors.forename: Giovanni Filippo
authors.initials: GF
authors.lastname: Palmieri
authors.forename: Barbara
authors.initials: B
authors.lastname: Costa
authors.forename: Antonio
authors.initials: A
authors.lastname: Di Stefano
authors.forename: Claudia
authors.initials: C
authors.lastname: Martini
mesh_terms: D001665:Binding Sites; D008024:Ligands; D015335:Molecular Probes / Q000138:chemical synthesis*; D015394:Molecular Structure; D011954:Receptors, Dopamine / Q000378:metabolism*; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D008024:Ligands; D015335:Molecular Probes; D011954:Receptors, Dopamine; D044005:Tetrahydroisoquinolines