A series of trans-2-amino-5(6)-chloro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes were synthesized and evaluated for their binding affinity toward D-1-like and D-2-like dopamine (DA) receptors. The affinity and selectivity of these compounds were measured in a test involving displacement of [H-3]SCH 23390 or [H-3]YM-09-151-2, respectively, from homogenates of porcine striatal membranes. All tested compounds were poorly effective at DA receptors (K-i nM > 1000). The results suggest that introduction of chlorine substituent in five or six position of previously synthesized trans-2-amino-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes decreases both D-1-like and D-2-like receptor affinity. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
|Autori interni:||COSTA, BARBARA|
|Autori:||Di Stefano A; Sozio P; Luisi G; Cacciatore I; Mosciatti B; Costa B; Lucacchini A; Martini C; Pinnen F|
|Titolo:||Synthesis and preliminary pharmacological evaluation of trans-2-amino-5(6)-chloro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as dopamine receptor ligands|
|Anno del prodotto:||2002|
|Digital Object Identifier (DOI):||10.1016/S0014-827X(02)01206-5|
|Appare nelle tipologie:||1.1 Articolo in rivista|