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.
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
COSTA, BARBARA;LUCACCHINI, ANTONIO;MARTINI, CLAUDIA;
2002-01-01
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
