- PIPERAZINES AS P2X7 ANTAGONISTS
-
Novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, enantiomers thereof or prodrugs thereof of Formula (I), wherein the substituents are as defined herein, which are useful as therapeutic agen
- -
-
Page/Page column 65
(2008/06/13)
-
- Affinity of 2-(tetrahydroisoquinolin-2-methyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for α-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled α2-adrenoceptor vs the [3H]yohimbine-labeled site
-
A series of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines were prepared and tested for α1- and α2-adrenoceptor affinity with radioligand binding. Several compounds, 5-fluoro- (5h), 5-chloro- (5j), 5,8-dimethoxy- (5r), and 5,8-dimethoxy-1-methyl- (5s) 2-(tetrahydroisoquinolin-2-ylmethyl)imidazoline, were found to be selective α2-adrenoceptor ligands on the basis of displacement of [3H]yohimbine from rat cerebral cortical membranes. One compound, 2-[(8-chloro tetrahydroisoquinolin-2-yl)methyl]imidazoline (5m), showed a 36-fold difference in affinity for the [3H]idazoxan-labeled α2-adrenoceptor relative to the [3H]yohimbine-labeled site, which may be evidence for α2-adrenoceptor subtypes.
- Clark,Berger,Garg,Weinhardt,Spedding,Kilpatrick,Brown,MacKinnon
-
p. 596 - 600
(2007/10/02)
-