A set of 1-(arylalkyl)quinolizidines, isosteric thioanalogues, and variously functionalized congeners were synthesized (1-25) and tested for affinity to sigma 1 and sigma 2 receptor subtypes, by displacing [3H]- (+)- pentazocine and [3H]DTG from guinea pig brain and rat brain preparations, respectively. All compounds exhibited a good affinity for the σ1 subtype, with subnanomolar Ki values for the best of them, while only modest or poor affinity for the σ2 subtype was observed (Tables 1 and 2). Some structure-activity relationships were put forward.
1-(Arylalkyl)quinolizidine derivatives and thio-isosteric analogues as ligands for sigma receptors
NOVELLI, FEDERICA;SPARATORE, FABIO
2004-01-01
Abstract
A set of 1-(arylalkyl)quinolizidines, isosteric thioanalogues, and variously functionalized congeners were synthesized (1-25) and tested for affinity to sigma 1 and sigma 2 receptor subtypes, by displacing [3H]- (+)- pentazocine and [3H]DTG from guinea pig brain and rat brain preparations, respectively. All compounds exhibited a good affinity for the σ1 subtype, with subnanomolar Ki values for the best of them, while only modest or poor affinity for the σ2 subtype was observed (Tables 1 and 2). Some structure-activity relationships were put forward.
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