SYNTHESIS AND BINDING AFFINITIES OF A SERIES OF 1,2-BENZISOXAZOLE-3-CARBOXAMIDES TO DOPAMINE AND SEROTONIN RECEPTORS

Authors
NUHRICH A VARACHELEMBEGE M VERCAUTEREN J DOKHAN R RENARD P DEVAUX G
Citation
A. Nuhrich et al., SYNTHESIS AND BINDING AFFINITIES OF A SERIES OF 1,2-BENZISOXAZOLE-3-CARBOXAMIDES TO DOPAMINE AND SEROTONIN RECEPTORS, European journal of medicinal chemistry, 31(12), 1996, pp. 957-964
Citations number
33
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
31
Issue
12
Year of publication
1996
Pages
957 - 964
Database
ISI
SICI code
0223-5234(1996)31:12<957:SABAOA>2.0.ZU;2-A
Abstract
A series of 1,2-benzisoxazole-3-carboxamides derived from tertiary cyc loalkylamines was synthesized and evaluated for affinity for serotoner gic (5-HT3 and 5-HT4) and dopaminergic (D-2) receptors using radioliga nd binding assays. The majority of compounds displayed a very weak aff inity for the studied neurotransmitter receptors. Only amides containi ng a conformationally rigid system retained a relative 5-HT3 receptor affinity. The presence of a quinuclidine group affected receptor inter action more favorably than the tropane framework.