SYNTHESIS AND SEROTONIN RECEPTOR-BINDING PROPERTIES OF 5-SUBSTITUTED 3-(1',2',5',6'-TETRAHYDROPYRIDIN-3'-YL) INDOLES

Authors
DAHLGREN T DEAN RL GHARAT LA JOHANSSON AM LAMBERT G LI HB NELSON DL YANG Y MARTIN AR
Citation
T. Dahlgren et al., SYNTHESIS AND SEROTONIN RECEPTOR-BINDING PROPERTIES OF 5-SUBSTITUTED 3-(1',2',5',6'-TETRAHYDROPYRIDIN-3'-YL) INDOLES, Bioorganic & medicinal chemistry letters, 5(24), 1995, pp. 2963-2968
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
24
Year of publication
1995
Pages
2963 - 2968
Database
ISI
SICI code
0960-894X(1995)5:24<2963:SASRPO>2.0.ZU;2-I
Abstract
A semi-rigid 5-hydroxytryptamine (5-HT) analogue, RU28253 [5-methoxy-3 -(1',2',5',6'-tetrahydropyridin-3'-yl) indole], is a potent 5-HT1 and 5-HT2 agonist. It is isomeric to RU24969 [5-methoxy-3-(1',2',5',6'-tet rahydropyridin-4'-yl) indole], a conformationally restricted 5-HT homo logue, which has been extensively used in the study and classification of 5-HT receptors. A series of RU28253 derivatives with diverse subst ituents on indole 5-position were synthesized and their dissociation c onstants determined at the 5-HT1 and 5-HT2 receptors.