BIVALENT INDOLES EXHIBITING SEROTONERGIC BINDING-AFFINITY

Authors
LEBOULLUEC KL MATTSON RJ MAHLE CD MCGOVERN RT NOWAK HP GENTILE AJ
Citation
Kl. Leboulluec et al., BIVALENT INDOLES EXHIBITING SEROTONERGIC BINDING-AFFINITY, Bioorganic & medicinal chemistry letters, 5(2), 1995, pp. 123-126
Citations number
19
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
2
Year of publication
1995
Pages
123 - 126
Database
ISI
SICI code
0960-894X(1995)5:2<123:BIESB>2.0.ZU;2-3
Abstract
A series of bis-5-carboxamidoindoles were prepared and examined in a n umber of serotonin assays (5HT(1A), 5HT(1D), 5HT(1E), and 5HT UT).(1) They were found to exhibit good affinity for the 5HT(1A) and 5HT(1D) r eceptor subtypes and to inhibit the 5HT uptake sites. Optimal 5HT(1D) potency was achieved for bivalent analogs 5f and 5g, whose linkers spa nned 7 and 8 alkyl units. Analogs with longer alkyl chain linkers (n= 10, 12), 5h and 5i, exhibited no selectivity for the 5HT(1D) receptor over the 5HT(1A) receptor.