THE DISCOVERY OF A SERIES OF NEW NON-INDOLE 5HT(1D) AGONISTS

Authors
VANLOMMEN G DEBRUYN M SCHROVEN M VERSCHUEREN W JANSSENS W VERRELST J LEYSEN J
Citation
G. Vanlommen et al., THE DISCOVERY OF A SERIES OF NEW NON-INDOLE 5HT(1D) AGONISTS, Bioorganic & medicinal chemistry letters, 5(22), 1995, pp. 2649-2654
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
22
Year of publication
1995
Pages
2649 - 2654
Database
ISI
SICI code
0960-894X(1995)5:22<2649:TDOASO>2.0.ZU;2-W
Abstract
The synthesis and SAR of a series of non-indole 5HT(1D) agonists is de scribed. The most interesting molecule of this series is compound 13, alniditan. It is active as a constrictor of the saphenous vein of the dog and of the pig basilar artery with ED(50) values of 9.09x10(-9)M a nd 2.29x10(-8)M respectively, and it has high affinities to the 5HT(1D )-receptor and to the 5HT(1D)-receptor with pK(i) values of 8.6 and 8. 3 respectively.