4-HETEROCYCLYL TETRAHYDROPYRIDINES AS SELECTIVE LIGANDS FOR THE HUMANDOPAMINE D-4 RECEPTOR

Authors
HAWORTH KE HARRISON T KULAGOWSKI JJ LEESON PD OWENS AP RIDGILL MP TEALL MR FIELDING M CHAPMAN K EMMS F MARWOOD R PATEL S MOSS KL
Citation
Ke. Haworth et al., 4-HETEROCYCLYL TETRAHYDROPYRIDINES AS SELECTIVE LIGANDS FOR THE HUMANDOPAMINE D-4 RECEPTOR, Bioorganic & medicinal chemistry letters, 7(17), 1997, pp. 2211-2216
Citations number
12
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
17
Year of publication
1997
Pages
2211 - 2216
Database
ISI
SICI code
0960-894X(1997)7:17<2211:4TASLF>2.0.ZU;2-6
Abstract
A series of 1,2,3,6-tetrahydropyridines 3 were synthesised, which resu lted in selective high affinity dopamine Dq ligands. The SAR of hetero cyclic replacements and aromatic substitution was investigated, leadin g to compounds of nanomolar binding affinity with excellent selectivit y over both D-2 and D-3 receptors. (C) 1997 Elsevier Science Ltd.