KETONES RELATED TO THE BENZOATE 5-HT4 RECEPTOR ANTAGONIST RS-23597 ARE HIGH-AFFINITY PARTIAL AGONISTS

Authors
CLARK RD JAHANGIR A LANGSTON JA WEINHARDT KK MILLER AB LEUNG E EGLEN RM
Citation
Rd. Clark et al., KETONES RELATED TO THE BENZOATE 5-HT4 RECEPTOR ANTAGONIST RS-23597 ARE HIGH-AFFINITY PARTIAL AGONISTS, Bioorganic & medicinal chemistry letters, 4(20), 1994, pp. 2477-2480
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
20
Year of publication
1994
Pages
2477 - 2480
Database
ISI
SICI code
0960-894X(1994)4:20<2477:KRTTB5>2.0.ZU;2-E
Abstract
The ketone analogue 5 of the 5-HT4 receptor antagonist RS-23597 (1) wa s found to be a 5HT(4) receptor partial agonist. Structure-activity re lationships developed for compound 5 led to the synthesis of 4-piperid inyl derivatives (15-18, 20) that were found to be partial agonists wi th increased affinity.