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
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.