Abstract
Structural modification of the 2-methoxy group and at the 4-position of the piperidine ring of the 5-HT 4 partial agonist 1 led to analogues with increased affinity for the 5-HT 4 receptor and loss of agonist activity. Similar modification of 2 resulted in 2-(3,5-dimethoxy) benzyloxy derivatives ( 23, 24, 26–28) that were found to be 5-HT 4 receptor antagonists with subnanomolar affinity.
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