Abstract A 5-HT 3 receptor agonist based on a benzamide scaffold was identified in a screening of a small commercial compound library, and an elaborate SAR study originating from this hit was performed. The design, synthesis, and functional characterisation of benzamide analogues at the 5-HT 3 A receptor yielded substantial information concerning the analogues as 5-HT 3 receptor agonists. However, the potencies of the derived ...