Thiacloprid, a chloronicotinyl insecticide, acts as a selective agonist at insect nAChRs. The IC50 values are 2.7 and 860 nM for Drosophilan AChRs and M10 mouse fibroblast cells expressing α4β2 subunit-containing nAChRs, respectively.

Cynandione A, an acetophenone derived from Cynanchum wilfordii, has anti-inflammatory activity and significantly reduces pro-inflammatory cytokine overexpression via macrophage α7 nAChR activation and subsequent IL-10 expression.

Darifenacin (UK-88525) is a muscarinic receptor M3 antagonist with anticonvulsant activity and can be used to study urinary incontinence and overactive bladder.