Cholinesterase (ChE) Agonist

Aclatonium napadisylate is a cholinergic agonist. Aclatonium napadisylate can increase amylase release and Ca²⁺ efflux. Aclatonium napadisylate can stimulate pancreatic exocrine secretion and increase motility and peristalsis of the gastrointestinal tract. Aclatonium napadisylate can be used for the research of gastrointestinal disorders.

Bis-Q is an acetylcholine (ACh) agonist that targets voltage-clamped muscle fibers of the fish Xenomystus nigris. Bis-Q exists in two forms: cis-Bis-Q (non-agonist) and trans-Bis-Q (agonist). Photoisomerization converts cis-Bis-Q to trans-Bis-Q, which induces agonist-induced currents. Channels activated by trans-Bis-Q and ACh have similar conductances and open times. Flashes increase the ratio of trans-Bis-Q to cis-Bis-Q until light equilibrium is reached. Further flashes transiently increase agonist-induced currents, indicating binding of trans-Bis-Q to desensitized receptors. Higher concentrations of cis-Bis-Q produce larger agonist-induced currents that decay exponentially..

WAY-361789 (SEN15924) is an orally active agonist for α7 nicotinic acetylcholine receptor (α7 nAChR) with an EC₅₀ of 0.18 μM. WAY-361789 improves the cognitive function, exhibits potential in ameliorating Alzheimer’s Disease and schizophrenia.

Itameline (RU 47213) is a prodrug with oral and long-lasting cholinergic activity. Itameline is a novel tetrahydropyridine-oxime that is cleaved in vivo to form an active metabolite, RU 35963. RU 35963 is a muscarinic receptor agonist that is nonselective with respect to receptor subtypes. Itameline possesses the capacity to reduce memory deficits induced by an impairment of cholinergic transmission in the rat.