Itameline


Itameline is a non-selective muscarinic [acetylcholine receptor] agonist which was under development for the treatment of Alzheimer's disease and memory disorders but was never marketed. It has been referred to as a "nootropic".
Itameline is a prodrug of RU-35963, an arecoline derivative. It is an agonist of the muscarinic acetylcholine M1 receptor as well as of other muscarinic acetylcholine receptors. Itameline is described as being superior to arecoline in terms of potency, central selectivity, and duration of action. The drug shows antiamnesic effects in animals, for instance reversing scopolamine-induced memory deficits. Structurally, it is a tetrahydropyridine similarly to xanomeline and milameline.
Itameline was first described in the scientific literature by 1992. It was under development by Hoechst Marion Roussel and reached phase 2 clinical trials by 1998 prior to the discontinuation of its development.