Encenicline (EVP-6124), shown in Figure 1, is a potent orthosteric agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR). This compound is being developed with the potential clinical indication
to treat cognitive impairment in patients with schizophrenia or Alzheimer’s disease (AD).
The primary circulating non-conjugated metabolites of encenicline are encenicline N-oxide, formed by oxidation of the quinuclidine nitrogen atom, and encenicline acid metabolite, a product formed through hydrolysis of an amide bond. Metabolite profiling has also indicated the presence of an N-glucuronide as well as other metabolites.
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