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EVP 6124/Encenicline hydrochloride is a partial, selective agonist of the α-7 nicotinic acetylcholine receptor (α7-nAChR). It is being developed for the treatment of cognitive deficits in schizophrenia and Alzheimer's disease. Cholinergic function declines in Alzheimer's, and currently approved acetylcholinesterase inhibitor therapies modestly improve cognitive deficits in patients with AD by way of boosting cholinergic transmission. The rationale of selective α7-nAChR agonists is that they will enhance cognition without causing side effects associated with over-activation of other nAChRs such as α4β2, or muscarinic AChRs. In rats, encenicline penetrates the blood-brain barrier and improves memory performance by potentiating the acetylcholine response. Encenicline has been reported to act as a co-agonist with acetylcholine. It sensitizes the α-7 nACh receptor to its natural ligand and renders sub-efficacious doses of AChEI drugs effective in restoring memory function in an object recognition task
| Identification | |
| Name | Encenicline |
| Synonyms | (R)-7-Chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide; EVP 6124 |
| Molecular Structure | |
| Molecular Formula | C16H17ClN2OS |
| Molecular Weight | 320.84 |
| CAS Registry Number | 550999-75-2 |
| Properties | |
| Solubility | Sparingly Soluble (0.19 g/L) (25 ºC), Calc.* |
| Density | 1.38±0.1 g/cm3 (20 ºC 760 Torr), Calc.* |
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