SEN12333 (intraperitoneal injection; 3 mg/kg) improves episodic memory in a novel object recognition task in rats in conditions of spontaneous forgetting as well as cognitive disruptions induced via glutamatergic or cholinergic mechanisms. SEN12333 also prevents a scopolamine-induced deficit in a passive avoidance task[1].
In Vitro
In whole-cell patch-clamp recordings, SEN12333 activates peak currents and maximal total charges similar to acetylcholine (EC50= 12 μM). SEN12333 displays functional antagonism at histamine H3 receptors (IC50=103 nM) and weak agonist activity at human ganglionic α3 nAChRs (IC50=8.5 μM)[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Corinne Beinat, et al. The Recent Development of α7 Nicotinic Acetylcholine Receptor (nAChR) Ligands as Therapeutic Candidates for the Treatment of Central Nervous System (CNS) Diseases.Curr Pharm Des. 2016;22(14):2134-51.
[2]. Renza Roncarati, et al. Procognitive and neuroprotective activity of a novel alpha7 nicotinic acetylcholine receptor agonist for treatment of neurodegenerative and cognitive disorders. J Pharmacol Exp Ther. 2009 May;329(2):459-68.
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