SEN12333

SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K_>i=260 nM) and acts as full agonist in functional Ca²⁺ flux studies (EC₅₀=1.6 μM). SEN 12333 is used for AD and schizophrenia research^[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].
In Vivo: 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].