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SEN 12333

Names

[ CAS No. ]:
874450-44-9

[ Name ]:
SEN 12333

[Synonym ]:
WAY-317,538
Carbazeran citrate

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR
Signaling Pathways >> Neuronal Signaling >> nAChR
Research Areas >> Neurological Disease

[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].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H25N3O2

[ Molecular Weight ]:
339.43100

[ Exact Mass ]:
339.19500

[ PSA ]:
54.46000

[ LogP ]:
3.20050

Safety Information

[ Hazard Codes ]:
Xn

Related Compounds