For research use only. Not for therapeutic Use.
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 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].
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].
| Catalog Number | R058511 |
| CAS Number | 874450-44-9 |
| Synonyms | 5-morpholin-4-yl-N-(4-pyridin-3-ylphenyl)pentanamide |
| Molecular Formula | C20H25N3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H25N3O2/c24-20(5-1-2-11-23-12-14-25-15-13-23)22-19-8-6-17(7-9-19)18-4-3-10-21-16-18/h3-4,6-10,16H,1-2,5,11-15H2,(H,22,24) |
| InChIKey | XCHIZTUBUXZESJ-UHFFFAOYSA-N |
| SMILES | C1COCCN1CCCCC(=O)NC2=CC=C(C=C2)C3=CN=CC=C3 |
| Reference | [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. |
