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NS3861

Names

[ CAS No. ]:
216853-59-7

[ Name ]:
NS3861

Biological Activity

[Description]:

NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively[1].

[Related Catalog]:

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

[In Vitro]

NS3861 displays the opposite β-subunit preference and a complete lack of activation at α4-containing receptors in HEK293 cell lines. NS3861 selectively activates α3- but not α4-containing nAChRs and it displays higher efficacy at the α3β2 receptor compared with the α3β4 receptor, with EC50s of 1.7 and 0.15 μM for α3β2 and α3β4 receptor, respectively[1]. NS3861 shows high affinity and partial agonist properties in α3β4-expressed nAChRs[2].

[In Vivo]

NS3861 enhances fecal pellet expulsion in a dose-dependent manner in mice that received long-term, but not short-term, morphine treatment[2].

[References]

[1]. Kasper Harpsøe, et al. Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors. J Biol Chem. 2013 Jan 25;288(4):2559-70.

[2]. Aravind R Gade, et al. Enhanced Sensitivity of α3β4 Nicotinic Receptors in Enteric Neurons after Long-Term Morphine: Implication for Opioid-Induced Constipation. J Pharmacol Exp Ther. 2016 Jun;357(3):520-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C12H14BrNS

[ Molecular Weight ]:
284.22

Related Compounds