NS 3861 is a neuronal nicotinic acetylcholine receptor (nAChR) agonist.1 It induces inward currents in patch-clamp assays using X. laevis oocytes expressing recombinant human α3β2- or α3β4 subunit-containing nAChR receptors (EC50s = 1.6 and 1 ?M, respectively). In vivo, NS 3861 (0.1 mg/kg) increases the number of fecal pellets expelled in mice exposed to long-term, but not short-term, morphine injections.2
References:
[1]. Harps?e, K., Hald, H., Timmermann, D.B., et al.Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptorsJ. Biol. Chem.288(4)2559-2570(2013).
[2]. Gade, A.R., Kang, M., Khan, F., et al.Enhanced sensitivity of α3β4 nicotinic receptors in enteric neurons after long-term morphine: Implication for opioid-induced constipationJ. Pharmacol. Exp. Ther.357(3)520-528(2016).