913830-15-6

NS 9283 is a positive allosteric modulator of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs) that potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC₅₀ = 4 μM). In vivo, NS 9283 potentiates ABT-594 analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia, paw skin incision post-operative pain, and monoiodoacetate-induced osteoarthritis. It reduces nicotine, but not sucrose, self-administration and reinstatement in rats when administered at a dose of 3.5 mg/kg.

NS 9283 is a positive allosteric modulator of α4β2 receptor affecting the potency of acetylcholine (Ach) related events. This has been linked to affect on everyday brain function including cognitive function and pain alleviation.

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[1] M GRUPE. Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors[J]. British Journal of Pharmacology, 2012, 168 8: 2000-2010. DOI: 10.1111/bph.12095
[2] CHANG Z. ZHU. Potentiation of analgesic efficacy but not side effects: Co-administration of an α4β2 neuronal nicotinic acetylcholine receptor agonist and its positive allosteric modulator in experimental models of pain in rats[J]. Biochemical pharmacology, 2011, 82 8: Pages 967-976. DOI: 10.1016/j.bcp.2011.05.007
[3] J. MAURER H S K Sandager‐Nielsen. Attenuation of nicotine taking and seeking in rats by the stoichiometry-selective alpha4beta2 nicotinic acetylcholine receptor positive allosteric modulator NS9283[J]. Psychopharmacology, 2016, 234 1: 475-484. DOI: 10.1007/s00213-016-4475-7