Cat. No. 5112
Chemical Name: 3-[3-(3-Pyridinyl)-1,2,4-oxadiazol-
Biological ActivityPositive allosteric modulator of α4β2 receptor; increases the potency of Ach-evoked currents ~60 fold without effecting the maximum efficacy (HEK293-hα4β2 cells). Reduces the rate of recovery from desensitization and slows the rate of deactivation. Displays a synergistic effect on the Emax when given with NS206 at 3α:2β receptors.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Mohler et al (2014) Discriminative-stimulus effects of NS9283, a nicotinic α4β2* positive allosteric modulator, in nicotine-discriminating rats. Psychopharmacology (Berl). 231 67. PMID: 23925734.
Grupe et al (2013) Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. Br.J.Pharmacol. 168 2000. PMID: 23278456.
Olsen et al (2013) Two distinct allosteric binding sites at α4β2 nicotinic acetylcholine receptors revealed by NS206 and NS9283 give unique insights to binding activity-associated linkage at Cys-loop receptors. J.Biol.Chem. 288 35997. PMID: 24169695.
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Keywords: NS 9283, supplier, NS9283, Acetylcholine, nicotinic, ⓮⓶, receptors, positive, allosteric, modulators, Tocris Bioscience, Nicotinic (α4β2) Receptor Modulator products
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Potent positive allosteric modulator of α4β2 nAChRs; also inhibitor of (α4)2(β2)3, muscle-type and Torpedo nAChRs
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