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Biological Activity for NS 9283
NS 9283 is a positive 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.
Compound Libraries for NS 9283
Technical Data for NS 9283
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for NS 9283
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for NS 9283
The following data is based on the product molecular weight 248.24. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||8.06 mL||40.28 mL||80.57 mL|
|2.5 mM||1.61 mL||8.06 mL||16.11 mL|
|5 mM||0.81 mL||4.03 mL||8.06 mL|
|25 mM||0.16 mL||0.81 mL||1.61 mL|
References for NS 9283
References are publications that support the biological activity of the product.
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
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
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 receptor J.Biol.Chem. 288 35997 PMID: 24169695
If you know of a relevant reference for NS 9283, please let us know.
View Related Products by Product Action
Keywords: NS 9283, NS 9283 supplier, NS9283, Acetylcholine, nicotinic, ⓮⓶, receptors, positive, allosteric, modulators, PAM, Nicotinic, (a4b2), Receptors, 5112, Tocris Bioscience
1 Citation for NS 9283
Citations are publications that use Tocris products. Selected citations for NS 9283 include:
Wang et al (2017) Unraveling amino acid residues critical for allosteric potentiation of (α4)3(β2)2-type nicotinic acetylcholine receptor responses. J.Med.Chem. 292 9988 PMID: 28446611
Do you know of a great paper that uses NS 9283 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.