Biological Activity
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
NS 9283 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 248.24 |
| Formula | C14H8N4O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 913830-15-6 |
| PubChem ID | 11998180 |
| InChI Key | HGFXDSQLRSWUBO-UHFFFAOYSA-N |
| Smiles | N#CC1=CC(C2=NC(C3=CN=CC=C3)=NO2)=CC=C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 4.96 | 20 | |
| DMSO | 12.41 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 248.24. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.03 mL | 20.14 mL | 40.28 mL |
| 5 mM | 0.81 mL | 4.03 mL | 8.06 mL |
| 10 mM | 0.4 mL | 2.01 mL | 4.03 mL |
| 50 mM | 0.08 mL | 0.4 mL | 0.81 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: NS 9283, supplier, NS9283, Acetylcholine, nicotinic, ⓮⓶, receptors, positive, allosteric, modulators, Nicotinic, (a4b2), Receptors, Nicotinic, (a4b2), Receptors, Tocris Bioscience
