NS 9283 |
Catalog No.GC45987
One-Click Copy Product Info
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NS 9283 est un modulateur allostérique positif du récepteur nicotinique de l'acétylcholine (nAChR) de la sous-unité α4β2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 913830-15-6
Sample solution is provided at 25 µL, 10mM.
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NS 9283 est un modulateur allostérique positif du récepteur nicotinique de l'acétylcholine (nAChR) de la sous-unité α4β2[1]. NARCs sont des canaux transmembranaires conventionnels contenant des cations et activés par des ligandes, appartenant à la superfamille des récepteur de la boucle Cys. Les sous-types neuronaux de ces récepteurs (par exemple, les sous-types α7 et α4β2) sont impliqués dans des processus neurocomportementaux tels que l'anxiété, le traitement central de la douleur, la prise alimentaire, le comportement de recherche de nicotine et de nombreuses fonctions cognitives[2]. NS 9283 peut être utilisé pour étudier divers troubles neurologiques, tels que le trouble du déficit de l'attention avec hyperactivité (TDAH), la schizophrénie, la maladie de Parkinson et la maladie d'Alzheimer[3, 4]. Dans des expériences électrophysiologiques, le NS 9283 peut augmenter l'amplitude des réponses évoquées par des agonistes du nAChR de types (α4)3(β2)2 [5].
In vivo, NS 9283 (3.5mg/kg) a réduit l'auto-administration de nicotine chez les rats après une injection intrapéritonéale[6]. NS 9283 (3.5μM/kg) a été administré par voie intrapéritonéale à des rats dans plusieurs modèles de douleur nociceptive/inflammatoire et a renforcé l'efficacité analgésique de ABT-594 chez les rats[7].
References:
[1] Yakel J L. Functional distribution and regulation of neuronal nicotinic ach receptors in the mammalian brain[J]. Nicotinic Receptors, 2014: 93-114.
[2] Pandya A A, Yakel J L. Effects of neuronal nicotinic acetylcholine receptor allosteric modulators in animal behavior studies[J]. Biochemical pharmacology, 2013, 86(8): 1054-1062.
[3] Hurst R, Rollema H, Bertrand D. Nicotinic acetylcholine receptors: from basic science to therapeutics[J]. Pharmacology & therapeutics, 2013, 137(1): 22-54.
[4] Terry Jr A V, Callahan P M. Nicotinic acetylcholine receptor ligands, cognitive function, and preclinical approaches to drug discovery[J]. Nicotine and Tobacco Research, 2019, 21(3): 383-394.
[5] Timmermann D B, Sandager‐Nielsen K, Dyhring T, et al. Augmentation of cognitive function by NS9283, a stoichiometry‐dependent positive allosteric modulator of α2‐and α4‐containing nicotinic acetylcholine receptors[J]. British journal of pharmacology, 2012, 167(1): 164-182.
[6] Maurer J J, Sandager-Nielsen K, Schmidt H D. Attenuation of nicotine taking and seeking in rats by the stoichiometry-selective alpha4beta2 nicotinic acetylcholine receptor positive allosteric modulator NS9283[J]. Psychopharmacology, 2017, 234: 475-484.
[7] Zhu C Z, Chin C, Rustay N R, et al. 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): 967-976.
| Cas No. | 913830-15-6 | SDF | |
| Canonical SMILES | N#CC1=CC(C2=NC(C3=CN=CC=C3)=NO2)=CC=C1 | ||
| Formula | C14H8N4O | M.Wt | 248.2 |
| Solubility | DMF: 10 mg/ml,DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml,DMSO: 3 mg/ml,Ethanol: Partially soluble | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.029 mL | 20.145 mL | 40.2901 mL |
| 5 mM | 805.8 μL | 4.029 mL | 8.058 mL |
| 10 mM | 402.9 μL | 2.0145 mL | 4.029 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)