NAS-181 dimesylate
Based on 3 publication(s) in Google Scholar
NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors.
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- Pureté: 96.37%
- CAS No.: 1217474-40-2
- Formule: C21H34N2O10S2
- Masse moléculaire:538.63
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NAS-181 dimesylate
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Activité biologique
Description
IC50 & Target
[1]|
Rat 5-HT1B Receptor 47 nM (IC50) |
In Vitro
NAS181 has very low affinities (Ki>3000 nM) for all other receptors examined, including 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7, α1-, α2-, and β-adrenoceptors, and dopamine D1 and D2[1].
NAS181 (10-1000 nM) dose-dependently potentiates the K+-stimulated [3H]-5-HT release in preloaded rat occipital cortical slices[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NAS181 (20 mg/kg; s.c.) enhances the 5-HT turnover in four rat brain regions (hypothalamus, hippocampus, striatum, and frontal cortex) with about 40%[1].
NAS181 (3 mg/kg; s.c.) produces a significant increase in the number of wet dog shakes in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats (250-300 g)
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Dosage:1, 5, 10 mg/kg
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Administration:S.c. in the scruff of the neck
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Result:Increased the ACh release in the frontal cortex, reaching the maximal value of 500% of the control group within 80 min after the injection of the highest dose.
Increased the ACh releases in VHipp with a maximum of 230% of the control values at 80 min after the injection of the highest dose.
Chemical Information
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CAS No. 1217474-40-2
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Appearance Solid
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Masse moléculaire 538.63
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Formule C21H34N2O10S2
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Color Off-white to light yellow
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SMILES
CS(=O)(O)=O.CS(=O)(O)=O.[C@H]1(COC2=CC=CC3=C2OCC(CN4CCOCC4)=C3)CNCCO1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
Distinct serotonergic pathways to the amygdala underlie separate behavioral features of anxiety. [Abstract]2022 Dec;25(12):1651-1663. PMID: 36446933 -
Transl Neurodegener
Dorsal raphe nucleus-hippocampus serotonergic circuit underlies the depressive and cognitive impairments in 5×FAD male mice. [Abstract]2024 Jul 24;13(1):34. PMID: 39044270 -
Solvant et solubilité
In Vitro:
DMSO : 62.5 mg/mL (116.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Berg S, et, al. (R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist. J Med Chem. 1998 May 21;41(11):1934-42. [Content Brief]
[2]. Hu XJ, et, al. Effects of the 5-HT1B receptor antagonist NAS-181 on extracellular levels of acetylcholine, glutamate and GABA in the frontal cortex and ventral hippocampus of awake rats: a microdialysis study. Eur Neuropsychopharmacol. 2007 Sep;17(9):580- [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8566 mL | 9.2828 mL | 18.5656 mL | 46.4141 mL |
| 5 mM | 0.3713 mL | 1.8566 mL | 3.7131 mL | 9.2828 mL | |
| 10 mM | 0.1857 mL | 0.9283 mL | 1.8566 mL | 4.6414 mL | |
| 15 mM | 0.1238 mL | 0.6189 mL | 1.2377 mL | 3.0943 mL | |
| 20 mM | 0.0928 mL | 0.4641 mL | 0.9283 mL | 2.3207 mL | |
| 25 mM | 0.0743 mL | 0.3713 mL | 0.7426 mL | 1.8566 mL | |
| 30 mM | 0.0619 mL | 0.3094 mL | 0.6189 mL | 1.5471 mL | |
| 40 mM | 0.0464 mL | 0.2321 mL | 0.4641 mL | 1.1604 mL | |
| 50 mM | 0.0371 mL | 0.1857 mL | 0.3713 mL | 0.9283 mL | |
| 60 mM | 0.0309 mL | 0.1547 mL | 0.3094 mL | 0.7736 mL | |
| 80 mM | 0.0232 mL | 0.1160 mL | 0.2321 mL | 0.5802 mL | |
| 100 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.4641 mL |
NAS-181 dimesylate Related Classifications
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