2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. NAS-181 dimesylate

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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NAS-181 dimesylate Chemical Structure

NAS-181 dimesylate Chemical Structure

CAS No. : 1217474-40-2

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Based on 1 publication(s) in Google Scholar

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NAS-181 dimesylate Related Antibodies

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1 Publications Citing Use of MCE NAS-181 dimesylate

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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Description

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[1][2].

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.

NAS-181 dimesylate Related Antibodies
In Vivo

NAS181 (1-10 mg/kg; s.c.) dose-dependently increases acetylcholine (ACh) release in the frontal, ventral hippocampus cortex and VHipp[1].
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.

Animal Model: Adult male Sprague-Dawley rats (250-300 g)
Dosage: 1, 5, 10 mg/kg
Administration: S.c. in the scruff of the neck
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.
Molecular Weight

538.63

Formula

C21H34N2O10S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CS(=O)(O)=O.CS(=O)(O)=O.[C@H]1(COC2=CC=CC3=C2OCC(CN4CCOCC4)=C3)CNCCO1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8566 mL 9.2828 mL 18.5656 mL
5 mM 0.3713 mL 1.8566 mL 3.7131 mL
View the 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.

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Purity & Documentation
References

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
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NAS-181 dimesylate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NAS-181 dimesylate1217474-40-25-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorrat5-HT1B5-HTInhibitorinhibitorinhibit

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