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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NAS-181 dimesylate Related Antibodies

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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)

Purity & Documentation
References
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NAS-181 dimesylate Related Classifications

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Help & FAQs
  • 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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