1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. NAS181

NAS181 

Cat. No.: HY-103156
Handling Instructions

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.

For research use only. We do not sell to patients.

NAS181 Chemical Structure

NAS181 Chemical Structure

CAS No. : 1217474-40-2

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

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.
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Please store the product under the recommended conditions in the Certificate of Analysis.

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NAS181
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HY-103156
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