NAS-181 free base
Based on 3 publication(s) in Google Scholar
NAS181 free base is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 free base shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 free base increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors.
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- CAS No.: 205242-61-1
- 화학식: C19H26N2O4
- 분자량:346.42
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NAS-181 free base
MoreAll 5-HT Receptor Isoforms
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Biological Activity
제품 설명
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. 205242-61-1
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분자량 346.42
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화학식 C19H26N2O4
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SMILES
[C@@H]1(CNCCO1)COC2=C3C(C=C(CO3)CN4CCOCC4)=CC=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
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 -
순도&문서
References
[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):580-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NAS-181 free base Related Classifications
HY-135507A Related Classifications
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