1217474-40-2
1217474-40-2
Chemical Structure
NAS-181 dimesylate
- CAS. Nr.: 1217474-40-2
- Formula:C21H34N2O10S2
- Molecular Weight:538.63
IUPAC Name: (R)-2-(((3-(morpholinomethyl)-2H-chromen-8-yl)oxy)methyl)morpholine dimethanesulfonate
InChIKey: WMRMIRRDPBKNMY-ZEECNFPPSA-N
SMILES: CS(=O)(O)=O.CS(=O)(O)=O.[C@H]1(COC2=CC=CC3=C2OCC(CN4CCOCC4)=C3)CNCCO1
Biological Activity: 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].
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NAS-181 dimesylate | 96.37% | 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 (Standard) | ≥98% | NAS-181 dimesylate (Standard) is the analytical standard of NAS-181 dimesylate (HY-103156). This product is intended for research and analytical applications. 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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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- [Content Brief]
