For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I010410 |
| CAS Number | 1217474-40-2 |
| Synonyms | methanesulfonic acid;(2R)-2-[[3-(morpholin-4-ylmethyl)-2H-chromen-8-yl]oxymethyl]morpholine |
| Molecular Formula | C21H34N2O10S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H26N2O4.2CH4O3S/c1-2-16-10-15(12-21-5-8-22-9-6-21)13-25-19(16)18(3-1)24-14-17-11-20-4-7-23-17;2*1-5(2,3)4/h1-3,10,17,20H,4-9,11-14H2;2*1H3,(H,2,3,4)/t17-;;/m1../s1 |
| InChIKey | WMRMIRRDPBKNMY-ZEECNFPPSA-N |
| SMILES | CS(=O)(=O)O.CS(=O)(=O)O.C1COC(CN1)COC2=CC=CC3=C2OCC(=C3)CN4CCOCC4 |
| Reference | [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. [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- |
