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[1][2].

Product Specifications

CAS Number

[1217474-40-2]

UNSPSC

12352005

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/nas181.html

Concentration

10mM

Purity

96.37

Solubility

DMSO : 62.5 mg/mL (ultrasonic)

Smiles

CS(=O)(O)=O.CS(=O)(O)=O.[C@H]1(COC2=CC=CC3=C2OCC(CN4CCOCC4)=C3)CNCCO1

Molecular Formula

C21H34N2O10S2

Molecular Weight

538.63

References & Citations

[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) :580-6.