NAS-181 (free base)
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[1][2].
Product Specifications
CAS Number
205242-61-1
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/nas-181-free-base.html
Smiles
[C@@H]1(CNCCO1)COC2=C3C(C=C(CO3)CN4CCOCC4)=CC=C2
Molecular Formula
C19H26N2O4
Molecular Weight
346.42
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
5-HT1 Receptor
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