NAS-181 free base 

NAS181 free base is a potent and selective antagonist of rat 5-HT_1B receptor, with a K_i of 47 nM. NAS181 free base shows 13-fold selectivity for r5-HT_1B over bovine 5-HT_1B receptor (K_i=630 nM). NAS181 free base increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT_1B autoreceptors^[1][2].

NAS181 has very low affinities (K_i>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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

346.42

C₁₉H₂₆N₂O₄

205242-61-1

[C@@H]1(CNCCO1)COC2=C3C(C=C(CO3)CN4CCOCC4)=CC=C2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]