1217474-40-2

1217474-40-2 structure

Name: NAS181
Chemical Name: NAS-181
CAS Number: 1217474-40-2
Molecular Formula: C₂₁H₃₄N₂O₁₀S₂
Molecular Weight: 538.632
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2021-05-03 14:26:03
Modify Date: 2024-01-09 20:42:42
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].

Name	NAS-181
Synonyms	Morpholine, 2-[[[3-(4-morpholinylmethyl)-2H-1-benzopyran-8-yl]oxy]methyl]-, (2R)-, methanesulfonate (1:2) MFCD06798366 (2R)-2-({[3-(4-Morpholinylmethyl)-2H-chromen-8-yl]oxy}methyl)morpholine methanesulfonate (1:2)

Description	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].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	Rat 5-HT1B Receptor:47 nM (IC50)
In Vitro	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].
In Vivo	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]. Animal Model: Adult male Sprague-Dawley rats (250-300 g) Dosage: 1, 5, 10 mg/kg Administration: S.c. in the scruff of the neck Result: Increased the ACh release in the frontal cortex, reaching the maximal value of 500% of the control group within 80 min after the injection of the highest dose. Increased the ACh releases in VHipp with a maximum of 230% of the control values at 80 min after the injection of the highest dose.
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. [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.

Molecular Formula	C₂₁H₃₄N₂O₁₀S₂
Molecular Weight	538.632
Exact Mass	538.165466

205242-62-2	1217474-40-2
114198-85-5	14993-64-7
15749-46-9	14993-65-8
1092443-52-1	824960-03-4
1883548-83-1	1397219-81-6
1158522-08-7	940364-43-2
134104-43-1	2138245-16-4
131615-57-1	6906-52-1
930439-75-1	1018584-77-4
1375289-11-4	849349-65-1