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.

Product information

CAS Number: 1217474-40-2

Molecular Weight: 538.63

Formula: C21H34N2O10S2

Chemical Name: (2R)-2-[({3-[(morpholin-4-yl)methyl]-2H-chromen-8-yl}oxy)methyl]morpholine; bis(methanesulfonic acid)

Smiles: CS(O)(=O)=O.CS(O)(=O)=O.C(C1COC2=C(C=CC=C2C=1)OC[C@H]1CNCCO1)N1CCOCC1

InChiKey: WMRMIRRDPBKNMY-ZEECNFPPSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. NAS181 (10-1000 nM) dose-dependently potentiates the K+-stimulated [3H]-5-HT release in preloaded rat occipital cortical slices.

In Vivo:

NAS181 (1-10 mg/kg; s.c.) dose-dependently increases acetylcholine (ACh) release in the frontal, ventral hippocampus cortex and VHipp. 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%. NAS181 (3 mg/kg; s.c.) produces a significant increase in the number of wet dog shakes in rats.

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