| Bioactivity | 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]. |
| Invitro | 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NAS-181 free base 相关抗体: |
| 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 205242-61-1 |
| Formula | C19H26N2O4 |
| Molar Mass | 346.42 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
NAS-181 free base
CAS: 205242-61-1 F: C19H26N2O4 W: 346.42
NAS181 free base is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 free base shows
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.