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CAS No. : 1217474-40-2
MCE 国际站:NAS-181 dimesylate
产品活性:NAS181 是一种有效和选择性的大鼠 5-HT1B 受体拮抗剂,Ki 值为 47 nM。NAS181 对 r5-HT1B 的选择性比牛 5-HT1B 受体 (Ki=630 nM) 高 13 倍。NAS181 通过抑制末端 r5-HT1B 自身受体来增加 5-HT 转换和 5-HT 的突触浓度。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:5-HT Receptor
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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