NAS181 is a potent and selective antagonist ofrat 5-HT_1Breceptor, with aK_iof 47 nM. NAS181 shows 13-fold selectivity for r5-HT_1Bover bovine 5-HT_1Breceptor (K_i=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT_1Bautoreceptors^[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].

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].

538.63

Solid

C₂₁H₃₄N₂O₁₀S₂

1217474-40-2

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 62.5 mg/mL(116.04 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。