YM348 is a potent and orally active5-HT_2Creceptoragonist, which shows a high affinity for cloned human5-HT_2Creceptor(K_i: 0.89 nM).

YM348 has high affinity for cloned human 5-HT_2Creceptors with a K_ivalue of 0.89 nM and lower affinities for human-cloned 5-HT_2B(K_i: 2.5 nM) and 5-HT_2Areceptors (K_i: 13 nM). To assess the binding specificity of YM348, a broad evaluation of an additional 46 binding sites including several other 5-HT receptor subtypes (1A, 1B, 1D, 3, 4, 5A, 6, 7) is performed. IC₅₀values of YM348 are found to be >1 μM for all of the binding sites except for the human 5-HT_1Areceptors (K_i: 130 nM), bovine 5-HT_1Dreceptors (K_i: 481 nM), human 5-HT₇receptors (K_i: 177 nM), and human α_2Areceptors (K_i: 126 nM).YM348 exhibits a full-agonistic activity on human 5-HT_2Aand 5-HT_2Breceptors. The EC₅₀values of YM348 for 5-HT_2C, 5-HT_2A, and 5-HT_2Breceptors are 1.0, 93 and 3.2 nM, respectively^[1].

Oral administration of YM348 induces penile erections and hypolocomotion in rats, being completely inhibited by a selective 5-HT_2Creceptor antagonist, SB242084. YM348 inhibits spontaneous activity in a dose-dependent manner with a minimum effective dose of 0.203 mg/kg^[1].

243.30

Oil

C₁₄H₁₇N₃O

372163-84-3

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

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

DMSO : 100 mg/mL(411.02 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 and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (10.28 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (10.28 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (10.28 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (10.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。