Methiothepin mesylate|74611-28-2|(马来酸甲硫替平; Metitepine mesylate; Ro 8-6837 mesylate)-陌孚医药/Medlife

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Methiothepin mesylate (Synonyms: 马来酸甲硫替平; Metitepine mesylate; Ro 8-6837 mesylate)

目录号: PL01631 纯度: ≥98%

CAS No. :74611-28-2

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中文名称	Methiothepin mesylate
中文别名	马来酸甲硫替平
英文名称	Methiothepin mesylate
英文别名	METHIOTHEPIN MESYLATE SEROTININ 5-HT(1) ANT;methanesulfonic acid,1-methyl-4-(3-methylsulfanyl-5,6-dihydrobenzo[b][1]benzothiepin-5-yl)piperazine;1-[10,11-Dihydro-8-(methylthio)dibenzo[b,f]thiepin-10-yl]-4-methylpiperazine mesylate salt;AC1MI866;Methiothepin mesylate;Methiothepin mesylate salt;Methiothepin methanesulfonate;Metitepine mesylate salt;Piperazine, 1-(10,11-dihydro-8-(methylthio)dibenzo(b,f)thiepin-10-yl)-4-methyl-, methanesulfonate;Metitepine mesylate;Ro 8-6837 mesylate
Cas No.	74611-28-2
分子式	C₂₀H₂₄N₂S₂^.CH₄O₃S
分子量	452.65
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	Methiothepin mesylate 是一种有效的，非选择性的 5-HT₂ receptor 拮抗剂，pK_d 值为 7.10 (5-HT_1A)，7.28 (5HT_1B)，7.56 (5HT_1C)，6.99 (5HT_1D)，7.0 (5-HT_5A)，7.8 (5-HT_5B)，8.74 (5-HT₆) 和 8.99 (5-HT₇)，pK_i 值为 8.50 (5HT_2A)，8.68 (5HT_2B) 和 8.35 (5HT_2C)。
生物活性	Methiothepin mesylate is a potent and non-selective 5-HT 2 receptor antagonist, with pK d s of 7.10 (5-HT 1A ), 7.28 (5HT 1B ), 7.56 (5HT 1C ), 6.99 (5HT 1D ), 7.0 (5-HT 5A ), 7.8 (5-HT 5B ), 8.74 (5-HT 6 ), and 8.99 (5-HT 7 ), and pK i s of 8.50 (5HT 2A ), 8.68 (5HT 2B ), and 8.35 (5HT 2C ).
性状	Solid
IC50 & Target[1][2]	5-HT1A Receptor 7.10 (pKd) 5-HT1B Receptor
体外研究(In Vitro)	Methiothepin mesylate is a 5-HT receptor antagonist, with pKds of 7.10, 7.28, 7.56, and 6.99 for 5-HT1A, 5HT1B, 5HT1C, 5HT1D. Methiothepin mesylate also shows pKds of 7.0, 7.8, 8.74, and 8.99 for 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7, respectively. Methiothepin exhibits high affinity at 5-HT2A, 5HT2B, and 5HT2C with pKis of 8.50, 8.68, and 8.35, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Schoeffter P, et al. 5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype. J Pharmacol Exp Ther. 1990 Jan;252(1):387-95. [2]. Knight AR, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. Epub 2004 Jul 30.

溶解度数据	In Vitro: DMSO : 62.5 mg/mL (138.08 mM; Need ultrasonic)H₂O : 50 mg/mL (110.46 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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