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产品总数：61489
| 中文名称 |
Ketanserin tartrate
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| 中文别名 |
酒石酸酮色林;酮舍林酒石酸盐;酒石酸酮色啉盐;酮肟物
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| 英文名称 |
Ketanserin tartrate
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| 英文别名 |
Ketanserin tartrate;Ketanserin tartrate,3-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-2,4[1H,3H]-quinazolinedionetartrate;Ketanserine tartrate;R41468 tartrate;KJK 945;Ket;Perketan;R 49945;Serepress;Sufrexal;Ketanserin;Ketanserinum;Ketaserin;Ketanserina;Ketanserine;Ketanserinum [INN-Latin];Ketanserine [INN-French];3-(2-(4-(4-Fluorobenzoyl)piperidin-1-yl)ethyl)quinazoline-2,4(1H,3H)-dione;Ketanserina [INN-Spanish];R 41468;[3H]-Ketanserin;R 41,468;C22H22FN3O3;3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione;97F9DE4CT4;FPCCSQOGAWCVBH-UHFFFAOYSA-N;3-[2-[4-(4-fluorobenzoyl)-1-piperi
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| Cas No. |
83846-83-7
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| 分子式 |
C22H22FN3O3
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| 分子量 |
395.43
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| 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)
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| 产品详情 |
Ketanserin (R41468) tartrate 是一种选择性的 5-HT2 receptor 拮抗剂。Ketanserin tartrate 也抑制 hERG 电流 (IhERG)，IC50 为 0.11 μM，这种作用具有浓度依赖性。
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| 生物活性 |
Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (I hERG ) in a concentration-dependent manner (IC 50 =0.11 μM).
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| 性状 |
Solid
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| IC50 & Target[1][2] |
5-HT2 Receptor hERG current 0.11 μM (IC50)
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| 体外研究(In Vitro) |
Ketanserin at 0.3 μM inhibits the voltage-dependent step current (IhERG.step) and tail current (IhERG.tail) of hERG channels with a 5-min exposure. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC50=22.0±7 μM), Ketanserin (IC50=152±23 μM). Ketanserin (50-350 μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC50 value of Cyproheptadine is 22±7 μM and Ketanserin is 152±23 μM. Ketanserin inhibits platelet aggregation with an IC50 of 240 (169-339) nM. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT 2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 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)
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| ClinicalTrial |
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| 参考文献 |
[1]. Tang Q, et al. The 5-HT2 antagonist Ketanserin is an open channel blocker of human cardiac ether-à-go-go-related gene (hERG) potassium channels. Br J Pharmacol. 2008 Oct;155(3):365-73.[2]. Khan N, et al. Investigation of cyclooxygenase and signaling pathways involved in human platelet aggregation mediated by synergistic interaction of various agonists. Drug Des Devel Ther. 2015 Jul 6;9:3497-506.
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| 溶解度数据 |
In Vitro: DMSO : 125 mg/mL (229.14 mM; Need ultrasonic)H2O : 6 mg/mL (11.00 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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