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G蛋白偶联受体/G蛋白
神经信号通路
/ 5-羟色胺受体 / Ritanserin/利坦色林

Ritanserin/利坦色林 {[allProObj[0].p_purity_real_show]}

货号：A189213 同义名： 利坦丝林 / R 55667

Ritanserin is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research.

Ritanserin/利坦色林 化学结构 CAS号：87051-43-2
Ritanserin/利坦色林 化学结构
CAS号：87051-43-2
Ritanserin/利坦色林 3D分子结构
CAS号：87051-43-2
Ritanserin/利坦色林 化学结构 CAS号：87051-43-2
Ritanserin/利坦色林 3D分子结构 CAS号：87051-43-2
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Ritanserin/利坦色林 纯度/质量文件 产品仅供科研

货号：A189213 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

 		98%
Venlafaxine ✔ 99%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 99%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 99%
Fluoxetine HCl ✔ 99.5%
Paroxetine HCl ✔ AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		95%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

 		99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

 		98%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

 		99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

 		98%
Tropisetron ✔ 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron HCl dihydrate ✔ 98%
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

 		99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

 		99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

 		++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ritanserin/利坦色林 生物活性

描述 Ritanserin is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors[3]. Ritanserin blocked CaV1.2 channel currents (ICa1.2) in a concentration-dependent manner (Kr = 3.61 µM); ICa1.2 inhibition was antagonized by Bay K 8644 and partially reverted upon washout. Conversely, the ritanserin analog ketanserin (100 µM) inhibited ICa1.2 by ~50%[4]. Ritanserin attenuates DGKα (Diacylglycerol kinase alpha) kinase activity while increasing the enzyme's affinity for ATP in vitro. In addition, R59022 and ritanserin function as DGKα inhibitors in cultured cells and activate protein kinase C (PKC)[5]. Ritanserin at doses of 1 and 3 mg/kg inhibited the development and expression of METH(methamphetamine)-induced behavioral sensitization in a dose-dependent manner. Furthermore, acute ritanserin inhibited METH challenge-induced increase in extracellular 5-HT but not DA levels in the prefrontal cortex[6].

Ritanserin/利坦色林 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00000187 Cocaine-Related Disorders Phase 2 Completed - United States, Pennsylvania ... 展开 >> University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 6178 收起 <<

Ritanserin/利坦色林 参考文献

[1]Gaikwad U, Parle M, et al. Effect of ritanserin and leuprolide alone and combined on marble-burying behavior of mice. Acta Pol Pharm. 2010 Sep-Oct;67(5):523-7.

[2]Johnson BA, Jasinski DR, et al. Ritanserin in the treatment of alcohol dependence--a multi-center clinical trial. Ritanserin Study Group. Psychopharmacology (Berl). 1996 Nov;128(2):206-15.

[3]Leysen JE, Gommeren W, Van Gompel P, Wynants J, Janssen PF, Laduron PM. Receptor-binding properties in vitro and in vivo of ritanserin: A very potent and long acting serotonin-S2 antagonist. Mol Pharmacol. 1985 Jun;27(6):600-11

[4]Fusi F, Trezza A, Sgaragli G, Spiga O, Saponara S, Bova S. Ritanserin blocks CaV1.2 channels in rat artery smooth muscles: electrophysiological, functional, and computational studies. Acta Pharmacol Sin. 2020 Sep;41(9):1158-1166

[5]Boroda S, Niccum M, Raje V, Purow BW, Harris TE. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017 Jan 1;123:29-39

[6]Ago Y, Nakamura S, Kajita N, Uda M, Hashimoto H, Baba A, Matsuda T. Ritanserin reverses repeated methamphetamine-induced behavioral and neurochemical sensitization in mice. Synapse. 2007 Sep;61(9):757-63

Ritanserin/利坦色林 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.94mL

4.19mL

2.09mL

Ritanserin/利坦色林 技术信息

CAS号87051-43-2
分子式C27H25F2N3OS
分子量 477.57
SMILES Code CC1=C(CCN2CCC(CC2)=C(C2=CC=C(F)C=C2)C2=CC=C(F)C=C2)C(=O)N2C=CSC2=N1
MDL No. MFCD00069341
别名 利坦丝林 ;R 55667
运输蓝冰
InChI Key JUQLTPCYUFPYKE-UHFFFAOYSA-N
Pubchem ID 5074
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二

Tags: Ritanserin | 87051-43-2 | R 55667 | R55667 | R-55667 | Histamine Receptor Inhibitor | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | 5-HT Receptor | Histamine Receptor | Dopamine Receptor | Adrenergic Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ritanserin/利坦色林 纯度/质量文件 | Ritanserin/利坦色林 亚型比较 | Ritanserin/利坦色林 生物活性 | Ritanserin/利坦色林 临床数据 | Ritanserin/利坦色林 参考文献 | Ritanserin/利坦色林 实验方案 | Ritanserin/利坦色林 技术信息

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