Ramosetron HCl | YM060 | 5-HT Receptor Antagonist | AmBeed-信号通路专用抑制剂

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Ramosetron HCl/盐酸雷莫司琼 {[allProObj[0].p_purity_real_show]}

货号：A671888 同义名： YM060; Ramosetron (hydrochloride)

Ramosetron HCl is a potent and selective 5-HT3 receptor antagonist for the treatment of nausea and vomiting.

Ramosetron HCl/盐酸雷莫司琼化学结构
CAS号：132907-72-3

Ramosetron HCl/盐酸雷莫司琼 3D分子结构
CAS号：132907-72-3

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Ramosetron HCl/盐酸雷莫司琼纯度/质量文件产品仅供科研

货号：A671888 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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5-羟色胺受体亚型比较

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 (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 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 (Rat), Ki: 50 nM 5-HT2C (Human), Ki: 2.5 nM						99%+
Loxapine succinate			++ 5-HT2 (bovine), Ki: 6.6 nM 5-HT2 (human), Ki: 6.8 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-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 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-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4	++++ 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-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 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-HT1D, pKi: 6 5-HT1B, pKi: 6.1	++ 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。

Ramosetron HCl/盐酸雷莫司琼生物活性

靶点

5-HT3

5-HT3 receptor, Ki:0.091 nM
5-HT3

5-HT3 receptor, Ki:0.091 nM

描述

Ramosetron Hydrochloride, a selective 5-HT3 receptor antagonist, has been on the market as an antiemetic drug for cancer patients receiving chemotherapy or anesthesia. The effective dose of ramosetron (hydrochlorid) to be injected for the near-complete prophylaxis of PONV (Postoperative nausea and vomiting) 6 to 24 hours after surgery in high-risk patients is a 0.6 mg bolus injection at the end of the surgery^[2]. Moreover, ramosetron (hydrochlorid) administered during induction of anaesthesia may affect maximal change in QTc interval during off-pump coronary artery bypass surgery^[3].

Ramosetron HCl/盐酸雷莫司琼参考文献

[1]Yahagi R, Machida Y, Onishi H. Mucoadhesive suppositories of ramosetron hydrochloride utilizing Carbopol. Int J Pharm. 2000 Jan 5;193(2):205-12.

[2]Lee S, Jeong S, Kim J, Jeong S. Effective Dose of Ramosetron for Prophylaxis of Postoperative Nausea and Vomiting in High-Risk Patients. Biomed Res Int. 2015;2015:951474. doi: 10.1155/2015/951474. Epub 2015 Jul 14. PMID: 26258145; PMCID: PMC4516817.

[3]Kim TK, Cho YJ, Lim CW, Min JJ, Choi EK, Hong DM, Jeon Y. Effect of ramosetron on QTc interval: a randomised controlled trial in patients undergoing off-pump coronary artery bypass surgery. BMC Anesthesiol. 2016 Aug 3;16(1):56. doi: 10.1186/s12871-016-0222-1. PMID: 27488394; PMCID: PMC4972982.

Ramosetron HCl/盐酸雷莫司琼实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.83mL

3.17mL

1.58mL

31.67mL

6.33mL

3.17mL

Ramosetron HCl/盐酸雷莫司琼技术信息

CAS号	132907-72-3
分子式	C₁₇H₁₈ClN₃O
分子量	315.8
SMILES Code	O=C(C1=CN(C)C2=C1C=CC=C2)[C@@H](C3)CCC4=C3NC=N4.[H]Cl
MDL No.	MFCD00894748

别名	YM060; Ramosetron (hydrochloride); Ramosetron Hydrochloride
运输	蓝冰
InChI Key	XIXYTCLDXQRHJO-RFVHGSKJSA-N
Pubchem ID	107999

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案

动物实验：配制的工作液建议现用现配，短期内尽快用完。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

Ramosetron HCl/盐酸雷莫司琼 {[allProObj[0].p_purity_real_show]}

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5-HT3	5-HT3 receptor, Ki:0.091 nM
5-HT3	5-HT3 receptor, Ki:0.091 nM

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