Granisetron | BRL 43694 | 5-HT Receptor Antagonist | AmBeed-信号通路专用抑制剂

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格拉司琼 /Granisetron 98%

货号：A308320 同义名： BRL 43694;Sancuso

Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

Granisetron 化学结构
CAS号：109889-09-0

Granisetron 3D分子结构
CAS号：109889-09-0

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Granisetron 纯度/质量文件产品仅供科研

货号：A308320 标准纯度： 98% 产品说明书

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

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024. Ambeed. [ A288696 ]; • JMC, 2024. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

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 (human platelets), IC50: 240 μM 5-HT (rat brain synaptosomes), IC50: 474 μM								99%+
Venlafaxine	✔								99%+
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%+
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								99%+
Trazodone	✔								98+%
Clomipramine HCl	✔								99%+
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								99%+
Duloxetine	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								99%+
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								99%+
Latrepirdine 2HCl	✔							GluR	99%+
Fluoxetine hydrochloride	✔								98%
Paroxetine hydrochloride	✔							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						98%
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 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM						99%
Agomelatine			✔						99%+
Clozapine			✔						99%+
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					99%+
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					99%+
VUF10166				++++ 5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM					99%+
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					98%
Asenapine maleate		+++ 5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6	++++ 5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		99%+
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		99%+
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-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		98%
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。

Granisetron 生物活性

靶点

5-HT3

描述

Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy^[1]. In other models of 5-HT3 receptor activity (rabbit isolated heart, Bezold-Jarisch reflex in anaesthetised rats), potent antagonism by BRL 43694 was demonstrated^[2]. Leukocyte accumulation was dose-dependently inhibited by granisetron both at 6 and 72 h after induction of inflammation. Granisetron increased PGE(2) level at a lower dose (50 microg/pouch) but higher doses (100 and 200 microg/pouch) inhibited the release. At the same time, TNFalpha production was decreased by the lower dose and increased by higher doses of granisetron in a reciprocal fashion^[3]. Granisetron protects against sepsis-induced ALI (acute lung injury) by suppressing macrophage Cxcl1/Cxcl2 expression and neutrophil recruitment in the lung^[4].

Granisetron 参考文献

[1]Duggan ST, Curran MP. Transdermal granisetron. Drugs. 2009;69(18):2597-605

[2]Sanger GJ, Nelson DR. Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron). Eur J Pharmacol. 1989 Jan 10;159(2):113-24

[3]Maleki-Dizaji N, Eteraf-Oskouei T, Fakhrjou A, Maljaie SH, Garjani A. The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation. Int Immunopharmacol. 2010 Sep;10(9):1010-6

[4]Wang J, Gong S, Wang F, Niu M, Wei G, He Z, Gu T, Jiang Y, Liu A, Chen P. Granisetron protects polymicrobial sepsis-induced acute lung injury in mice. Biochem Biophys Res Commun. 2019 Jan 22;508(4):1004-1010

[5]Maleki-Dizaji N, Eteraf-Oskouei T, Fakhrjou A, Maljaie SH, Garjani A. The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation. Int Immunopharmacol. 2010 Sep;10(9):1010-6

[6]Wang J, Gong S, Wang F, Niu M, Wei G, He Z, Gu T, Jiang Y, Liu A, Chen P. Granisetron protects polymicrobial sepsis-induced acute lung injury in mice. Biochem Biophys Res Commun. 2019 Jan 22;508(4):1004-1010

Granisetron 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

16.00mL

3.20mL

1.60mL

32.01mL

6.40mL

3.20mL

Granisetron 技术信息

CAS号	109889-09-0
分子式	C₁₈H₂₄N₄O
分子量	312.409

别名	BRL 43694;Sancuso;Sustol;Granisetronum;Kevatril
运输	蓝冰

存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(80.02 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

格拉司琼 /Granisetron 98%

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最近浏览的产品

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