Granisetron

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Chemical Structure| 109889-09-0 同义名 : BRL 43694; Sancuso; Sustol; Granisetronum; Kevatril
CAS号 : 109889-09-0
货号 : A308320
分子式 : C18H24N4O
纯度 : 98%
分子量 : 312.41
MDL号 : MFCD00865550
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -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
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].
实验方案
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
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