生物活性：Granisetron-d3 is the deuterium labeled Granisetron. Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy[1][2].
细胞效力(Cellular Effect)
HEK293
Cell Line
Type
Value
Description
References
HEK293
EC50
0.32 μM
Compound: Granisetron, Kutril
Agonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells by FLIPR assay
Agonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells by FLIPR assay
[PMID: 24128813]
HEK293
EC50
0.5 μM
Compound: Granisetron, Kutril
Agonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells by FLIPR assay
Agonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells by FLIPR assay
[PMID: 24128813]
HEK293
IC50
311 μM
Compound: granisetron
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
[PMID: 23241029]
HEK293
IC50
4.3 μM
Compound: granisetron
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
[PMID: 23241029]
HEK293
IC50
5 μM
Compound: granisetron
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
[PMID: 23241029]
体外研究(In Vitro)：Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Granisetron-d3 相关抗体:
MTNR1A Antibody
分子量：315.43
Formula：C18H21D3N4O
CAS 号：1224925-64-7
非标记 CAS：109889-09-0
中文名称：格拉司琼-d3
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (526 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
 [Content Brief]
[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.
 [Content Brief]
[3]. Maleki-Dizaji N, Eteraf-Oskouei T, Fakhrjou 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.
 [Content Brief]
[4]. Boccia RV, Gordan LN, Clark G, Efficacy and tolerability of transdermal granisetron for the control of chemotherapy-induced nausea and vomiting associated with moderately and highly emetogenic multi-day chemotherapy: a randomized, double-blind, phase III study. Support Care Cancer. 2011 Oct;19(10):1609-17.
 [Content Brief]