Every lot is tried & tested in a relevant biological assay.
- Sanger, G.J. and Nelson, D.R. (1989) Eur.J.Pharmacol. 159, 113.
- Alomone Labs Granisetron Hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells.Currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Antagonist Granisetron hydrochloride (#G-105) was applied 30 seconds before stimulation at 1 and 10 nM, as indicated and inhibited the 5-HT induced current in a dose-dependent and reversible manner.
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid Tryptophan by the enzyme Tryptophan-decarboxylase. The 5-HT3 channel is a ligand gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.
Granisetron Hydrochloride is a synthetic, potent and selective antagonist of 5-HT3A channel. Unlike other 5-HT antagonists Granisetron has little affinity for other receptors while having a pKi of 8.42 for 5-HT3A receptor2. Granisetron binds to an extracellular domain of the receptor. Currently, Granisetron is widely used in clinical practices to prevent vomiting and diarrhea post chemotherapy, radiotherapy and surgery. It was also found to alleviate the effects of irritable bowel syndrome3. Granisetron and other antiemetics induce cardiovascular side effects including orthostatic hypotension and the prolongation of the QT interval that might cause Torsades de Pointes (TdP) ventricular tachycardia4.
Granisetron hydrochloride (#G-105) is a highly pure, synthetic, and biologically active compound.