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 receptor. 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 syndrome. 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 tachycardia.
产品描述
A Potent and Selective Blocker of 5-Hydroxytryptamine Receptor 3A
产品形式
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 channel.
