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Granisetron hydrochloride

Catalog No. T1042   CAS 107007-99-8
Synonyms: BRL 43694A, Granisetron HCl

Granisetron hydrochloride (Granisetron HCl) is a serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.

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Granisetron hydrochloride Chemical Structure
Granisetron hydrochloride, CAS 107007-99-8
Pack Size Availability Price/USD Quantity
10 mg In stock $ 32.00
25 mg In stock $ 51.00
50 mg In stock $ 74.00
100 mg In stock $ 129.00
200 mg In stock $ 188.00
500 mg In stock $ 319.00
1 mL * 10 mM (in DMSO) In stock $ 81.00
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Purity: 99.94%
Purity: 99.88%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Granisetron hydrochloride (Granisetron HCl) is a serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.
Targets&IC50 5-HT3:17μM
In vitro Granisetron blocks the delayed rectifier current (IK) of feline isolated ventricular myocytes with a KD of 4.3 mM. Granisetron shows an intrinsic voltage-dependence as the block increases with depolarization. Granisetron blocks from the intracellular side at a binding site located 10% across the transmembrane electrical field. Granisetron (3 mM) prolongs the action potential duration (APD) by about 30% at 0.5 Hz in feline isolated ventricular myocytes. [1] Granisetron but not Ondansetron, could prevent the activation of putative 5-H; autoreceptors, thus leading to a decrease in serotonin release by the enterochromaffin cells. [2]
In vivo Granisetron provides a substantial benefit against cisplatin-induced emesis in the piglet, some animals being completely protected during both the acute and the delayed phases. [2] Granisetron (1 mg/kg, i.m.) administered three times per day reduces significantly the retching+vomiting response induced by cisplatin on days 1 and 2 by 100.0% and 75.0%, respectively, in cats. [3] Granisetron or dexamethasone significantly improves macroscopic and histologic scores, curtails myeloperoxidase activity and diminishes colonic levels of inflammatory cytokines and malondialdehyde in rats. [4] Granisetron, not only prevents cholera toxin-induced jejunal net fluid secretion but also, and in proportion, inhibits 5-HT release into the intestinal lumen of mice. [5]
Synonyms BRL 43694A, Granisetron HCl
Molecular Weight 348.87
Formula C18H25ClN4O
CAS No. 107007-99-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.49 mg/mL (10 mM), Sonication is recommended.

TargetMolReferences and Literature

1. de Lorenzi FG, et al. Br J Pharmacol,1994, 113(2), 527-535. 2. Grélot L, et al. J Pharmacol Exp Ther. 1996 Oct;279(1):255-61. 3. Rudd JA, et al. Eur J Pharmacol, 2000, 391(1-2), 145-150. 4. Fakhfouri G, et al. Hum Exp Toxicol,2010, 29(4), 321-328. 5. Turvill JL, et al. Br J Pharmacol, 2000, 130(5), 1031-1036.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library GPCR Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Anti-Parkinson's Disease Compound Library

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Keywords

Granisetron hydrochloride 107007-99-8 GPCR/G Protein Neuroscience 5-HT Receptor Granisetron BRL 43694A inhibit Granisetron HCl Granisetron Hydrochloride 5-hydroxytryptamine Receptor Serotonin Receptor Inhibitor inhibitor

 

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