Granisetron hydrochloride

SKU: orb1227041

Description

Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. IC50 Value: 17uM (GR reduced 5-HT-evoked contractions)(In Vitro):In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. In isolated rabbit heart, GR 0.003-0.03 nM dose-dependently reduced s-HT tachycardia; at high levels GR reduced submaximal and maximal responses to 5-HT.(In Vivo):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. The GTDS displayed non-inferiority to oral granisetron: complete control was achieved by 60% of patients in the GTDS group, and 65% in the oral granisetron group (treatment difference, -5%; 95% confidence interval, -13-3). Both treatments were well tolerated, the most common adverse event being constipation.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 107007-99-8
• MW: 348.87
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₅ClN₄O
• SMILES: Cl.CN1N=C(C(=O)NC2CC3CCCC(C2)N3C)C2=CC=CC=C12
• Target: 5-HT Receptor
• Solubility: Ethanol: 1 mg/mL (2.86 mM); Water: 70 mg/mL (200.64 mM); DMSO: 1 mg/mL (2.86 mM)

Bioactivity

• In Vivo:
  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. The GTDS displayed non-inferiority to oral granisetron: complete control was achieved by 60% of patients in the GTDS group, and 65% in the oral granisetron group (treatment difference,-5%; 95% confidence interval,-13-3). Both treatments were well tolerated, the most common adverse event being constipation.
  Read more...
• In Vitro:
  In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. In isolated rabbit heart, GR 0.003-0.03 nM dose-dependently reduced s-HT tachycardia; at high levels GR reduced submaximal and maximal responses to 5-HT.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRL 43694

Quick Database Links

Gene Symbol

5-HT Receptor