Ondansetron hydrochloride dihydrate

SKU: orb1308522

Description

Ondansetron hydrochloride dihydrate

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 103639-04-9
• MW: 365.86
• Purity: 99.71%
• Formula: C₁₈H₁₉N₃O·HCl·2H₂O
• SMILES: c12c3c(n(c1CCC(C2=O)Cn1c(ncc1)C)C)cccc3.Cl.O.O
• Target: 5-HT Receptor
• Solubility: DMSO:10 mg/mL (27.33 mM);Ethanol:38 mg/mL (103.86 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.73 mM);H2O:67 mg/mL (183.13 mM)

Bioactivity

• Target IC50:
  5-HT3 receptor:810 nM
• In Vivo:
  Ondansetron(Ond) is well tolerated and its side effects are mild. Ond acts on the CNS as well as on the peripheral nervous system (PNS). Ondansetron is available both for oral and intravenous administration. The bioavailability of orally administered ondansetron is only 60%. The low bioavailability is due to a significant first-pass metabolism. The peak plasma concentration of ondansetron is usually reached at approximately 1.5 h after oral administration. A major portion of this drug, about 75%, is bound to plasma proteins. Ondansetron is currently used to prevent and treat nausea and vomiting associated with chemotherapy, radiation treatment and general anesthesia. It has been shown to inhibit GABA and glycine receptor activity in animal models. Therapeutic dose of Ond allows delivery of significantly higher amounts of Dox to the brain tissue in vivo, which is otherwise disallowed by the BBB. The rate of penetration of the blood-brain barrier by Ond is very low.
• In Vitro:
  Ondansetron is a potent, highly selective, competitive antagonist at 5-HT3 receptors. It demonstrates some affinity to other receptor subtypes, including 5-HT1B, 5-HT1C, 5-HT4, opioid, and 1-adrenergic receptors, and to the μ-opioid receptor. However, ondansetron has 1000:1 selectivity toward 5-HT3 receptors. Ondansetron is found to be the most potent HERG-channel blocker among several 5-HT3 antagonists, with an IC50 of 810 nM and has been reported to block Na+ channels.
• Cell Research:
  Cells are plated in 60-mm Petri dishes (2×105 per dish) and cultured in serumcontained medium for 24 h. The next day the medium is removed and serum-contained medium with or without Dox (0.1 or 0.5 μg/ml) and Ond (10 or 30 μg/ml) in combination or respectively, is added. After 3 days, the cells are washed twice with PBS, trypsinized, and counted by using the trypan blue exclusion method.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5HTReceptor, 5-hydroxytryptamine Receptor, 5HT Receptor, 5-HT3, 5-HT Receptor, cancer surgery, cancer chemotherapy, inhibit, NSC 665799, nausea, Ondansetron Hydrochloride, Ondansetron hydrochloride, Ondansetron hydrochloride dihydrate, Ondansetron hydrochloride Dihydrate, NSC665799, NSC-665799, GR38032, GR-38032, GR 38032, GR 38032 hydrochloride dihydrate, Inhibitor, Serotonin Receptor, radiation, SN307, SN-307, SN 307, SN 307 hydrochloride dihydrate, vomiting

Compound Identifiers

PubChem CID

59774