RS 42358-197

SKU: orb1705449

Description

RS 42358-197 (RS 25259-007) is a selective antagonist of the serotonin 5-HT3 receptor. This compound is utilized in neuroscience and pharmacology research to investigate receptor function and modulation in both cellular assays and animal models of emesis and nociception.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 135729-55-4
• MW: 330.85
• Purity: 99.70% (May vary between batches)
• Formula: C₁₉H₂₃ClN₂O
• SMILES: O=C1C2=C3C(=CN1[C@H]4C5CCN(C4)CC5)CCCC3=CC=C2.Cl
• Target: 5-HT Receptor
• Solubility: DMSO:11 mg/mL (33.25 mM)

Bioactivity

• In Vivo:
  In anesthetized rats. RS 42358-197, administered by the intravenous, intraduodenal or transdermal route, dose-dependently inhibited the Bezold-Jarisch reflex induced by 2-methyl 5-HT (ID50:0.05 micrograms/kg; i.v., 5.7 micrograms/kg; i.d., and 11.6 micrograms/chamber, respectively). In this regard, when administered intraduodenally, RS 42358-197 was more potent and exhibited a longer duration of action than either ondansetron or granisetron. In dogs, RS 42358-197, administered either intravenously or orally, dose-dependently inhibited the emesis induced by cisplatin, actinomycin and cyclophosphamide, but not that induced by apomorphine. When tested at maximally effective doses against cisplatin-induced emesis in dogs, RS 42358-197 had a longer duration of antiemetic activity (> 6 h) than ondansetron (2 h). RS 42358-197, administered orally, also afforded protection against cisplatin-induced emesis in ferrets. At doses that showed marked anti-emetic activity in dogs (10-100 micrograms/kg; i.v. and 100-1000 micrograms/kg; i.d.), RS 42358-197 did not produce any hemodynamic changes.
• In Vitro:
  RS 42358-197 acts against 5-HT-induced contractions in the guinea pig ileum (low-potency phase), yielding a pA2 estimate of 8.1.

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5HTReceptor, 5HT Receptor, 5-HT3, RS-42358-197, RS42358-197, RS 25259-007, RS 42358-197

Compound Identifiers

PubChem CID

148209