| Name | RS 42358-197 |
| Description | RS 42358-197 (RS 25259-007) is a competitive 5-HT3 receptor antagonist. |
| 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[1]. |
| 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[1]. |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 11 mg/mL (33.25 mM)
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| Keywords | RS 42358-197 |
| Inhibitors Related | Serotonin hydrochloride | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Mirtazapine | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
United States
