RS 42358-197

Research use only, not for human use.

RS 42358-197 is the S-isomer of RS-42358, which is the novel 5-HT3 receptor antagonist.

RS 42358-197 is the S-isomer of RS-42358, which is the novel 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.(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.

RS42358-197; RS-42358-197; RS 25259-007

Others

Other Targets

Antifection;Platelet aggregation

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135729-55-4

330.9

C19H23ClN2O

>98% (HPLC)

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Cl.O=c1n(cc2CCCc3cccc1c23)[C@@H]1CN2CCC1CC2

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(-20℃)

With Ice Pack

≥ 2 years