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- W2568416364 abstract "Abstract Abstract 4826 Introduction Clinical studies have shown that palonosetron is more effective than first generation 5-HT3 receptor antagonists (5HT3RAs) for preventing chemotherapy induced nausea and vomiting (CINV). In addition, NK-1 receptor antagonists have been shown to augment the the antiemetic activity of the 5HT3RAs and dexamethasone to inhibit CINV. While palonosetron is effective in preventing delayed CINV, it does not directly bind to the NK-1 receptor. Recent data, however, has revealed significant receptor “cross-talk” between the NK-1 and 5HT3 signaling pathways. Alteration of 5HT3 receptor activity has been shown to cause downstream effects on NK-1 signaling, and vice versa. We postulated that if palonosetron differentially inhibited the NK-1/5HT3 crosstalk, this could help explain the differences observed in the clinic. Methods We carried out in vivo electrophysiology experiments in rats where single neuronal recordings of nodose ganglia expressing both NK-1 and 5HT3 receptors were collected. Results First, we showed that neuronal responses to substance P (SP), a known non-selective agonist of the NK-1 receptor, were significantly enhanced in the presence of cisplatin. Second, we found that palonosetron, but not ondansetron or granisetron (1st generation 5HT3RAs), could dose-dependently inhibit the cisplatin-induced SP enhancement. This inhibition was observed when palonosetron was administered 30 minutes before or 5 or 10 h after cisplatin administration. Conclusion The results are consistent with previous mechanism of action (MOA) experiments indicating that palonosetron uniquely exhibits allosteric binding, positive cooperativity and receptor internalization at the 5HT3 receptor. Taken together, the MOA studies may help explain the unique results observed with palonosetron in the clinic. Disclosures Li: Eisai, Inc: Research Funding. Wu:Eisai: Research Funding. Rojas:Eisai, Inc: Employment. Cantoreggi:Helsinn Healthcare: Employment. Sebastiani:Helsinn Healthcare: Employment. Slusher:Eisai, Inc: Employment." @default.
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- W2568416364 date "2009-11-20" @default.
- W2568416364 modified "2023-09-28" @default.
- W2568416364 title "Palonosetron Uniquely Inhibits Substance P-Mediated Neuronal Responses in Rat Nodose Ganglia." @default.
- W2568416364 doi "https://doi.org/10.1182/blood.v114.22.4826.4826" @default.
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