NDLI: Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor.

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Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Rojas, Camilo Stathis, Marigo Thomas, Ajit G. Massuda, Ed B. Massuda, Edward B. Alt, Jesse Zhang, Jie Rubenstein, Edward Rubenstein, Ed Sebastiani, Silvia Cantoreggi, Sergio Snyder, Solomon H. Slusher, Barbara
Description	Country affiliation: United States Author Affiliation: Rojas C ( Research and Translational Development, MGI PHARMA INC, 6611 Tributary St., Baltimore, MD 21224-6515, USA. camilo.rojas@mgipharma.com)
Abstract	BACKGROUND: Palonosetron is a 5-HT(3)-receptor antagonist (5-HT(3)-RA) that has been shown to be superior to other 5-HT(3)-RAs in phase III clinical trials for the prevention of acute, delayed, and overall chemotherapy-induced nausea and vomiting. The improved clinical efficacy of palonosetron may be due, in part, to its more potent binding and longer half-life. However, these attributes alone are not sufficient to explain the results with palonosetron. We sought to elucidate additional differences among 5-HT(3)-RAs that could help explain the observations in the clinic. METHODS: Receptor site saturation binding experiments were performed with [3H] palonosetron, [3H] granisetron, and [3H] ondansetron to obtain the corresponding Scatchard analyses and Hill coefficients. Diagnostic equilibrium binding experiments and kinetic dissociation experiments were conducted to examine competitive versus potential allosteric interactions between ondansetron, granisetron and palonosetron and the 5-HT(3) receptor. Finally, the long-term effect of the three antagonists on receptor function as measured by Ca2+ influx in HEK 293 cells expressing the 5-HT(3)-receptor was compared. RESULTS: Analyses of binding isotherms using both Scatchard and Hill plots suggested positive cooperativity for palonosetron and simple bimolecular binding for both granisetron and ondansetron. Equilibrium diagnostic tests discriminated differential effects of palonosetron on [3H] ligand binding indicating that palonosetron was an allosteric antagonist whereas granisetron and ondansetron were competitive antagonists. Using dissociation rate strategies, palonosetron was shown to be an allosteric modifier that accelerated the rate of dissociation from the receptor of both granisetron and ondansetron. Differences in the binding mode of palonosetron to the 5-HT(3) receptor were shown to have an impact on receptor function. In these experiments, cells were incubated with each antagonist, followed by infinite dilutions and dissociation for 2.5 h; cells previously incubated with either granisetron or ondansetron showed calcium-ion influx similar to control cells that had not been exposed to a 5-HT(3) receptor antagonist. In contrast, substantial inhibition of calcium-ion influx was observed in cells that had been incubated with palonosetron. CONCLUSIONS: Palonosetron exhibited allosteric binding and positive cooperativity when binding to the 5-HT(3) receptor. Palonosetron also triggered functional effects that persisted beyond its binding to the 5-HT(3) receptor at the cell surface. Differences in binding and effects on receptor function may be relevant to the unique beneficial actions of palonosetron. To our knowledge, this is the first report showing palonosetron's interaction with the 5-HT(3) receptor at the molecular level, clearly differentiating it from other 5-HT(3)-RAs.
File Format	HTM / HTML
ISSN	00032999
Issue Number	2
Volume Number	107
e-ISSN	15267598
Journal	Anesthesia & Analgesia
Language	English
Publisher	Lippincott Williams & Wilkins
Publisher Date	2008-08-01
Publisher Place	United States
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Discipline Anesthesiology Antiemetics Metabolism Isoquinolines Quinuclidines Receptors, Serotonin, 5-ht3 Animals Binding Sites Calcium Cell Line Granisetron Ondansetron Postoperative Nausea And Vomiting Prevention & Control Radioligand Assay Serotonin 5-ht3 Receptor Antagonists Transfection Journal Article
Content Type	Text
Resource Type	Article
Subject	Anesthesiology and Pain Medicine

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