A neuropeptide with diverse biological activities
Ondansetron-13C-d3 is intended for use as an internal standard for the quantification of ondansetron by GC- or LC-MS. Ondansetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 receptor (Ki = 1.6 nM).1 It is selective for the 5-HT3 receptor over the 5-HT1A-D, 5-HT2, and 5-HT4 receptors (Kis = >1,200 nM). It inhibits 5-HT-induced depolarization of isolated rat vagus nerve and contraction of isolated guinea pig ilium longitudinal muscle-myenteric plexus preparations in a concentration-dependent manner ex vivo.2 In a ferret model of cisplatin-induced emesis, ondansetron reduces the number of retching and vomiting episodes and increases the latency time to vomit when administered at a dose of 0.01 mg/kg and eliminates retching and vomiting when administered at a dose of 0.1 mg/kg.3 Ondansetron (0.5 and 1 mg/kg) also decreases immobility time in a forced swim test and increases time spent in the light chamber and latency to leave the light chamber in the light/dark exploration test in a mouse model of diabetes induced by streptozotocin , indicating antidepressant-like and anxiolytic activities.4 Formulations containing ondansetron have been used in the treatment of nausea and vomiting associated with chemotherapy, radiotherapy, or following surgery.
1.van Wijingaarden, I., Hamminga, D., van Hes, R., et al.Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivativesJournal of Medicinal Chemistry36(23)3693-3699(1993) 2.Butler, A., Hill, J.M., Ireland, S.J., et al.Pharmacological properties of GR38032F, a novel antagonist at 5-HT3 receptorsBr. J. Pharmacol.94(2)397-412(1988) 3.Stables, R., Andrews, P.L.R., Bailey, H.E., et al.Antiemetic properties of the 5HT3-receptor antagonist, GR38032FCancer Treat. Rev.14(3-4)333-336(1987) 4.Gupta, D., Radhakrishnan, M., and Kurhe, Y.Ondansetron, a 5HT3 receptor antagonist reverses depression and anxiety-like behavior in streptozotocin-induced diabetic mice: Possible implication of serotonergic systemEur. J. Pharmacol.74459-66(2014)
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