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DMSO: 35mg/mL; H2O: 64mg/mL; EtOH: <1mg/mL
Selective 5-HT3 receptor antagonist and alpha-7-nicotinic receptor agonist
REVIEW Tropisetron is a highly potent and selective competitive antagonist of the 5-HT3 receptor, a subclass of serotonin receptors located on peripheral neurons and within the CNS. Surgery and treatment with certain substances, including some chemotherapeutic agents, may trigger the release of serotonin (5-HT) from enterochromaffin-like cells in the visceral mucosa and initiate the emesis reflex and its accompanying feeling of nausea. Tropisetron selectively blocks the excitation of the presynaptic 5-HT3 receptors of the peripheral neurons in this reflex, and may exert additional direct actions within the CNS on 5-HT3 receptors mediating the actions of vagal input to the area postrema.
Muller, W.; T. Stratz (2004). Local treatment of tendinopathies and myofascial pain syndromes with the 5-HT3 receptor antagonist tropisetron. Scand J Rheumatic Suppl. 119 (119): 44-48. PMID 15515413. Retrieved 2007-05-17.
Macor JE, Gurley D, Lanthorn T, Loch J, Mack RA, Mullen G, Tran O, Wright N, Gordon JC (February 2001). The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist. Bioorganic & Medicinal Chemistry Letters 11 (3): 319-21. doi:10.1016/S0960-894X(00)00670-3. PMID 11212100.
Cui R, Suemaru K, Li B, Kohnomi S, Araki H (May 2009). Tropisetron attenuates naloxone-induced place aversion in single-dose morphine-treated rats: role of alpha7 nicotinic receptors. European Journal of Pharmacology 609 (1-3): 74-7. doi:10.1016/j.ejphar.2008.12.051. PMID 19374878.
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