Tropisetron-d5 is intended for use as an internal standard for the quantification of tropisetron by GC- or LC-MS. Tropisetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 5.3 nM).1,2 It is also an antagonist of the α9 nicotinic acetylcholine receptor (nAChR; IC50 = 166 nM) and a partial agonist of the α7 nAChR (Ki = 6.9 nM).3,4
1.Mawe, G.M., Branchek, T.A., and Gershon, M.D.Peripheral neural serotonin receptors: Identification and characterization with specific antagonists and agonistsProc. Natl. Acad. Sci. USA83(24)9799-9803(1986) 2.Round, A., and Wallis, D.I.The depolarizing action of 5-hydroxytryptamine on rabbit vagal afferent and sympathetic neurones in vitro and its selective blockade by ICS 205-930Br. J. Pharmacol.88(2)485-494(1986) 3.Shiina, A., Shirayama, Y., Niitsu, T., et al.A randomised, double-blind, placebo-controlled trial of tropisetron in patients with schizophreniaAnn. Gen. Psychiatry9(27)(2010) 4.Rothlin, C.V., Katz, E., Verbitsky, M., et al.The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptorsMol. Pharmacol.55(2)248-254(1999)