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Tropisetron Hydrochloride

CAS No. : 105826-92-4

Biological Activity：Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
IC50 value: 70.1 ± 0.9 nM
Target: 5-HT3 receptor; α7-nicotinic receptor
in vitro: Retinal ganglion cells(RGCs) pretreated with 100 nM tropisetron before glutamate increased cell survival to an average of 105% compared to controls. Inhibition studies using the alpha7 nAChR antagonist, MLA (10 nM), support the hypothesis that tropisetron is an effective neuroprotective agent against glutamate-induced excitotoxicity; mediated by α7 nAChR activation. Tropisetron had no discernible effects on pAkt levels but significantly decreased p38 MAPK levels associated with excitotoxicity from an average of 15 ng/ml to 6 ng/ml [2]. Tropisetron, but not granisetron, significantly inhibits the phosphatase activity of calcineurin, over-expresses the CB(1) receptors at both transcriptional and protein levels, and reduces cAMP content in cerebellar granule neurons (CGNs) [4].
in vivo: Animals were treated intracerebroventricularly with tropisetron, mCPBG (selective 5-HT3 receptor agonist) or mCPBG plus tropisetron on days 1, 3, 5 and 7. Tropisetron significantly diminished the elevated levels of these markers and reversed the cognitive deficit. Interestingly, tropisetron was also found to be a potent inhibitor of calcineurin phosphatase activity [1]. tropisetron (5mg/kg/day) plus mCPBG (10mg/kg/day), and granisetron (5mg/kg/day) intraperitoneally on days 3-35 post-immunization. Treatment with tropisetron and granisetron markedly suppressed the clinical symptoms of EAE (p<0.001) and reduced leukocyte infiltration as well as demyelination in the spinal cord (p<0.05) [3].

Research Area：Neurological Disease

Targets：5-HT Receptor

Related Screening Libraries:Drug Repurposing Compound Library Plus;FDA-Approved Drug Library Plus;FDA-Approved Drug Library Mini;Bioactive Compound Library Plus;GPCR/G Protein Compound Library;Neuronal Signaling Compound Library;FDA-Approved Drug Library;Anti-Cancer Compound Library;CNS-Penetrant Compound Library;Drug Repurposing Compound Library;NMPA-Approved Drug Library;Orally Active Compound Library;Neurotransmitter Receptor Compound Library;FDA Approved & Pharmacopeial Drug Library;Anti-Alzheimer’s Disease Compound Library;Neuroprotective Compound Library;Anti-Parkinson’s Disease Compound Library;Neurodegenerative Disease-related Compound Library;5-HT Receptor Compound Library;FDA-Approved Anticancer Drug Library;Coagulation and Anti-coagulation Compound Library;

Related Small Molecules:F 13714;Mosapride-d5;Nuciferine;Renzapride;LY 344864 racemate;Harmine hydrochloride;Valerenic acid;Arotinolol;Melitracen-d6 hydrochloride;WAY-100635;Nelotanserin;Flupentixol-d4 dihydrochloride;Cariprazine-d6 hydrochloride;Tetrahydro-β-carboline;CP-809101;Volinanserin-d4 hydrochloride;Masupirdine free base;BRL-15572 dihydrochloride;LY393558;Brexpiprazole S-oxide

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