Tetrahydropapaverine is a tryptophan hydroxylase inhibitor with IC50 value of 5.7μM for inactivating tryptophan hydroxylase prepared from the P815 cells, leading to a decrease in serotonin content by the inhibition of tryptophan hydroxylase activity. Tetrahydropapaverine dose-dependently decreased serotonin content at concentration ranging in 5-20μM in P815 cells and inhibitied serotonin content by 42.1% at 5μM post 24h. Tetrahydropapaverine un-competitively inhibited P815-tryptophan hydroxylase with the substrate L-tryptophan, and non-competitively with the cofactor DL-6-methyl-5,6,7,8-tetrahydropteridin. Tetrahydropapaverine exhibited toxic effect on TH-positive neurons and total cells with EC50 value of 180μ and 265μM, respectively.
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