p-Chlorophenylalanine is a TPH inhibitor working by binding irreversibly to tryptophanhydroxylase to cause depletion of serotonin in the brain.
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P-Chlorophenylalanine is a synthetic 5-HT inhibitor mainly used to investigate the effects of near-total depletion of 5-HT. Intraperitoneal injection with 100mg/kg and 150mg/kg decreased 5-HT and 5-HIAA (the 5-HT metabolite) concentrations significantly in all brain regions, including cortex, striatum, hippocampus, hypothalamus and brain stem, with greater decreases at the higher dose in rats. Dose of p-Chlorophenylalanine, 100mg/kg once daily for 3 days, blocked the effects of central tryptophan on thermoregulation and performance, accelerated cutaneous heat dissipation, and abolished the fatigue in exercising rats dosed with tryptophan, i.c.v. .
作用机制
P-chlorophenylalanine is a competitive inhibitor of tryptophan hydroxylase in vitro.[3]
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