Tryptophan Hydroxylase Inhibitor

Telotristat besilate is a potent tryptophan hydroxylase inhibitor with an in vivo IC₅₀ of 0.028 μM.

TPH2 agonist-1 (compound 20e) is an orally active, blood-brain barrier permeable, 1,3,4-oxadiazol-2 (3H)-one-derived TPH2 agonist. TPH2 agonist-1 upregulates TPH2 expression, elevates 5-HT and GABA levels, and exhibits antiepileptic activity in SCN1A-deficient models. TPH2 agonist-1 stabilizes the electrophysiological activity of neuronal networks and inhibits abnormal spike and burst activities. TPH2 agonist-1 shows no significant hERG inhibition or cytotoxicity, and it can be used in studies related to severe myoclonic epilepsy of infancy (Dravet syndrome).

ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC₅₀ of 8 nM.

Fenclonine (Standard) is the analytical standard of Fenclonine. This product is intended for research and analytical applications. Fenclonine is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine can be used in carcinoid syndrome research.

PCPA methyl ester (hydrochloride) (Standard) is the analytical standard of PCPA methyl ester (hydrochloride) (HY-101456). This product is intended for research and analytical applications. PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability.

Telotristat (Standard) is the analytical standard of Telotristat. This product is intended for research and analytical applications. Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC₅₀ of 0.028 μM.

AGN‑2979 (SC 48274; BTG 1501) is an orally active and selective tryptophan hydroxylase inhibitor with antidepressant-like and anxiolytic-like activities. AGN‑2979 inhibits stress-induced activation of tryptophan hydroxylase, thereby limiting the biosynthesis of 5-hydroxytryptamine in the brain. AGN-2979 possesses non-sedative anxiolytic and cognitive-enhancing properties. AGN-2979 is applicable to research related to depression and generalized anxiety disorder.

6-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes.