Tryptophan Hydroxylase
Tryptophan hydroxylase (TPH) is the rate-limiting enzyme in the biosynthesis of the biogenic monoamine serotonin (5-hydroxytryptamine, 5-HT). TPH belongs to the family of the aromatic amino acid hydroxylases, including phenylalanine hydroxylase (PAH) and tyrosine hydroxylase (TH), which all have a strict requirement for dioxygen, non-heme iron (II) and tetrahydrobiopterin (BH4).Tryptophan hydroxylase is activated by phosphorylating conditions (ATP-Mg2+) in a calcium-dependent, cyclic AMP-independent manner. Two existing TPH isoforms (TPH-1 and TPH-2) are responsible for the generation of two distinct serotonergic systems in vertebrates.
TPH1, predominantly expressed in the gastrointestinal tract and pineal gland, mediates 5-HT biosynthesis in non-neuronal tissues, while TPH2, mainly found in the raphe nuclei of the brain stem, is accountable for the production of 5-HT in the brain. TPH-1, the principal enzyme for peripheral serotonin biosynthesis, provides a novel target to design anabolic agents for osteoporosis. TPH2 is a phenotypic marker for serotonin neurons and is known to be extremely labile to oxidation. As a major modulator of 5-HT neurotransmission and the stress response, TPH2 is of both pathophysiological and pharmacological significance, and is emerging as a new therapeutic target for the treatment of stress disorders.
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Tryptophan Hydroxylase Related Products (30)
Related Products (30)
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Antibodies (1)
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Telotristat besilate
0 ImagesCat. No.: HY-13055ECAS No.: 1374745-52-4Telotristat besilate is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.
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Fenprinast
0 ImagesCat. No.: HY-19596CAS No.: 75184-94-0
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TPH2 agonist-1
0 ImagesCat. No.: HY-181575TPH2 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).
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ACT-678689
0 ImagesACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM.
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Oudenone derivative-1 potassium
0 ImagesCat. No.: HY-170738CAS No.: 34200-97-0Oudenone derivative-1 potassium is a derivative of Oudenone. Oudenone, a metabolite of the fungus, is a catecholamine biosynthesis and tyrosine hydroxylases inhibitor.
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Fenclonine (Standard)
0 ImagesSynonyms: 4-Chloro-DL-phenylalanine (Standard); PCPA (Standard); CP-10188 (Standard)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.
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PCPA methyl ester hydrochloride (Standard)
0 ImagesCat. No.: HY-101456RCAS No.: 14173-40-1Synonyms: 4-Chloro-DL-phenylalanine methyl ester hydrochloride (Standard)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.
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Telotristat (Standard)
0 ImagesSynonyms: LP-778902 (Standard)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.
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AGN-2979
0 ImagesCat. No.: HY-19046ACAS No.: 53873-21-5Synonyms: SC 48274; BTG 1501AGN‑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.
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6-Fluorotryptophan (Standard)
0 ImagesCat. No.: HY-W092533RCAS No.: 7730-20-36-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes.
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