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 (29)
Related Products (29)
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Antibodies (1)
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Fenclonine
0 ImagesSynonyms: 4-Chloro-DL-phenylalanine; PCPA; CP-10188Fenclonine 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
0 ImagesSynonyms: 4-Chloro-DL-phenylalanine methyl ester hydrochloridePCPA 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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4-Chloro-L-phenylalanine
0 ImagesSynonyms: L-PCPA4-Chloro-L-phenylalanine (L-PCPA) is a tryptophan hydroxylase inhibitor targeting TPH1 and TPH2, with the activity of blocking serotonin biosynthesis. 4-Chloro-L-phenylalanine reduces the levels of serotonin and its metabolites in the brain without impairing the survival of serotonergic neurons. 4-Chloro-L-phenylalanine enhances anhedonic, depression-like and anxiety-like behaviors in mice with depleted noradrenergic and dopaminergic neurons. 4-Chloro-L-phenylalanine acts as a decarboxylation substrate for aromatic L-amino acid decarboxylase from Bacillus atrophaeus. 4-Chloro-L-phenylalanine can be used in studies related to Parkinson's disease.
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LP-533401
0 ImagesLP-533401 is a Tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
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Telotristat
0 ImagesSynonyms: LP-778902Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.
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Mimosinamine
0 ImagesCat. No.: HY-182578CAS No.: 37053-15-9Mimosinamine is a hydroxylase inhibitor with Fe2+ chelating activity. Mimosinamine inhibits bovine adrenal tyrosine hydroxylase, rat liver phenylalanine hydroxylase, and rat brainstem tryptophan hydroxylase. Mimosinamine can be used in the research of hypertension.
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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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Telotristat ethyl
0 ImagesSynonyms: LX1032; LX1606Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
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Telotristat etiprate
0 ImagesSynonyms: LX1606 HippurateTelotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
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LX-1031
0 ImagesLX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
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LP-533401 hydrochloride
0 ImagesLP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
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p-Ethynylphenylalanine
0 ImagesSynonyms: 4-Ethynyl-L-phenylalaninep-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM. p-Ethynylphenylalanine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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p-Ethynylphenylalanine hydrochloride
0 ImagesSynonyms: 4-Ethynyl-L-phenylalanine hydrochloridep-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM. p-Ethynylphenylalanine (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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6-Fluorotryptophan
0 Images6-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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Rodatristat ethyl
0 ImagesSynonyms: KAR5585Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH).
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Tetrahydropapaverine hydrochloride
0 ImagesTetrahydropapaverine hydrochloride is a tetrahydroisoquinoline (TIQ) compound with inhibitory effects on tryptophan hydroxylase (TPH) (IC50 = 5.7 μM). Tetrahydropapaverine hydrochloride decreases intracellular serotonin content in murine mastocytoma P815 cells, with an IC50 value of 6.2 μM. Tetrahydropapaverine hydrochloride can be used for studies on potential neurotoxicity in monoaminergic neurons.
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Rodatristat
0 ImagesSynonyms: KAR5417Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) and TPH2 inhibitor with IC50s value of 33 nM and 7 nM, respectively, and shows robust reduction of intestinal serotonin (5-HT) levels in mice.
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TPT-004
0 ImagesTPT-004 is a selective and oraly active tryptophan hydroxylases (TPH) inhibitor with IC50s of 77 nM and 16 nM for TPH1 and TPH2, repsectively. TPT-004 exhibits exceptional selectivity for TPH1 compared with other members of the AAAH family. TPT-004 shows efficacy peripheral serotonin attenuation and colorectal tumor growth in mice[1][2].
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Fenclonine hydrochloride
0 ImagesSynonyms: 4-Chloro-DL-phenylalanine hydrochloride; PCPA hydrochloride; CP-10188 hydrochlorideFenclonine hydrochloride is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine hydrochloride can be used in carcinoid syndrome research.
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TPH1-IN-1
0 ImagesCat. No.: HY-156093CAS No.: 3040015-86-6TPH1-IN-1 (compound 40) is a xanthine derivative and an inhibitor of tryptophan hydroxylase TPH1 (IC50: 110.1 nM). TPH1-IN-1 has good in vitro activity and liver microsome stability, and effectively inhibits adipocyte differentiation of T3-L1 cells.
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