Tryptophan Hydroxylase Inhibitor

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 (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.

4-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.

LP-533401 is a Tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC₅₀ of 0.028 μM.

Mimosinamine 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.

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).

Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.

LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a K_i 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.

p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a K_i 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.

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

Rodatristat 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).

Tetrahydropapaverine 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.

Rodatristat (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.

TPT-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].

Fenclonine 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.

TPH1-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.