Chemical Properties
Crystalline
Uses
4-Chloro-DL-phenylalanine has been used:
- as tryptophan hydroxylase 1 (TPH1) inhibitor to treat kras+ male zebrafish
- to induce insomnia in rat models
- used to treat embryos to examine its effect on serotonin
- for the selection of Enterococcus faecalis transformants with pESentA32 plasmid
- to feed flies to explore serotonin effect
Uses
4-Chloro-DL-phenylalanine is an irreversible tryptophan hydroxylase inhibitor that depletes serotonin in the brain.
Uses
An irreversible tryptophan hydroxylase inhibitor.
Definition
ChEBI: 2-amino-3-(4-chlorophenyl)propanoic acid is a phenylalanine derivative.
Biological Activity
4-Chloro-DL-phenylalanine (Fenclonine, PCPA, CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). 4-Chloro-DL-phenylalanine acts pharmacologically to deplete endogenous levels of serotonin.
Biochem/physiol Actions
4-Chloro-DL-phenylalanine (PCPA) is an inhibitor of 5-hydroxytrytamine (5-HT) synthesis. It helps to improve the inflammation of lung tissue and remodeling pulmonary artery. PCPA can reduce the expression of tryptophan hydroxylase 1 (TPH1), matrix metalloproteinase (MMP) and pro-inflammatory factors.
Safety Profile
An experimental
teratogen. When heated to decomposition it
emits toxic fumes of NOx and Cl-.
in vivo
4-Chloro-DL-phenylalanine(PCPA) markedly attenuates MCT(monocrotaline)-induced pulmonary vascular remodeling and lung inflammation, inhibits the expression of Tph-1 and SERT and suppresses the expression of MMP-2/-9, TIMP-1/-2, interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α) and intercellular adhesion molecule-1 (ICAM-1). PCPA inhibits 5-HT by suppressing Tph-1, regulating SERT and the serotonin downstream signaling pathway.
