fenclonine

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    Fenclonine, also known as para-chlorophenylalanine (PCPA), acts as a selective and irreversible inhibitor of tryptophan hydroxylase, which is a rate-limiting enzyme in the biosynthesis of serotonin.
    It has been used experimentally to treat carcinoid syndrome, but the side effects, mostly hypersensitivity reactions and psychiatric disturbances, have prevented development for this use.
    The effects of serotonin depletion from fenclonine are so drastic that serotonin cannot even be detected immunohistochemically within the first day after administration of a control dose. Tryptophan hydroxylase activity can be detected neither in cell bodies or nerve terminals. After one week 10% of control values (the baseline extrapolated for the study) had replenished in the raphe nucleus, and after two weeks from initial treatment as much was again detected in the hypothalamus region. Aromatic L-amino acid decarboxylase (AADC) levels were at no time affected.
    It is used in scientific research in humans and animals to investigate the effects of serotonin depletion.


    See also


    α-Methyl-para-tyrosine (AMPT, metirosine)
    para-Chloroamphetamine (PCA)
    Telotristat ethyl (Xermelo)
    AGN-2979


    References

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fenclonine

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Fenclonine - Wikipedia

Fenclonine, also known as para-chlorophenylalanine (PCPA), acts as a selective and irreversible inhibitor of tryptophan hydroxylase, which is a rate-limiting enzyme in the biosynthesis of serotonin. [2]

Fenclonine | C9H10ClNO2 | CID 4652 - PubChem

A selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine acts pharmacologically to deplete endogenous levels of serotonin.

Fenclonine - an overview | ScienceDirect Topics

Fenclonine is a 5-HT depleting agent that selectively and irreversibly blocks tryptophan hydroxylase, the key enzyme in the synthesis pathway of serotonin (5-HT), leading to a reduction in serotonin levels.

Fenclonine - an overview | ScienceDirect Topics

The history of the development of 5-HTP as an effective treatment for fibromyalgia began with studies on the drug fenclonine.58 This drug blocks the enzyme that inhibits the conversion of tryptophan to 5-HTP and, as a result, blocks serotonin production.

FENCLONINE - gsrs.ncats.nih.gov

fenclonine [inn] SRS_LOCATOR Kai Waløen, Rune Kleppe, Aurora Martinez & Jan Haavik (2017) Tyrosine and tryptophan hydroxylases as therapeutic targets in human disease, Expert Opinion on Therapeutic Targets, 21:2, 167-180, DOI: 10.1080/14728222.2017.1272581

FENCLONINE - National Center for Advancing Translational …

Fenclonine, also known as p-chlorophenylalanine, is an inhibitor of tryptophan hydroxylase, the enzyme that plays a rate-limiting role in the biosynthesis of serotonin. Fenclonine was studied for the treatment of carcinoid syndrome, but the psychological side effects, prevented for the further development for this use.

Clinical and biochemical effects of fenclonine: a serotonin

Clinical and biochemical effects of fenclonine: a serotonin depletor. Clinical and biochemical effects of fenclonine: a serotonin depletor Dis Nerv Syst. 1968 May;29(5):Suppl:147-52. Authors V Y Cremata Jr, B K Koe. PMID: 5673619 No abstract available. Publication types ...

Fenclonine - MeSH - NCBI - National Center for Biotechnology …

A selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine acts pharmacologically to deplete endogenous levels of serotonin. Year introduced: 1993 (1971) Restrict to …

Fenclonine (4-Chloro-DL-phenylalanine) - MedChemExpress

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.

(2R)-2-amino-3- (4-chlorophenyl)propanoic acid - PubChem

(2R)-2-amino-3- (4-chlorophenyl)propanoic acid | C9H10ClNO2 | CID 667429 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.