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
AGN-2979 is a glutarimide tryptophan hydroxylase activation inhibitor. It shows antidepressant properties in rodent models of Depression (mood), depression.
References
Glutarimides
O-methylated phenols
Tryptophan hydroxylase inhibitors ...
References
Amino acid derivatives
Chloroarenes
Tryptophan hydroxylase inhibitors
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