Progesterone and progestins: effects on brain, allopregnanolone and beta-endorphin.

Details

Serval ID
serval:BIB_EF250A61090B
Type
Article: article from journal or magazin.
Publication sub-type
Review (review): journal as complete as possible of one specific subject, written based on exhaustive analyses from published work.
Collection
Publications
Title
Progesterone and progestins: effects on brain, allopregnanolone and beta-endorphin.
Journal
The Journal of steroid biochemistry and molecular biology
Author(s)
Pluchino N., Luisi M., Lenzi E., Centofanti M., Begliuomini S., Freschi L., Ninni F., Genazzani A.R.
ISSN
0960-0760 (Print)
ISSN-L
0960-0760
Publication state
Published
Issued date
12/2006
Peer-reviewed
Oui
Volume
102
Number
1-5
Pages
205-213
Language
english
Notes
Publication types: Journal Article ; Research Support, Non-U.S. Gov't ; Review
Publication Status: ppublish
Abstract
The increased use of hormonal therapies over the last years has led to improve the knowledge of pharmacological, biochemical and metabolic properties of several progestins and their effects in target tissues, such as the central nervous system. Progesterone and synthetic progestational agents are able to modulate the synthesis and release of several neurotransmitters and neuropeptides in response to specific physiological and pathological stimuli. While these actions may relay on differential activation of progesterone receptor or recruitment of intracellular pathways, some of the differences found between synthetic progestins may depend on the specific conversion to neuroactive steroids, such as the 3-alpha, 5-alpha reduced metabolite, allopregnanolone. This is a potent endogenous steroid that rapidly affects the excitability of neurons and glia cells through direct modulation of the GABA-A receptors activity exerting hypnotic/sedative, anxiolytic, anaesthetic and anticonvulsive properties. Estrogens increase the CNS and serum levels of allopregnanolone and the addition of certain but not all synthetic progestins determines a further increase in allopregnanolone levels, suggesting that the metabolism into this reduced product is related to the chemical structure of progestin molecule used. In addition, depending on specific progestin molecule used, different interaction are found with the estradiol-induced beta-endorphin synthesis and release, showing that diverse progestins have specific and divergent actions on the opiatergic system. These results highlight the concept that natural and synthetic progesterone receptor agonists may systematically induce different biological actions in CNS. This may have far-reaching implications for the clinical effects and related indications of each compound.
Keywords
Animals, Brain/drug effects, Humans, Pregnanolone/metabolism, Progesterone/pharmacology, Progesterone/physiology, Progestins/pharmacology, Progestins/physiology, beta-Endorphin/metabolism
Pubmed
Web of science
Create date
15/09/2023 12:25
Last modification date
27/09/2023 9:33
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