Cited by 89Ion Channels and ReceptorsIon channel regulation and functionNeuroscience and Neuropharmacology Research

Pregnenolone sulfate: from steroid metabolite to TRP channel ligand

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Harteneck, Christian·2013·Molecules

Abstract

Pregnenolone sulfate is a steroid metabolite with a plethora of actions and functions. As a neurosteroid, pregnenolone sulfate modulates a variety of ion channels, transporters, and enzymes. Interestingly, as a sulfated steroid, pregnenolone sulfate is not the final- or waste-product of pregnenolone being sulfated via a phase II metabolism reaction and renally excreted, as one would presume from the pharmacology textbook knowledge. Pregnenolone sulfate is also the source and thereby the starting point for subsequent steroid synthesis pathways. Most recently, pregnenolone sulfate has been functionally "upgraded" from modulator of ion channels to an activating ion channel ligand. This review will focus on molecular aspects of the neurosteroid, pregnenolone sulfate, its metabolism, concentrations in serum and tissues and last not least will summarize the functional data.

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Crossref · 10.3390/molecules181012012

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  • Pregnenolone sulfate may be produced by side chain cleavage of cholesterol sulfate by CYP11A1 rather than by sulfation of pregnenolone.

    “Thus, pregnenolone sulfate which is an active neurosteroid in the brain [73], may be produced by side chain cleavage of cholesterol sulfate by CYP11A1 rather than by sulfation of pregnenolone.”

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Authors
Harteneck, C.
Affiliations
University of Tübingen (DE)
Corresponding author
Harteneck, Christian
Venue
Molecules
Publisher
MDPI AG
Published
2013-09-27
Volume
18
Issue
10
Pages
12012-12028
ISSN
1420-3049 (ISSN-L)
OpenAlex
W2049983327
Cited by
89
References
125
Citations by year
2026: 2 · 2025: 7 · 2024: 7 · 2023: 2 · 2022: 6 · 2021: 8 · 2020: 9 · 2019: 9 · 2018: 11 · 2017: 10 · 2016: 7 · 2015: 5 · 2014: 6
FWCI
0.79
Type
journal article
Language
en
Open access
Locations
  • Molecules (publishedVersion, cc-by)
  • Europe PMC (PubMed Central) (publishedVersion, other-oa)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Topics
  • Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords
pregnenolone sulfate, neurosteroids, steroid sulfates, TRP channels, ion channel modulation, steroid metabolism, phase II metabolism, steroid synthesis
MeSH terms
Animals, Humans, Ligands, Pregnenolone, Signal Transduction, Receptors, N-Methyl-D-Aspartate, Receptors, GABA, Transient Receptor Potential Channels

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