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Pregnenolone Sulfate: From Steroid Metabolite to TRP Channel Ligand

Department of Pharmacology and Experimental Therapy, Institute of Experimental and Clinical Pharmacology and Toxicology, Eberhard Karls University, Tübingen 72074, Germany
Hospitals and Clinics, Interfaculty Center of Pharmacogenomics and Drug Research, University of Tübingen, Tübingen 72074, Germany
Molecules 2013, 18(10), 12012-12028;
Received: 2 September 2013 / Revised: 20 September 2013 / Accepted: 21 September 2013 / Published: 27 September 2013
(This article belongs to the Special Issue Steroids)
PDF [952 KB, uploaded 18 June 2014]


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. View Full-Text
Keywords: neurosteroids; pregnenolone sulfate; steroid metabolism; ion channel modulation; TRP channels neurosteroids; pregnenolone sulfate; steroid metabolism; ion channel modulation; TRP channels

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Harteneck, C. Pregnenolone Sulfate: From Steroid Metabolite to TRP Channel Ligand. Molecules 2013, 18, 12012-12028.

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