Allopregnanolone

Description: Allopregnanolone, also known as 5alpha-pregnan-3alpha-ol-20-one or 3alpha, 5alpha-tetrahydroprogesterone (3alpha, 5alpha-THP), or SAGE-547, Brexanolone, and Allotetrahydroprogesterone, is a progesterone metabolite that serves as an allosteric modulator of the GABA (gamma-aminobutyric acid) receptor. It has the potential for the treatment of Alzheimer’s Disease, epilepsy and depression. Allopregnanolone is an endogenous inhibitory pregnane neurosteroid that is synthesized from progesterone. Allopregnanolone has effects similar to those of other positive allosteric modulators of the GABA action at GABAA receptor such as the benzodiazepines, including anxiolytic, sedative, and anticonvulsant activity. Endogenously produced allopregnanolone exerts a pivotal neurophysiological role by fine-tuning of GABAA receptor and modulating the action of several positive allosteric modulators and agonists at GABAA receptor.

References: J Neurosci. 2005 May 11; 25(19):4706-18; PLoS One. 2015 Jun 3; 10(6):e0128313; Neuroscience. 2013 Jul 23; 243:64-75.