Description
Allopregnanolone is an endogenous inhibitory pregnane neurosteroid that is synthesized from progesterone . It acts as a positive allosteric modulator of GABA
A receptors at nM concentrations (exhibiting the greatest potentiation at isoforms containing δ subunits) and of GABA
C receptors at μM concentrations. Allopregnanolone displays effects similar to other GABA
A receptor potentiators such as benzodiazepines, including potent anticonvulsant, anxiolytic, and sedative activity.
Uses
(3α)-Allopregnanolone acts as a GABAA receptor positive allosteric modulator. (3α)-Allopregnanolone is a metabolite of Progesterone (P755900). (3α)-Allopregnanolone is a neuroactive steroid present in the blood and also the brain.
Definition
ChEBI: Brexanolone is a 3-hydroxy-5alpha-pregnan-20-one in which the hydroxy group at position 3 has alpha-configuration. It is a metabolite of the sex hormone progesterone and used for the treatment of postpartum depression in women. It has a role as a human metabolite, an antidepressant, a GABA modulator, an intravenous anaesthetic and a sedative.
Biological Activity
GABA A receptor positive allosteric modulator. Neuroactive steroid.
References
1) Belelli and Lambert (2005),?Neurosteroids: endogenous regulators of the GABA(A) receptor; Nat. Rev. Neurosci,,?6?565
2) Reddy?et al. (2010),?Neurosteroids: endogenous role in the human brain and therapeutic potentials; Prog. Brain Res.,?186?113
3) Frieder?et al. (2019),?Pharmacotherapy of Postpartum Depression: Current Approaches and Novel Drug Development; CNS Drugs,?33?265
4) Balan?et al.?(2019),?Endogenous Neurosteroid (3α,5α)3-Hydroxypregnan-20-one Inhibits Toll-like-4 Receptor Activation and Proinflammatory Signaling in Macrophages and Brain; Sci. Rep.,?9?1220
5) Chang?et al.?(2019),?Neurosteroid allopregnanolone inhibits glutamate release from rat cerebrocortical nerve terminals; Synapse,?73?e22076
6) Cho?et al.?(2018),?Increased Superoxide Dismutase 2 by Allopregnanolone Ameliorates ROS-Mediated Neuronal Death in Mice with Pilocarpine-Induced Status Epilepticus; Neurochem. Res.,?43?1464
