Allopregnanolone (516-54-1) is an endogenous neurosteroid which acts as a positive allosteric modulator of GABAA receptors.1,2 Recently FDA approved (Brexanolone) for postpartum depression.3 Inhibits TLR4 receptor activation and inflammatory signaling in macrophages and brain.4 Inhibits glutamate release5 and displays neuroprotective effects in various animal models6.
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