描述

Allopregnanolone is under investigation for the treatment of Super-Refractory Status Epilepticus.Allopregnanolone has been investigated for the treatment of Severe Postpartum Depression.

IC50 & Target

GABA,

体外

Allopregnanolone induces a significant increase in proliferation of neuroprogenitor cells derived from the rat hippocampus and human neural stem cells derived from the cerebral cortex in a dose-dependent manner. Allopregnanolone increases the expression of genes that promote mitosis and inhibits the expression of genes that repress cell proliferation. Its biosynthesis begins with progesterone, which is converted to dihydroprogesterone by the enzyme 5α-DHP and after that, the enzyme 3α-HSOR catalyses the reduction of dihydroprogesterone toward allopregnanolone.

体内

• Allopregnanolone increases both the K+-evoked [3H]-glutamate and [3H]-GABA release in P rats. The neurosteroid also increases the basal release of [3H]-glutamate in VO rats in an effect that is dependent on the modulation of NMDA receptors as is reverted by Mg2+. At therapeutic doses by either subcutaneous or intravenous routes, allopregnanolone mouse plasma levels range between 34-51ng/mL by 30min. Allopregnanolone-induced neurogenesis correlates with restoration of learning and memory function in a mouse model of Alzheimer’s disease and is comparably efficacious in aged normal mice. Progesterone and allopregnanolone has shown neuroprotective effects in different experimental models including stroke and spinal cord injury.

1 mg

5 mg

10 mg

1 mM

3.1398 mL

15.6991 mL

31.3982 mL

5 mM

0.6280 mL

3.1398 mL

6.2796 mL

10 mM

0.3140 mL

1.5699 mL

3.1398 mL

50 mM

0.0628 mL

0.3140 mL

0.6280 mL