Target intelligence / Profile preview

Allopregnanolone (ALLO)

Target
ALLO
Molecular classification
Neuroactive Steroid, Pregnane Steroid, GABA_A receptor positive allosteric modulator
01

Overview

Allopregnanolone is a neuroactive steroid and a metabolite of progesterone. It functions primarily as a potent positive allosteric modulator of GABA_A receptors, enhancing inhibitory neurotransmission in the central nervous system. It exhibits anxiolytic, sedative, and anticonvulsant properties, and it plays a role in neurogenesis. Dysregulation of allopregnanolone levels or sensitivity is implicated in mood disorders, particularly postpartum depression and stress-induced psychiatric conditions, making it a therapeutic target for these disorders.

Other names
3α-hydroxy-5α-pregnan-20-one3α,5α-tetrahydroprogesteroneTHP
02

Mechanism of action

Positive allosteric modulator of GABA_A receptors, enhancing GABAergic inhibition by increasing chloride ion influx. Can directly activate GABA_A receptors at high concentrations.

03

Biological functions

GABAergic neurotransmission enhancementNeurogenesisAnxiolysisSedationAnticonvulsant activityModulation of neuronal excitability
04

Disease associations

Mood disordersPostpartum depressionAnxiety disordersEpilepsyStress-related psychiatric conditions
05

Safety considerations

Potential for sedation and cognitive impairmentTolerance and dependence with long-term useInteraction with other CNS depressantsImpact on hormonal balance
06

Interacting drugs

Benzodiazepines

2 more in the full profile.

07

Biomarkers

Plasma allopregnanolone levels (for diagnosis and treatment monitoring)Cerebrospinal fluid allopregnanolone levels

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