Gosset Molecular Classification
Neuroactive Steroid, Pregnane Steroid, GABA_A receptor positive allosteric modulator
Other Names
3α-hydroxy-5α-pregnan-20-one, 3α,5α-tetrahydroprogesterone, THP
Disease Roles
Allopregnanolone 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.
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.
Biological Functions
GABAergic neurotransmission enhancement
Neurogenesis
Anxiolysis
Sedation
Anticonvulsant activity
Modulation of neuronal excitability
Disease Associations
Mood disorders
Postpartum depression
Anxiety disorders
Epilepsy
Stress-related psychiatric conditions
Safety Considerations
- Potential for sedation and cognitive impairment
- Tolerance and dependence with long-term use
- Interaction with other CNS depressants
- Impact on hormonal balance
Interacting Drugs
Benzodiazepines
GABA_A receptor agonists
GABA_A receptor modulators
Associated Biomarkers
| Biomarker |
|---|
| Plasma allopregnanolone levels (for diagnosis and treatment monitoring) |
| Cerebrospinal fluid allopregnanolone levels |