Buy Allopregnanolone (hormone) Cas 516-54-1

Allopregnanolone is a naturally occurring neurosteroid which is made in the body from the hormone progesterone.^[9][10] As a medication, allopregnanolone was referred to as brexanolone, sold under the brand name Zulresso,^[6][11] and was used to treat postpartum depression.^[10][12][13] It was given by injection into a vein.^[10][6]

Side effects of brexanolone may include sedation, sleepiness, dry mouth, hot flashes, and loss of consciousness.^[6][10] It was a neurosteroid and acts as a positive allosteric modulator of the GABA_A receptor, the major biological target of the inhibitory neurotransmitter γ-aminobutyric acid (GABA).^[6]

Brexanolone was approved for medical use in the United States in 2019 and withdrawn from approval in 2025.^[10][14] The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.^[15] The long administration time, as well as the cost for a one-time treatment, have raised concerns about accessibility for many women.^[16]

Brexanolone was used to treat postpartum depression in adult women, administered as a continuous intravenous infusion over a period of 60 hours, and essential tremor.^[10][17]

Women experiencing moderate to severe postpartum depression when treated with a single dose of intravenous brexanolone display a significant reduction in HAM-D scores which persisted 30 days post-treatment.^[18]

Side effects of brexanolone include dizziness (10–20%), sedation (13–21%), headache (18%), nausea (10%), dry mouth (3–11%), loss of consciousness (3–5%), and flushing (2–5%).^{[6][10][8][19]} It can produce euphoria to a degree similar to that of alprazolam (3–13% at infusion doses of 90–270 μg over a one-hour period).^[6] Serious or severe adverse effects are rare but may include altered state of consciousness, syncope, presyncope, fatigue, and insomnia.^[19]

In the US, the Food and Drug Administration requires a Risk Evaluation and Mitigation Strategy (REMS) to counteract the risks of excessive sedation and loss of consciousness. It requires that all patients be monitored for those symptoms every 2 hours in planned non sleep periods and that oxygen saturation be monitored with continuous pulse oximetry.^[20]

Allopregnanolone possesses a wide variety of effects, including, in no particular order, antidepressant, anxiolytic, stress-reducing, rewarding,^[21] prosocial,^[22] antiaggressive,^[23] prosexual,^[22] sedative, pro-sleep,^[24] cognitive, memory-impairment, analgesic,^[25] anesthetic, anticonvulsant, neuroprotective, and neurogenic effects.^[9] Fluctuations in the levels of allopregnanolone and the other neurosteroids seem to play an important role in the pathophysiology of mood, anxiety, premenstrual syndrome, catamenial epilepsy, and various other neuropsychiatric conditions.^[26][27][28]