delta subunit

Every compound in the sci-wiki that affects delta subunit; the ones you can source are floated to the front, then the reference-only entries. Tap any for the full entry, mechanism, and outlets.

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←delta subunit2/2

Anticonvulsant

Ganaxolone

Ganaxolone (research code CCD-1042; brand name Ztalmy) is a synthetic neuroactive steroid, specifically the 3-beta-methyl analog of the endogenous neurosteroid allopregnanolone (a metabolite of progesterone). It is a positive allosteric modulator (a molecule that amplifies a receptor's response to its natural activator) of the GABA-A receptor, the brain's principal inhibitory chloride channel, and it enhances both synaptic (phasic) and extrasynaptic (tonic) inhibition, with particularly strong activity at delta-subunit-containing receptors. In March 2022 it became the first medicine approved by the United States Food and Drug Administration for seizures associated with CDKL5 deficiency disorder (a rare genetic developmental and epileptic encephalopathy caused by mutations in the cyclin-dependent kinase-like 5 gene), and the first synthetic neurosteroid approved as an anticonvulsant. The defining 3-beta-methyl group makes ganaxolone orally bioavailable, metabolically stable, and non-hormonal, distinguishing it from its parent neurosteroid, which requires intravenous administration.

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Antidepressant

Zuranolone

Zuranolone (development code SAGE-217; marketed as Zurzuvae) is an orally bioavailable synthetic analog of allopregnanolone (a naturally occurring neurosteroid derived from progesterone) that acts as a positive allosteric modulator (a compound that amplifies a receptor's response to its own transmitter) of the GABA-A receptor (the brain's principal inhibitory chloride channel). It was engineered by Sage Therapeutics from the same neurosteroid scaffold as the intravenous agent brexanolone, but with a modified 3-hydroxy pyrazole substitution that confers metabolic stability suitable for once-daily oral tablets rather than a continuous infusion. In August 2023 the United States Food and Drug Administration approved zuranolone for postpartum depression (a major depressive episode arising in the weeks after childbirth), making it the first oral drug indicated specifically for that condition. It is notable for producing an antidepressant response within days when given as a short, fixed two-week course, in contrast with the weeks-long onset of conventional monoamine antidepressants.

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