For research use only, not for therapeutic use.
Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively[1].<br>Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively. Zuranolone is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD) and major depressive disorder (MDD). Zuranolone shows >30 μM inhibition in a cardiac panel of eight relevant cardiac ion channels. At 10 μM concentration of Zuranolone, only binding at the glycine (57%), sigma receptors (88%), and inhibition of the transient receptor potential vanilloid 1 (TRPV1, 95%) is noted[1].<br>Acute administration of Zuranolone (0.3 to 10 mg/kg, ip) effectively reduces pentylenetretazol (PTZ)-induced seizures in mice (MECplasma=85 nM) as well as produces a dose-dependent anticonvulsant effect in the mouse 6 Hz electrical stimulation model. In the rat model of status epilepticus (SE), Zuranolone (0.3 to 5 mg, iv) abolishes both behavioral and electrographic seizure activity, even when administered 60 min after induction of SE. Additional PK studies of Zuranolone in dog show low clearance (<10% of hepatic blood flow), resulting in excellent oral bioavailability (F=68%)[1].
| Catalog Number | I020350 |
| CAS Number | 1632051-40-1 |
| Molecular Formula | C₂₅H₃₅N₃O₂ |
| Purity | ≥95% |
| Reference | [1]. Martinez Botella G, et al. Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1′-yl)-19-nor-5β-pregnan-20-one: A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor. J Med Chem. 2017 Sep 28;60(18):7810-7819. |
