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CAS No. : 1632051-40-1
MCE 国际站:Zuranolone
产品活性:Zuranolone 是一个口服有效的 GABAA 受体的神经活性类固醇正向变构调节剂, 对 α1β2γ2 和 α4β3δ GABAA 受体的 EC50 值分别为 296 和 163 nM。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:GABA Receptor
In Vitro: 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.
In Vivo: 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%).
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