Zuranolone 是一个口服有效的 GABA_A 受体的神经活性类固醇正向变构调节剂, 对 α₁β₂γ₂ 和 α₄β₃δ GABA_A 受体的 EC₅₀ 值分别为 296 和 163 nM。

Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABA A receptor, with EC 50 s of 296 and 163 nM for α 1 β 2 γ 2 and α 4 β 3 δ GABA A receptors, respectively.

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EC50: 296 nM (α1β2γ2 GABAA receptor), 163 nM (α4β3δ GABAA receptor)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Acute administration of Zuranolone (0.3 to 10 mg/kg, ip) effectively reduces pentylenetretazol (PTZ)-induced seizures in mice (MEC plasma =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%). has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[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 Che

In Vitro: DMSO : 100 mg/mL (244.16 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (insoluble)配制储备液