|1-(2-((3R,5R,8R,9R,10S,13S,14S,17S)-3-羟基-3,13-二甲基十六氢-1H-环戊二烯并[a]菲-17-基)-2-氧代乙基)-1H-吡唑-4-甲腈|CsnPharm

CAS No.: 1632051-40-1

Zuranolone Catalog No. CSN23715

Synonyms: SAGE-217;S-812217;SGE 797

SAGE-217 is an agonist of GABAA receptor with EC50s of 296 nM and 163 nM for α1β2γ2 and α4β3δ respectively.

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实验方案

技术信息

生物活性

描述The family of GABA_A receptors, broadly expressed in the brain, are pentameric ion channels primarily composed of two alpha subunits (α1-α6), two beta subunits (β1-β3) and one additional subunit (γ1-γ3, δ, ε, π, or θ). GABA, acting via the GABA_A receptor, can influence a wide range of brain circuits that are central to a variety of behavioral states, such as anxiety levels, seizures, sleep, vigilance, and memory. SAGE-217, belonging to neuroactive steroids (NASs), is a positive allosteric modulators (PAM) of synaptic and extrasynaptic GABA_A receptors, with EC₅₀s of 296 and 163 nM for α1β2γ2 and α4β3δ GABA_A receptors, respectively. In vitro CYP inhibition (IC₅₀) was >30 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4, and CYP2B6. Further, SAGE-217 showed >30 μM inhibition in a cardiac panel of eight relevant cardiac ion channels. At 10 μM concentrations of SAGE-217, only binding at the glycine (57%), sigma receptors (88%), and inhibition of the transient receptor potential vanilloid 1 (TRPV1, 95%) was noted. Acute administration of 3 (0.3–10 mg/kg, ip) effectively reduced pentylenetretazol (PTZ)-induced seizures in mice (MEC_plasma = 85 nM; SAGE-217 (0.3–3 mg/kg, ip)) as well as producing a dose-dependent anticonvulsant effect in the mouse 6 Hz electrical stimulation model. In the rat lithium-pilocarpine model of status epilepticus (SE), SAGE-217 (0.3–5 mg, iv) abolished both behavioral and electrographic seizure activity, even when administered 60 min after induction of SE. Furthermore, SAGE-217 is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD), major depressive disorder (MDD), and essential tremor (ET)^[1].
参考文献

[1] Martinez Botella G, Salituro FG, Harrison BL, et al. Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor. J Med Chem. 2017;60(18):7810‐7819

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4416 mL
- 12.2081 mL
- 24.4162 mL
- 5 mM
- 0.4883 mL
- 2.4416 mL
- 4.8832 mL
- 10 mM
- 0.2442 mL
- 1.2208 mL
- 2.4416 mL

技术信息

CAS号

1632051-40-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H35N3O2

运输

蓝冰

分子量

409.56

别名

SAGE-217;S-812217;SGE 797;DXN-51401

溶解度

DMSO	98.0 mg/mL (239.3 mM)

动物实验配方

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