Etazolate hydrochloride  (Synonyms: SQ 20009; EHT 0202 hydrochloride)

Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC₅₀ of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABA_A) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects^{[1][2][3][4][5]}.

Etazolate hydrochloride (SQ 20009; 25 µM) 在 LtT7.TR 细胞中显着增加精氨酸酶和 ODC 蛋白质水平的表达(精氨酸酶和 ODC 分别为～3.1 倍和～1.6 倍) ^[2]。

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

Etazolate hydrochloride (SQ 20009; 1, 3, 10 mg/kg; 腹腔给药) 在小鼠创伤性脑损伤 (TBI) 后持续改善识别记忆并减少运动过度活跃^[3]。
Etazolate hydrochloride (0.5, 1 mg/kg; 灌胃给药; 每天一次; 21 天) 在瑞士白化小鼠 (22-25 g)中显着抑制慢性不可预知的轻度应激 (CUMS) 诱导的行为 (减少蔗糖消耗并增加不动的持续时间) 和生化 (增加脂质过氧化和亚硝酸盐水平；降低谷胱甘肽、超氧化物歧化酶和过氧化氢酶活性) 的变化^[4]。
Etazolate hydrochloride (0.5, 1 mg/kg; 腹腔注射; 单次) 在雄性 Wistar 大鼠 (250-275 g) 中拮抗 Reserpine (HY-N0480; 1 mg/kg;腹腔注射) 诱导的体温过低^{[5]< /sup>。}

325.79

C₁₄H₂₀ClN₅O₂

35838-58-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Xuemei Wei, et al. Targeting phosphodiesterase 4 as a therapeutic strategy for cognitive improvement. Bioorg Chem. 2023 Jan;130:106278.  [Content Brief]

  [2]. Arijit Bhattacharya, et al.Role of a differentially expressed cAMP phosphodiesterase in regulating the induction of resistance against oxidative damage in Leishmania donovani. Free Radic Biol Med. 2009 Nov 15;47(10):1494-506.  [Content Brief]

  [3]. Eleni Siopi, et al. Etazolate, an α-secretase activator, reduces neuroinflammation and offers persistent neuroprotection following traumatic brain injury in mice. Neuropharmacology. 2013 Apr;67:183-92.  [Content Brief]

  [4]. Ankur Jindal, et al. Etazolate, a phosphodiesterase 4 inhibitor reverses chronic unpredictable mild stress-induced depression-like behavior and brain oxidative damage. Pharmacol Biochem Behav. 2013 Apr;105:63-70.  [Content Brief]

  [5]. Ankur Jindal, et al. Antidepressant-like effect of etazolate, a cyclic nucleotide phosphodiesterase 4 inhibitor--an approach using rodent behavioral antidepressant tests battery. Eur J Pharmacol. 2012 Aug 15;689(1-3):125-31.  [Content Brief]