Etazolate hydrochloride

Etazolate hydrochloride用途

盐酸依他唑酯(SQ 20009)是一种口服活性的4型磷酸二酯酶(PDE4)选择性抑制剂,IC50为2μM。盐酸依他唑酯是一种γ-氨基丁酸a(GABAA)受体调节剂。盐酸依他唑酯是一种α-分泌酶激活剂,可诱导可溶性淀粉样前体蛋白(sAPPα)的产生。盐酸依他唑酯是一种吡唑啉类衍生物,可提高cAMP水平。盐酸依他唑酯具有抗焦虑、抗抑郁和抗炎作用[1][2][3][4][5]。

Etazolate hydrochloride名称

[ CAS 号 ]:
35838-58-5

[ 英文名 ]:
Etazolate hydrochloride

[英文别名 ]:

Etazolate hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

研究领域 >> 炎症/免疫

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[ 靶点 ]

PDE4:2 μM (IC50)

[体外研究]

盐酸依他唑酯(SQ 20009；25µM)在 LtT7.TR型细胞中显着增加精氨酸酶和开放式数据中心蛋白质水平的表达(精氨酸酶和开放式数据中心分别为～3.1倍和～1.6倍) [2]。

[体内研究]

盐酸依他唑酯(SQ 20009；1、3、10 mg/kg；腹腔给药) 在小鼠创伤性脑损伤 (待定)后持续改善识别记忆并减少运动过度活跃[3]。盐酸依他唑酯(0.5,1mg/kg；灌胃给药; 每天一次; 21天) 在瑞士白化小鼠 (22-25克)中显着抑制慢性不可预知的轻度应激 (立方米)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]。盐酸依他唑酯(0.5,1mg/kg；腹腔注射; 单次) 在雄性 Wistar公司大鼠 (250-275克)中拮抗利血平(HY-N0480；1 mg/kg；腹腔注射) 诱导的体温过低[5] 动物模型：28-30 g的雄性瑞士小鼠[3]剂量：1、3、10 mg/kg给药：IP结果：TBI后5分钟和2小时给药时大脑水肿减轻。改善认知记忆,减少TBI后持续性的运动过度。

[参考文献]

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

[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.

[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.

[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.

[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.

Etazolate hydrochloride物理化学性质

[ 密度 ]:
1.25g/cm3

[ 沸点 ]:
427.6ºC at 760mmHg

[ 分子式 ]:
C₁₄H₂₀ClN₅O₂

[ 分子量 ]:
325.79400

[ 闪点 ]:
212.4ºC

[ 精确质量 ]:
325.13100

[ PSA ]:
81.40000

[ LogP ]:
3.31060

[ 储存条件 ]:
室温

Etazolate hydrochlorideMSDS

详细MSDS(安全技术说明书)

Etazolate hydrochloride安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 危险品运输编码 ]:
NONH for all modes of transport

Etazolate hydrochloride文献

Etazolate improves performance in a foraging and homing task in aged rats.

Eur. J. Pharmacol. 634(1-3) , 95-100, (2010)

Etazolate is a phosphodiesterase 4 (PDE4) inhibitor and GABAA receptor modulator that also stimulates alpha-secretase activity and neurotrophic soluble amyloid precursor protein (sAPPalpha) production...

Physostigmine inhibition of 3',5'-cyclic AMP phosphodiesterase from cat sciatic nerve.

J. Pharmacol. Exp. Ther. 228(3) , 656-61, (1984)

This study was designed to determine whether cholinergic drug interaction with cyclic (c) AMP phosphodiesterase (PDE) might account for part of the effects of this class of drugs at the neuromuscular ...

[Pharmacologic value of cyclic nucleotide phosphodiesterase inhibitors].

Ann. Pharm. Fr. 42(2) , 99-112, (1984)

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