Etazolate hydrochloride

[Description]:

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 (GABAA) 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].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

PDE4:2 μM (IC50)

[In Vitro]

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]。

[In Vivo]

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>。 Animal Model: Male Swiss mice with 28-30 g[3] Dosage: 1, 3, 10 mg/kg Administration: IP Result: Reduced cerebral œdema when delivered 5 min and 2 h post-TBI. Improved recognition memory and reduces locomotor hyperactivity in a persistent manner following TBI.

[References]

[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.

[ Density]:
1.25g/cm3

[ Boiling Point ]:
427.6ºC at 760mmHg

[ Molecular Formula ]:
C₁₄H₂₀ClN₅O₂

[ Molecular Weight ]:
325.79400

[ Flash Point ]:
212.4ºC

[ Exact Mass ]:
325.13100

[ PSA ]:
81.40000

[ LogP ]:
3.31060

Click to get detail MSDS

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
R36/37/38

[ RIDADR ]:
NONH for all modes of transport

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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