Etazolate (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]}. In Vitro:Etazolate hydrochloride (SQ 20009; 25 µM) significantly increases the expression of arginase and ODC at the protein level (∼3.1- and ∼1.6-fold for arginase and ODC, respectively) in LtT7.TR cells^[2].
In Vivo:Etazolate hydrochloride (SQ 20009; 1, 3, 10 mg/kg; IP) improves recognition memory and reduces locomotor hyperactivity in a persistent manner following traumatic brain injury (TBI) in mice^[3].
Etazolate hydrochloride (0.5, 1 mg/kg; p.o.; once a day during 21 days) significantly inhibits the chronic unpredictable mild stress (CUMS)-induced behavioral (decreases sucrose consumption and increases duration of immobility) and biochemical (increases lipid peroxidation and nitrite level; decreases glutathione, superoxide dismutase and catalase activity) changes in Swiss Albino mice (22-25 g)^[4].
Etazolate hydrochloride (0.5, 1 mg/kg; i.p.; single dose) antagonizes the Reserpine (HY-N0480; 1 mg/kg; i.p.)-induced hypothermia in male Wistar rats (250-275 g)^[5].