| Identification | Back Directory | [Name]
ETAZOLATE | [CAS]
35838-58-5 | [Synonyms]
Nsc163611
Etazolate hydrochloride solid
Ethyl 1-ethyl-4-(isopropylidenehydrazino)-1H-pyrazolo[3,4-B]pyridine-5-carboxylate monohydrochloride
1-ethyl-4-[(1-methylethylidene)hydrazino]1h-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl ester hydrochloride
1H-Pyrazolo[3,4-B]pyridine-5-carboxylic acid, 1-ethyl-4-[(1-methylethylidene)hydrazino]-, ethyl ester, monohydrochloride
SQ20009, 1-Ethyl-4-[(1-methylethylidene)hydrazino]1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl ester hydrochloride | [Molecular Formula]
C14H18N5O2HCl | [MDL Number]
MFCD00209848 | [MOL File]
35838-58-5.mol |
| Chemical Properties | Back Directory | [Melting point ]
193-194 °C | [storage temp. ]
room temp | [solubility ]
H2O: >20mg/mL (Solutions should be freshly prepared.) | [form ]
solid | [color ]
white | [Water Solubility ]
H2O: >20mg/mL (Solutions should be freshly prepared.) |
| Hazard Information | Back Directory | [Uses]
Antipsychotic. | [Uses]
Etazolate Hydrochloride is an acyclic nucleotide phosphodiesterase 4 inhibitor, which also exhibits antidepressant-like activity in acute and chronic mouse and rat model of depression. | [Biological Activity]
etazolate hydrochloride is a pde-4 inhibitor and selective gaba-a receptor modulator [3].pde-4 modulates the release of inflammatory mediators through camp-dependent and -independent mechanisms. selective targeting pde-4 is a novel therapeutic approach in the treatment of inflammation-associated respiratory diseases, such as asthma and copd (chronic obstructive pulmonary disease) [1].in rat neuronal cortical cells, etazolate hydrochloride (0.2 μm) induced sappα through the stimulation of the α-secretase pathway, and exerted a neuroprotective effect against aβ which was associated with sappα induction via the gaba-a receptor [2].in 159 alzheimer’s disease patients, etazolate hydrochloride in combination with one achei (acetycholinesterase inhibitor) was shown to be safe and generally well tolerated in the phase iia study over a 3-month treatment period [3]. | [Biochem/physiol Actions]
Selective inhibitor of cAMP-specific phosphodiesterase. | [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].
| Animal Model: | Male Swiss mice with 28-30 g[3] | | Dosage: | 1, 3, 10 mg/kg | | Administration: | IP | | Result: | Reduced cerebral ?dema when delivered 5 min and 2 h post-TBI.
Improved recognition memory and reduces locomotor hyperactivity in a persistent manner following TBI.
|
| [IC 50]
PDE4: 2 μM (IC50) | [References]
[1] dastidar s g, rajagopal d, ray a. therapeutic benefit of pde4 inhibitors in inflammatory diseases.[j]. current opinion in investigational drugs, 2007, 8(5):364-72.
[2] marcade m, bourdin j, loiseau n, et al. etazolate, a neuroprotective drug linking gaba(a) receptor pharmacology to amyloid precursor protein processing.[j]. journal of neurochemistry, 2008, 106(1):392-404.
[3] vellas b; sol o; snyder pj; ousset pj; haddad r; maurin m; lemarié jc; désiré l; pando mp; eht0202/002 study group. eht0202 in alzheimer's disease: a 3-month, randomized, placebo-controlled, double-blind study.[j]. current alzheimer research, 2011, 8(2):203-12. |
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