Disease relevance of etazolate

• Adenylate cyclase inhibitors and etazolate (a type 4 phosphodiesterase inhibitor) alone produced changes in the haemograms similar to those caused by Bacillus subtilis [1].

High impact information on etazolate

• Etazolate (SQ20009): electrophysiology and effects on [3H]flunitrazepam binding in cultured cortical neurons [2].
• Ferrous, but not ferric, Ec DOS had phosphodiesterase (PDE) activity of nearly 0.15 min(-1) with cAMP, which was optimal at pH 8.5 in the presence of Mg(2+) and was strongly inhibited by CO, NO, and etazolate, a selective cAMP PDE inhibitor [3].
• Furthermore, etazolate inhibited the [3H]DHP binding in a Lubrol-solubilized fraction with an IC50 value of 6-8 microM [4].
• These results provide evidence that etazolate, like pentobarbital, modulates benzodiazepine binding via the DHP-sensitive site of the benzodiazepine-GABA receptor-ionophore complex [4].
• Amrinone, milrinone and pentoxifylline inhibited lipopolysaccharide-induced TNF-alpha secretion, with IC50 values of 14.8, 81.6 and 748 microM, respectively, whereas Ro-2D, 1724 and etazolate had no effect on lipopolysaccharide-induced TNF-alpha secretion [5].

Biological context of etazolate

• Pyrazolopyridines, such as etazolate (SQ 20009), enhance [3H]diazepam binding to a Lubrol-solubilized fraction that has specific binding sites for 3H benzodiazepines, [alpha-3H]dihydropicrotoxinin (DHP) and [3H]muscimol [4].
• Hydrolysis and subsequent cyclization of etazolate hydrochloride and related compounds in aqueous solutions: application of PMR and mass spectrometry in accelerated stability studies [6].

Anatomical context of etazolate

• Facilitatory effects of SQ 20009 [1-ethyl-4-(isopropylidenehydrazine)-1H-pyrazolo-(3,4-b)-pyridine-5-carboxylic acid, ethyl ester, HCl] were investigated at the frog sartorious neuromuscular junction [7].

Associations of etazolate with other chemical compounds

• Orders of potency determined at IC50 levels (concentrations required for 50% inhibition) were SQ 20009 greater than RO 20-1724 greater than papaverine greater than bufexamac greater than indomethacin greater than theophylline greater than p-biphenylylacetic acid greater than or less than glycyrrhetinic acid for inhibition of both PDE and mitosis [8].
• Characteristics common to choleretic increments of bile induced by theophylline, glucagon and SQ-20009 in the dog [9].
• Theophylline, glucagon, and SQ-20009 induce a choleresis in the dog characterized by a proportionate increase in erythritol clearance and bile flow, no increase in bile salt excretion, and by an isosmotic solution of similar electrolyte composition [9].
• Thus, etazolate and cartazolate directly stimulate [3H]flunitrazepam binding (with EC50 values of 1.2 microM and 0.3 microM respectively) by increasing the apparent affinity of [3H]flunitrazepam for its binding sites [10].

Gene context of etazolate

• Motor nerve terminal facilitatory action of SQ 20009: an inhibitor of cyclic nucleotide phosphodiesterase [7].

References