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].
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.
