PDE-4 inhibitor and selective GABA-A receptor modulator
CAS：35838-58-5
分子式：C14H19N5O2.HCl
分子量：325.8
纯度：98%
存储：Store at -20°C

Background:

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].

参考文献:
[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.