Etazolate
Encyclopedia
Etazolate is an anxiolytic
drug
which is a pyrazolopyridine
derivative and has unique pharmacological
properties. It acts as a positive allosteric modulator
of the GABAA receptor at the barbiturate
binding site
, as an adenosine antagonist
of the A1 and A2 subtype
s, and as a phosphodiesterase inhibitor
selective for the PDE4 isoform. It is currently in clinical trial
s for the treatment of Alzheimer's disease
.
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
drug
Drug
A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...
which is a pyrazolopyridine
Pyrazolopyridine
The pyrazolopyridines are a chemical class of anxiolytic drugs which act as positive allosteric modulators of the GABAA receptor at the barbiturate binding site. They include the following compounds:* Cartazolate * Etazolate * ICI-190,622...
derivative and has unique pharmacological
Pharmacology
Pharmacology is the branch of medicine and biology concerned with the study of drug action. More specifically, it is the study of the interactions that occur between a living organism and chemicals that affect normal or abnormal biochemical function...
properties. It acts as a positive allosteric modulator
Positive allosteric modulator
A positive allosteric modulator is a drug which increases the activity of a receptor indirectly via activation of an allosteric site on the protein. PAMs are similar to agonists in that they contribute to overall receptor activation, but they are different because they do so in a functionally...
of the GABAA receptor at the barbiturate
Barbiturate
Barbiturates are drugs that act as central nervous system depressants, and can therefore produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, as hypnotics, and as anticonvulsants...
binding site
Binding site
In biochemistry, a binding site is a region on a protein, DNA, or RNA to which specific other molecules and ions—in this context collectively called ligands—form a chemical bond...
, as an adenosine antagonist
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
of the A1 and A2 subtype
Adenosine A2 receptor
Two subtypes of adenosine A2 receptors are known. Both are G protein-coupled adenosine receptors:* Adenosine A2A receptor* Adenosine A2B receptor...
s, and as a phosphodiesterase inhibitor
Phosphodiesterase inhibitor
A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase , therefore preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate and cyclic guanosine monophosphate by the respective PDE...
selective for the PDE4 isoform. It is currently in clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
s for the treatment of Alzheimer's disease
Alzheimer's disease
Alzheimer's disease also known in medical literature as Alzheimer disease is the most common form of dementia. There is no cure for the disease, which worsens as it progresses, and eventually leads to death...
.