Cartazolate
Encyclopedia
Cartazolate is a drug
of the pyrazolopyridine
class. It acts as a GABAA receptor positive allosteric modulator
at the barbiturate
binding site
of the complex and has anxiolytic
effects in animals. It is also known to act as an adenosine antagonist
at the A1 and A2 subtype
s and as a phosphodiesterase inhibitor
. Cartazolate was tested in human clinical trial
s and was found to be efficacious for anxiety
but was never marketed.
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...
of the 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...
class. It acts as a GABAA receptor 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...
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...
of the complex and has anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
effects in animals. It is also known to act 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...
at 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...
. Cartazolate was tested in human 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 and was found to be efficacious for anxiety
Anxiety
Anxiety is a psychological and physiological state characterized by somatic, emotional, cognitive, and behavioral components. The root meaning of the word anxiety is 'to vex or trouble'; in either presence or absence of psychological stress, anxiety can create feelings of fear, worry, uneasiness,...
but was never marketed.