Suritozole (MDL 26,479) is an investigational
cognition enhancer. It acts as a partial
inverse agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
A neutral antagonist has no activity in the absence of an agonist or inverse agon ...
at the
benzodiazepine receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on ...
site on the GABA
A ion channel complex, but does not have either
anxiogenic
An anxiogenic or panicogenic substance is one that causes anxiety. This effect is in contrast to anxiolytic agents, which inhibits anxiety. Together these categories of psychoactive compounds may be referred to as anxiotropic compounds.
Anxiogen ...
or
convulsant A convulsant is a drug which induces convulsions and/or epileptic seizures, the opposite of an anticonvulsant. These drugs generally act as stimulants at low doses, but are not used for this purpose due to the risk of convulsions and consequent exc ...
effects, unlike other BZD inverse agonists such as
DMCM.
It was investigated for the treatment of
depression and
Alzheimer's disease
Alzheimer's disease (AD) is a neurodegeneration, neurodegenerative disease that usually starts slowly and progressively worsens. It is the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in short-term me ...
,
but clinical development seems to have been discontinued.
Synthesis
The reaction between monomethylhydrazine
0-34-4(1) and methyl isothiocyanate (Trapex)
56-61-6(2) gave 2,4-dimethylthiosemicarbazide
621-75-6(3). Amide formation with 3-fluorobenzoyl chloride
711-07-5(4) yielded 1-(3-fluorobenzoyl)-2,4-dimethylthiosemicarbazide
10623-52-4(5). Cyclization to Suritozole (6).
See also
*
GABAA receptor negative allosteric modulator
*
GABAA receptor § Ligands
References
Nootropics
Fluoroarenes
Triazoles
Thiocarbonyl compounds
GABAA receptor negative allosteric modulators
{{nervous-system-drug-stub