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 ...

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).

References

Nootropics Fluoroarenes Triazoles Thiocarbonyl compounds GABAA receptor negative allosteric modulators {{nervous-system-drug-stub

Synthesis

See also

References