Ro4938581 is a
nootropic
Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic dietary supplement, supplements or drugs and other substances that are claimed to improve cognitive function ...
drug invented in 2009 by a team working for
Hoffmann-La Roche, which acts as a subtype-selective
inverse agonist at the
α5 subtype of the
benzodiazepine binding site on the
GABAA receptor
Receptor may refer to:
* Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...
. It has good selectivity for the α
5 subtype and did not produce
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 e ...
or
anxiogenic effects in animal studies, making it a promising potential nootropic. Ro4938581 and a related derivative
basmisanil
Basmisanil (; developmental codes RG-1662 and RO5186582) is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairmen ...
(RG-1662, RO5186582) have subsequently been investigated for the alleviation of
cognitive dysfunction
Cognitive disorders (CDs), also known as neurocognitive disorders (NCDs), are a category of mental health disorders that primarily affect cognitive abilities including learning, memory, perception, and problem solving. Neurocognitive disorders i ...
in
Down syndrome
Down syndrome or Down's syndrome, also known as trisomy 21, is a genetic disorder caused by the presence of all or part of a third copy of chromosome 21. It is usually associated with physical growth delays, mild to moderate intellectual dis ...
.
See also
*
GABAA receptor negative allosteric modulator
*
GABAA receptor § Ligands
References
Imidazobenzodiazepines
Triazolobenzodiazepines
GABAA receptor negative allosteric modulators
Nootropics
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