Iomazenil (also known as Ro16-0154,
INN,
USAN; benzodine) is an
antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
and 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 ...
of
benzodiazepine
Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, ...
and a potential treatment for
alcohol use disorder
Alcoholism is, broadly, any drinking of alcohol that results in significant mental or physical health problems. Because there is disagreement on the definition of the word ''alcoholism'', it is not a recognized diagnostic entity. Predomin ...
. The compound was introduced in 1989 by pharmaceutical company
Hoffmann-La Roche
F. Hoffmann-La Roche AG, commonly known as Roche, is a Swiss multinational healthcare company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX ...
as an
Iodine-123-labelled
SPECT
Single-photon emission computed tomography (SPECT, or less commonly, SPET) is a nuclear medicine tomographic imaging technique using gamma rays. It is very similar to conventional nuclear medicine planar imaging using a gamma camera (that is, ...
tracer for imaging benzodiazepine receptors (
GABAA receptors) in the brain. Iomazenil is an analogue of
flumazenil (Ro15-1788).
Use in brain research
123I-labelled iomazenil can be used to image
epileptic seizure foci as an alternative to
18F-fludeoxyglucose PET imaging
Positron emission tomography (PET) is a functional imaging technique that uses radioactive substances known as radiotracers to visualize and measure changes in metabolic processes, and in other physiological activities including blood flow, ...
.
The effect of iomazenil of reducing levels of
GABA in the brain was used by researchers to exacerbate symptoms in patients with
schizophrenia in a laboratory study, supporting the theory that a GABA deficiency underlies that disease.
Alcohol treatment
Researchers at
Yale University and
Veterans Affairs Connecticut Healthcare System have been testing iomazenil as a potential treatment for
drunkenness due to its ability to bind alcohol receptors in the brain.
See also
*
GABAA receptor negative allosteric modulator
*
GABAA receptor § Ligands
References
External links
*
*
*
{{Benzodiazepines
Alcohol and health
Carboxylate esters
Ethyl esters
Convulsants
GABAA receptor negative allosteric modulators
Imidazobenzodiazepines
Iodoarenes