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Iomazenil

Chemical compound

Chemical compound

(123I) | elimination_half-life =

Iomazenil (also known as Ro16-0154, INN, USAN; benzodine) is an antagonist and partial inverse agonist of benzodiazepine and a potential treatment for alcohol use disorder. The compound was introduced in 1989 by pharmaceutical company Hoffmann-La Roche as an Iodine-123-labelled SPECT 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.

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.

References

References

  1. (1989). "Imaging benzodiazepine receptors in the human brain by single photon emission computed tomography (SPECT)". International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology.
  2. (January 2003). "Radiopharmaceuticals for single-photon emission computed tomography brain imaging". Seminars in Nuclear Medicine.
  3. (February 2003). "Is central benzodiazepine receptor imaging useful for the identification of epileptogenic foci in localization-related epilepsies?". European Journal of Nuclear Medicine and Molecular Imaging.
  4. (February 2011). "Probing GABA receptor function in schizophrenia with iomazenil". Nature Publishing Group.
  5. (13 May 2012). "Tests begin on new drink-busting drug". Independent on Sunday.
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alcohol-and-health carboxylate-esters ethyl-esters convulsants gabaa-receptor-negative-allosteric-modulators imidazobenzodiazepines iodobenzene-derivatives
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