Iomazenil (also known as Ro16-0154, INN, USAN; benzodine) is an antagonist and partial inverse agonist of benzodiazepine and a potential treatment for alcohol abuse. 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).[1]
Use in brain research [edit]
I-123-labelled iomazenil can be used to image epileptic seizure foci as an alternative to Fludeoxyglucose (18F) PET imaging.[2][3]
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.[4]
Alcohol treatment [edit]
Researcher Deepak D'Souza and colleagues at Yale University and Veterans Affairs Connecticut Healthcare System are testing iomazenil as a potential treatment for drunkenness due to its ability to bind alcohol receptors in the brain.[5]
References [edit]
- ^ Höll, K; Deisenhammer E, Dauth J, Carmann H, Schubiger PA (1989). "Imaging benzodiazepine receptors in the human brain by single photon emission computed tomography (SPECT)". Int J Rad Appl Instrum B 16 (8): 759–63.
- ^ Kung, Hank F.; Mei-Ping Kung , Seok Rye Choi (January 2003). "Radiopharmaceuticals for single-photon emission computed tomography brain imaging". Seminars in Nuclear Medicine 33 (1): 2–13. doi:10.1053/snuc.2003.127296. PMID 12605353.
- ^ Goethals, I; Van de Wiele C, Boon P, Dierckx R (February 2003). "Is central benzodiazepine receptor imaging useful for the identification of epileptogenic foci in localization-related epilepsies?". Eur J Nucl Med Mol Imaging 30 (2): 325–8.
- ^ Ahn, Kyungheup; Gil R, Seibyl J, Sewell RA, D'Souza DC (February 2011). "Probing GABA receptor function in schizophrenia with iomazenil". Neuropsychopharmacology (Nature Publishing Group) 36 (3): 677–83. doi:10.1038/npp.2010.198. PMC 3055690. PMID 21068719.
- ^ Dobson, Roger; Jonathan Owen (13 May 2012). "Tests begin on new drink-busting drug". Independent on Sunday. Retrieved 20 May 2012.
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