Template:UNII (123I) Template:UNII (123I)
|Chemical and physical data|
|Molar mass||407.290 g/mol|
|3D model (Jmol)||Interactive image|
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).
Use in brain research
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.
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.
- 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.
- [123I]Iomazenil, Molecular Imaging and Contrast Agent Database, NCBI
- Effects of Delta-9-THC and Iomazenil in Healthy Humans, Clinicaltrials.gov
- Ability of Partial Inverse Agonist, Iomazenil, to Block Ethanol Effects in Humans