Iomazenil

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Iomazenil
123I-Iomazenil.svg
Systematic (IUPAC) name
ethyl 7-(123I)iodo-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
Clinical data
Legal status ?
Identifiers
CAS number 127985-21-1
127396-36-5 (123I)
ATC code None
PubChem CID 65959
ChemSpider 59362
Synonyms Ro 16-0154
Chemical data
Formula C15H14123IN3O3
Mol. mass 407.290 g/mol

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]

  1. ^ 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. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ Dobson, Roger; Jonathan Owen (13 May 2012). "Tests begin on new drink-busting drug". Independent on Sunday. Retrieved 20 May 2012. 

External links[edit]