Iomazenil

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).[1]

Iomazenil
Clinical data
Other namesRo 16-0154
Identifiers
IUPAC name
  • ethyl 7-iodanyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H14123IN3O3
Molar mass407.290 g/mol
3D model (JSmol)
SMILES
  • CCOC(=O)c1c2n(cn1)-c3cccc(c3C(=O)N(C2)C)I
InChI
  • InChI=1S/C15H14IN3O3/c1-3-22-15(21)13-11-7-18(2)14(20)12-9(16)5-4-6-10(12)19(11)8-17-13/h4-6,8H,3,7H2,1-2H3/i16-4
  • Key:FRIZVHMAECRUBR-KIWWSDKQSA-N

Use in brain research

123I-labelled iomazenil can be used to image epileptic seizure foci as an alternative to 18F-fludeoxyglucose 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

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.[5]

See also

References
  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)". International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology. 16 (8): 759–63. doi:10.1016/0883-2897(89)90158-x. PMID 2559905.
  2. Kung HF, Kung MP, Choi SR (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?". European Journal of Nuclear Medicine and Molecular Imaging. 30 (2): 325–8. doi:10.1007/s00259-002-1083-z. PMID 12552355. S2CID 27969321.
  4. Ahn K, 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 R, Owen J (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. US National Center for Biotechnology Information (NCBI). 2004.
  • Clinical trial number NCT00982982 for "Effects of Delta-9-THC and Iomazenil in Healthy Humans" at ClinicalTrials.gov
  • Clinical trial number NCT01590277 for "Ability of Partial Inverse Agonist, Iomazenil, to Block Ethanol Effects in Humans" at ClinicalTrials.gov
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