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Iomazenil

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Iomazenil
Clinical data
Other namesRo 16-0154
Identifiers
  • ethyl 7-iodanyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC15H14123IN3O3
Molar mass407.290 g/mol
3D model (JSmol)
  • CCOC(=O)c1c2n(cn1)-c3cccc(c3C(=O)N(C2)C)I
  • 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

Iomazenil (also known asRo16-0154,INN,USAN;benzodine) is anantagonist and partialinverse agonist ofbenzodiazepine and a potential treatment foralcohol use disorder. The compound was introduced in 1989 by pharmaceutical companyHoffmann-La Roche as anIodine-123-labelledSPECT tracer for imaging benzodiazepine receptors (GABAA receptors) in the brain. Iomazenil is an analogue offlumazenil (Ro15-1788).[1]

Use in brain research

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123I-labelled iomazenil can be used to imageepileptic seizure foci as an alternative to18F-fludeoxyglucosePET imaging.[2][3]

The effect of iomazenil of reducing levels ofGABA in the brain was used by researchers to exacerbate symptoms in patients withschizophrenia in a laboratory study, supporting the theory that a GABA deficiency underlies that disease.[4]

Alcohol treatment

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Researchers atYale University andVeterans Affairs Connecticut Healthcare System have been testing iomazenil as a potential treatment fordrunkenness due to its ability to bind alcohol receptors in the brain.[5]

See also

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References

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  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.36 (3). Nature Publishing Group: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. Retrieved20 May 2012.

External links

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