Iomazenil

Iomazenil

Systematic (IUPAC) name
ethyl 7-iodanyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
Identifiers
CAS Number	127985-21-1 Template:CAS (123I)
PubChem	CID: 65959
ChemSpider	59362
UNII	B851121553
ChEMBL	CHEMBL2105020
Synonyms	Ro 16-0154
Chemical data
Formula	C15H14123IN3O3
Molecular mass	407.290 g/mol
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

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 (GABA_A receptors) in the brain. Iomazenil is an analogue of flumazenil (Ro15-1788).

Use in brain research

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

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.

Alcohol treatment

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.

External links

• [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