Chemical compound
Pharmaceutical compound
Iomazenil Other names Ro 16-0154
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 ) Formula C15 H14 123 IN3 O3 Molar mass 407.290 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 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]
Use in brain research
123 I-labelled iomazenil can be used to image epileptic seizure foci as an alternative to 18 F-fludeoxyglucosePET 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
^ 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 . ^ 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 . ^ 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 . ^ 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 . ^ Dobson R, Owen J (13 May 2012). "Tests begin on new drink-busting drug" . Independent on Sunday . Retrieved 20 May 2012 .
External links
Ionotropic
GABAA Tooltip γ-Aminobutyric acid A receptor
Positive modulators (abridged; see here for a full list): α-EMTBL Alcohols (e.g., drinking alcohol , 2M2B )Anabolic steroids Avermectins (e.g., ivermectin )Barbiturates (e.g., phenobarbital )Benzodiazepines (e.g., diazepam )Bromide compounds (e.g., potassium bromide )Carbamates (e.g., meprobamate )Carbamazepine Chloralose Chlormezanone Clomethiazole Dihydroergolines (e.g., ergoloid (dihydroergotoxine) )Etazepine Etifoxine Fenamates (e.g., mefenamic acid )Flavonoids (e.g., apigenin , hispidulin )Fluoxetine Flupirtine Imidazoles (e.g., etomidate )Kava constituents (e.g., kavain )Lanthanum Loreclezole Monastrol Neuroactive steroids (e.g., allopregnanolone , cholesterol , THDOC )Niacin Niacinamide Nonbenzodiazepines (e.g., β-carbolines (e.g., abecarnil ), cyclopyrrolones (e.g., zopiclone ), imidazopyridines (e.g., zolpidem ), pyrazolopyrimidines (e.g., zaleplon ))Norfluoxetine Petrichloral Phenols (e.g., propofol )Phenytoin Piperidinediones (e.g., glutethimide )Propanidid Pyrazolopyridines (e.g., etazolate )Quinazolinones (e.g., methaqualone )Retigabine (ezogabine) ROD-188 Skullcap constituents (e.g., baicalin )Stiripentol Sulfonylalkanes (e.g., sulfonmethane (sulfonal) )Topiramate Valerian constituents (e.g., valerenic acid )Volatiles /gases (e.g., chloral hydrate , chloroform , diethyl ether , paraldehyde , sevoflurane )Negative modulators: 1,3M1B 3M2B 11-Ketoprogesterone 17-Phenylandrostenol α3IA α5IA (LS-193,268) β-CCB β-CCE β-CCM β-CCP β-EMGBL Anabolic steroids Amiloride Anisatin β-Lactams (e.g., penicillins , cephalosporins , carbapenems )Basmisanil Bemegride Bicyclic phosphates (TBPS , TBPO , IPTBO )BIDN Bilobalide Bupropion CHEB Chlorophenylsilatrane Cicutoxin Cloflubicyne Cyclothiazide DHEA DHEA-S Dieldrin (+)-DMBB DMCM DMPC EBOB Etbicyphat FG-7142 (ZK-31906) Fiproles (e.g., fipronil )Flavonoids (e.g., amentoflavone , oroxylin A )Flumazenil Fluoroquinolones (e.g., ciprofloxacin )Flurothyl Furosemide Golexanolone Iomazenil (123 I) IPTBO Isopregnanolone (sepranolone) L-655,708 Laudanosine Lindane MaxiPost Morphine Morphine-3-glucuronide MRK-016 Naloxone Naltrexone Nicardipine Nonsteroidal antiandrogens (e.g., apalutamide , bicalutamide , enzalutamide , flutamide , nilutamide )Oenanthotoxin Pentylenetetrazol (pentetrazol) Phenylsilatrane Picrotoxin (i.e., picrotin , picrotoxinin and dihydropicrotoxinin )Pregnenolone sulfate Propybicyphat PWZ-029 Radequinil Ro 15-4513 Ro 19-4603 RO4882224 RO4938581 Sarmazenil SCS Suritozole TB-21007 TBOB TBPS TCS-1105 Terbequinil TETS Thujone U-93631 Zinc ZK-93426 GABAA -ρ Tooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABAB Tooltip γ-Aminobutyric acid B receptor
Information related to Iomazenil
