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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/31 07:05:01」(JST)

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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

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

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

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

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, Clinicaltrials.gov

English Journal

Analysis of a child who developed abnormal neuropsychiatric symptoms after administration of oseltamivir: a case report.

Morimoto K1,2, Nagaoka K3, Nagai A4, Kashii H5, Hosokawa M6, Takahashi Y7, Ogihara T8, Kubota M9.
BMC neurology.BMC Neurol.2015 Aug 5;15:130. doi: 10.1186/s12883-015-0393-2.
BACKGROUND: Neuropsychiatric side effects of oseltamivir occur occasionally, especially in infants and young patients, but nothing is known about possible contributory factors.CASE PRESENTATION: We report a case of a 15-year-old Japanese female with influenza infection who developed abnormal psychia
PMID 26242979

Role of GABA Deficit in Sensitivity to the Psychotomimetic Effects of Amphetamine.

Ahn KH1, Sewell A1, Elander J1, Pittman B2, Ranganathan M1, Gunduz-Bruce H3, Krystal J1, D'Souza DC1.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology.Neuropsychopharmacology.2015 May 8. doi: 10.1038/npp.2015.132. [Epub ahead of print]
Some schizophrenia patients are more sensitive to amphetamine (AMPH)-induced exacerbations in psychosis-an effect that correlates with higher striatal dopamine release. This enhanced vulnerability may be related to gamma-aminobutyric acid (GABA) deficits observed in schizophrenia. We hypothesized th
PMID 25953357

Upregulated GABA Inhibitory Function in ADHD Children with Child Behavior Checklist-Dysregulation Profile: 123I-Iomazenil SPECT Study.

Nagamitsu S1, Yamashita Y1, Tanigawa H2, Chiba H3, Kaida H2, Ishibashi M2, Kakuma T4, Croarkin PE5, Matsuishi T1.
Frontiers in psychiatry.Front Psychiatry.2015 Jun 2;6:84. doi: 10.3389/fpsyt.2015.00084. eCollection 2015.
The child behavior checklist-dysregulation profile (CBCL-DP) refers to a pattern of elevated scores on the attention problems, aggression, and anxiety/depression subscales of the child behavior checklist. The aim of the present study was to investigate the potential role of GABA inhibitory neurons i
PMID 26082729

Japanese Journal

Cognitive Dysfunction Survey of the Japanese Patients with Moyamoya Disease (COSMO-JAPAN Study): Study Protocol

Neurologia medico-chirurgica advpub(0), 2015
NAID 130004922316

Cognitive Dysfunction Survey of the Japanese Patients with Moyamoya Disease (COSMO-JAPAN Study): Study Protocol

Neurologia medico-chirurgica 55(3), 199-203, 2015
NAID 130004725004

頭部外傷後高次脳機能障害に対するIomazenil SPECT多施設共同研究 (特集高次脳機能障害と画像診断(前編))

PET journal (26), 45-47, 2014
NAID 40020149201

「イオマゼニル」

Iomazenil
Systematic (IUPAC) name
	ethyl 7-(123I)iodo-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
Identifiers
CAS Registry Number	127985-21-1; 127396-36-5 (123I)
ATC code	None
PubChem	CID: 65959
ChemSpider	59362
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 ;

　　[★]

英: iomazenil
商: ベンゾダイン
関: イオマゼニル(123I)

放射性医薬品;てんかん診断薬

[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.

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iomazenil