IOMAZENIL

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C15H14IN3O3
Molecular Weight	411.1944
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOC(=O)C1=C2CN(C)C(=O)C3=C(I)C=CC=C3N2C=N1

InChI

InChIKey=FRIZVHMAECRUBR-UHFFFAOYSA-N

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

HIDE SMILES / InChI

Molecular Formula	C15H14IN3O3
Molecular Weight	411.1944
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2161451
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/21068719 https://www.ncbi.nlm.nih.gov/pubmed/16061765

Iomazenil (also known as Ro16-0154, benzodine) is a partial inverse agonist of central-type benzodiazepine receptors (BZR) which binds specifically to BZR with high affinity 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.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABAergic synapse 4 Target ID: map04727 Sources: http://www.genome.jp/dbget-bin/www_bget?dr:D02283 \| https://www.ncbi.nlm.nih.gov/pubmed/21068719	Modulator 846
GABA-A receptor; agonist GABA site 13 Target ID: CHEMBL2109244 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8781136 \| https://www.ncbi.nlm.nih.gov/pubmed/8988959 \| http://www.sigmaaldrich.com/catalog/product/sigma/sml0645?lang=en®ion=RU	Antagonist 2849

Conditions

Condition	Modality	Targets	Highest Phase	Product
Acohol dependence 1 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11003213	Diagnostic		Preclinical	Unknown Approved Use Unknown
Schizophrenia 305 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21068719	Diagnostic		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Blood-brain barrier transport and protein binding of flumazenil and iomazenil in the rat: implications for neuroreceptor studies.	1999-09	10478646
SPECT imaging of the benzodiazepine receptor: feasibility of in vivo potency measurements from stepwise displacement curves.	1991-09	1652627
Receptor binding characterization of the benzodiazepine radioligand 125I-Ro16-0154: potential probe for SPECT brain imaging.	1990	2174487

Patents

Sample Use Guides

In Vivo Use Guide

Clinically stable chronic schizophrenia patients received iomazenil (3.7 ug) administered intravenously over 10 min

Route of Administration: Intravenous

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:12:25 GMT 2025` Edited by `admin` on `Mon Mar 31 18:12:25 GMT 2025`
Record UNII	7DVX185FLQ
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

RO 16-0154

Preferred Name

English

IOMAZENIL

Common Name

English

4H-IMIDAZO(1,5-A)(1,4)BENZODIAZEPINE-3-CARBOXYLIC ACID, 5,6-DIHYDRO-7-IODO-5-METHYL-6-OXO-, ETHYL ESTER

Systematic Name

English

RO-16-0154

Code

English

RO16-0154

Code

English

Code System Code Type Description

FDA UNII

7DVX185FLQ