BEFLOXATONE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C15H18F3NO5
Molecular Weight	349.3023
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC[C@H]1CN(C(=O)O1)C2=CC=C(OCC[C@@H](O)C(F)(F)F)C=C2

InChI

InChIKey=IALVDLPLCLFBCF-CHWSQXEVSA-N

InChI=1S/C15H18F3NO5/c1-22-9-12-8-19(14(21)24-12)10-2-4-11(5-3-10)23-7-6-13(20)15(16,17)18/h2-5,12-13,20H,6-9H2,1H3/t12-,13-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C15H18F3NO5
Molecular Weight	349.3023
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16160936 | https://adisinsight.springer.com/drugs/800001426

Befloxatone (MD-370,503) is a reversible inhibitor of monoamine oxidase A that was developed by Synthelabo for the treatment of depression, social phobias, and panic disorders. This drug participated in phase III clinical trials in France for depression. In addition participated in phase II for smoking cessation, anxiety disorders. Befloxatone has a good safety profile, lacking sedative, convulsant, anticholinergic and cardiovascular effects. However, all studies were discontinued.

Originator

Approval Year

PubMed

Title	Date	PubMed
Mapping the cerebral monoamine oxidase type A: positron emission tomography characterization of the reversible selective inhibitor [11C]befloxatone.	2003 May	12606609
Acute inhibition of cardiac monoamine oxidase A after tobacco smoke inhalation: validation study of [11C]befloxatone in rats followed by a positron emission tomography application in baboons.	2005 Jul	15833896
Cerebral monoamine oxidase A inhibition in tobacco smokers confirmed with PET and [11C]befloxatone.	2009 Feb	19142115
Electrophysiological characterization of harmane-induced activation of mesolimbic dopamine neurons.	2010 Mar 10	20026027

Patents

Sample Use Guides

In Vivo Use Guide

To assess the effects of single oral doses of befloxatone (5, 10, and 20 mg) on psychomotor performance and memory, a randomized, double-blind, five-way, crossover study with both placebo and amitriptyline (50 mg) was carried out in 15 healthy male volunteers.

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 16:56:22 GMT 2023` Edited by `admin` on `Sat Dec 16 16:56:22 GMT 2023`
Record UNII	4H75PAD8M3
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

BEFLOXATONE

Official Name

English

BEFLOXATONE [MI]

Common Name

English

befloxatone [INN]

Common Name

English

BEFLOXATONE [MART.]

Common Name

English

Befloxatone [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C667