Document Detail

Inhibition of a type B monoamine oxidase inhibitor, (E)-2-(4-fluorophenethyl)-3-fluoroallylamine (MDL-72974A), on semicarbazide-sensitive amine oxidases isolated from vascular tissues and sera of different species.
MedLine Citation:
PMID:  1739419     Owner:  NLM     Status:  MEDLINE    
(E)-2-(4-Fluorophenethyl)-3-fluoroallylamine hydrochloride (MDL-72974A) has been discovered recently to be a very potent and highly selective type B monoamine oxidase inhibitor. We have found that this inhibitor is also capable of inhibiting semicarbazide-sensitive amine oxidases (SSAOs) obtained from vascular tissues and sera of different species. The inhibition of SSAO by MDL-72974A was irreversible and time dependent. It was competitive without preincubation of the enzyme with the inhibitor and demonstrated a mixed-type of inhibition when the enzyme was preincubated with the inhibitor. The IC50 values were estimated to be 2 x 10(-9) M, 5 x 10(-9) M, 8 x 10(-8) M and 2 x 10(-8) M for SSAO from dog aorta, rat aorta, bovine aorta and human umbilical artery, respectively. SSAO obtained from bovine serum was relatively insensitive to MDL-72974A (IC50 = 3 x 10(-7) M. Following intraperitoneal administration of MDL-72974A, rat brain MAO-B was inhibited with the ED50 value being about 0.2 mg/kg. Rat aorta SSAO was also inhibited and to a similar extent by the same dose. MDL-72974A is the most potent SSAO inhibitor that has been described thus far.
P H Yu; D M Zuo
Related Documents :
24304579 - Ghrelin accelerates the healing of oral ulcers in non-sialoadenectomized and sialoadene...
5399 - Studies on peroxisomes. v. effect of ethyl p-chlorophenoxyisobutyrate on the centrifuga...
8925849 - Synthesis and in vivo studies of a specific monoamine oxidase b inhibitor: 5-[4-(benzyl...
3021279 - Aminophylline shortens thiopental sleep-time and enhances noradrenergic neurotransmissi...
1159629 - Extraneuronal monoamine oxidase in rat heart: biochemical characterization and electron...
2724679 - Effect of diethylnitrosamine on monoamine oxidase in rat liver.
6996219 - Mutagenicity of urine from rats and mice treated with acrylonitrile.
20412799 - Recrudescence of toxoplasma gondii infection in chronically infected rats (rattus norve...
7070579 - Effect of thyroid dysfunction upon phospholipid composition and cdp-choline incorporati...
Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Biochemical pharmacology     Volume:  43     ISSN:  0006-2952     ISO Abbreviation:  Biochem. Pharmacol.     Publication Date:  1992 Jan 
Date Detail:
Created Date:  1992-03-17     Completed Date:  1992-03-17     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0101032     Medline TA:  Biochem Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  307-12     Citation Subset:  IM    
Department of Psychiatry, University of Saskatchewan, Saskatoon, Canada.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Allyl Compounds*
Amino Acid Oxidoreductases / blood,  drug effects,  isolation & purification*
Aorta / drug effects,  enzymology
Butylamines / administration & dosage,  pharmacology*
Caudate Nucleus / drug effects,  enzymology
Dose-Response Relationship, Drug
Mitochondria, Liver / drug effects,  enzymology
Monoamine Oxidase / blood
Monoamine Oxidase Inhibitors / pharmacology*
Rats, Inbred Strains
Semicarbazides / pharmacology*
Umbilical Arteries / enzymology
Reg. No./Substance:
0/Allyl Compounds; 0/Butylamines; 0/Monoamine Oxidase Inhibitors; 0/Semicarbazides; 119386-96-8/mofegiline; EC 1.4.-/Amino Acid Oxidoreductases; EC Oxidase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Irreversible inhibition of thromboxane (TX) A2 synthesis by Y-20811, a selective TX synthetase inhib...
Next Document:  Purification of the human blood platelet thromboxane A2/prostaglandin H2 receptor protein.