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    
Abstract/OtherAbstract:
(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.
Authors:
P H Yu; D M Zuo
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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    
Affiliation:
Department of Psychiatry, University of Saskatchewan, Saskatoon, Canada.
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MeSH Terms
Descriptor/Qualifier:
Allyl Compounds*
Amino Acid Oxidoreductases / blood,  drug effects,  isolation & purification*
Animals
Aorta / drug effects,  enzymology
Butylamines / administration & dosage,  pharmacology*
Cattle
Caudate Nucleus / drug effects,  enzymology
Deamination
Dogs
Dose-Response Relationship, Drug
Humans
Kinetics
Male
Mitochondria, Liver / drug effects,  enzymology
Monoamine Oxidase / blood
Monoamine Oxidase Inhibitors / pharmacology*
Rats
Rats, Inbred Strains
Semicarbazides / pharmacology*
Umbilical Arteries / enzymology
Chemical
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 1.4.3.4/Monoamine Oxidase

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


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