Document Detail


Selective inhibition of the A form of monoamine oxidase by 4-dimethylamino-alpha-methylphenylalkylamine derivatives in the rat.
MedLine Citation:
PMID:  7088264     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The inhibitory effects on monoamine oxidase (MAO) of some dimethylamino-alpha-phenylalkylamine derivatives were examined in a rat brain mitochondrial preparation in vitro and in rat brain slices following oral administration. In the in vitro assay the compounds were shown to be selective inhibitors of the A form of MAO, being 100-600 times more potent in inhibiting the deamination of [14C]5-hydroxytryptamine than that of [14C]phenetylamine. Using an ex vivo brain slice technique it was found that the new compounds were reversible and very selective inhibitors of type A MAO in the rat brain and the most potent compounds (FLA 405, 314, 336 and 558) were equipotent with clorgyline. The compounds increased the monoamine concentrations in whole rat brain, particularly that of 5-hydroxytryptamine, in the same dose range which produced MAO inhibition. Some of the new compounds, e.g. FLA 336 and FLA 717, caused only weak potentiation of the vaso-pressor effect of orally administered tyramine.
Authors:
A L Ask; W Hellström; S Norrman; S O Ogren; S B Ross
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Neuropharmacology     Volume:  21     ISSN:  0028-3908     ISO Abbreviation:  Neuropharmacology     Publication Date:  1982 Apr 
Date Detail:
Created Date:  1982-08-07     Completed Date:  1982-08-07     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0236217     Medline TA:  Neuropharmacology     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  299-308     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Culture Techniques
Deamination
Dopamine / metabolism
Hypothalamus / drug effects*,  enzymology
Male
Mitochondria / drug effects*,  enzymology
Monoamine Oxidase / metabolism*
Monoamine Oxidase Inhibitors* / pharmacology*
Norepinephrine / metabolism
Phenethylamines / metabolism,  pharmacology*
Rats
Rats, Inbred Strains
Serotonin / metabolism
Structure-Activity Relationship
Tyramine / metabolism
Chemical
Reg. No./Substance:
0/Monoamine Oxidase Inhibitors; 0/Phenethylamines; 50-67-9/Serotonin; 51-41-2/Norepinephrine; 51-67-2/Tyramine; EC 1.4.3.4/Monoamine Oxidase

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


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