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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1981-12-21
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pubmed:abstractText |
1 A number of aromatic-N-propargyl (acetylenic) compounds and indoleamines were tested for their inhibitory action on monoamine oxidase (MAO) type A and type B using the substrates 5-hydroxytryptamine (5-HT), beta-phenylethylamine (PEA) and dopamine. 2 Structure activity studies with aromatic-N-propragyl (acetylenic) derivatives have shown that MAO inhibitory potency is least dependent on the aromatic portion of the compounds. N-methylated propargyl derivatives are the most active and replacement of the methyl group with a higher alkyl or aromatic group results in significant reduction of activity. The triple bond in the N-propargyl portion is absolutely essential for activity and must be beta-to the nitrogen. It is the acetylenic group that gives these compounds their irreversible MAO inhibitory property. 3 The present study has indicated that since the acetylenic compounds resemble the enzyme substrates the distance between the aromatic ring and the N-propargyl terminal is crucial in designating the type A or type B MAO inhibitory property. For MAO type A inhibition, a distance equivalent to at least three carbon units is required, while for the inhibition of the B type enzyme this distance can be 1 or 2 carbon units. 4 The compounds AGN-1133 and AGN-1135 show most promise in Parkinson's disease or as anti-depressants because of their irreversible selective type B MAO inhibition in vitro and in vivo. 5 A number of indoleamine derivatives were found to be reversible selective type A inhibitors.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-1172524,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-1203627,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-13979700,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-14184932,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-14907713,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-14934658,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-4748552,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-481419,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-4850215,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-5054207,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-5066229,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-5659776,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-5960901,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-619909,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-65560,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-6768943,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-6793119,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-708454,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-7262,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-728327,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-745014,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-745015,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-745020,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-834248,
http://linkedlifedata.com/resource/pubmed/commentcorrection/7284698-96466
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
73
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
55-64
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
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pubmed:year |
1981
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pubmed:articleTitle |
Selective acetylenic 'suicide' and reversible inhibitors of monoamine oxidase types A and B.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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