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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
1987-12-9
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pubmed:abstractText |
Twenty derivatives bearing substituents on the phenolic function of (-)-3-(3-hydroxyphenyl)-N-propylpiperidine [(-)-3-PPP] were synthesized and tested as prodrugs. The carbamate ester derivatives were found to be the most suitable prodrugs, and especially the 4-isopropylphenylcarbamate 20 was capable of escaping the first-pass metabolism and still generating high plasma levels of the parent compound. Four hours after an oral dose of 100 mumol/kg to rats, a plasma level of 2400 nmol/L of (-)-3-PPP was detected by an HPLC method. This was 90 times the level reached after 4 h (27 nmol/L) when (-)-3-PPP itself was given orally at the same dose.
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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 |
Nov
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2008-12
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:3669008-Animals,
pubmed-meshheading:3669008-Carbamates,
pubmed-meshheading:3669008-Pharmaceutical Preparations,
pubmed-meshheading:3669008-Piperidines,
pubmed-meshheading:3669008-Prodrugs,
pubmed-meshheading:3669008-Rats,
pubmed-meshheading:3669008-Rats, Inbred Strains,
pubmed-meshheading:3669008-Receptors, Dopamine,
pubmed-meshheading:3669008-Structure-Activity Relationship
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pubmed:year |
1987
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pubmed:articleTitle |
Carbamate ester derivatives as potential prodrugs of the presynaptic dopamine autoreceptor agonist (-)-3-(3-hydroxyphenyl)-N-propylpiperidine.
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pubmed:affiliation |
Astra Alab AB, Research & Development Laboratories, Södertälje, Sweden.
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pubmed:publicationType |
Journal Article
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