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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
15
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pubmed:dateCreated |
1993-8-31
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pubmed:abstractText |
The enantiomers of 6,7,8,9-tetrahydro-N,N-di-n-propyl-3H-benz[e]indol-8- amine (S-(-)-2b and R-(+)-2b) and their corresponding 1-formyl analogs (S-(-)-6 and R-(+)-6) were prepared and evaluated pharmacologically for serotonergic and dopaminergic activity. The introduction of a formyl group in the 1-position shifted the pharmacological profile of 2b from a mixed D2/5-HT1A agonists to a selective 5-HT1A agonist (6). The enantiomers of 6 were agonists with full intrinsic activity and had an affinity comparable to that of 8-hydroxy-2-(di-n-propylamino)tetrahydronaphthalene (8-OH-DPAT). In contrast to 8-OH-DPAT, the enantiomers of compound 6 were found to have good oral availability.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
23
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pubmed:volume |
36
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2059-65
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:8340910-8-Hydroxy-2-(di-n-propylamino)tetralin,
pubmed-meshheading:8340910-Administration, Oral,
pubmed-meshheading:8340910-Animals,
pubmed-meshheading:8340910-Behavior, Animal,
pubmed-meshheading:8340910-Biological Availability,
pubmed-meshheading:8340910-Indoles,
pubmed-meshheading:8340910-Male,
pubmed-meshheading:8340910-Rats,
pubmed-meshheading:8340910-Rats, Sprague-Dawley,
pubmed-meshheading:8340910-Serotonin Receptor Agonists,
pubmed-meshheading:8340910-Stereoisomerism,
pubmed-meshheading:8340910-Structure-Activity Relationship
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pubmed:year |
1993
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pubmed:articleTitle |
(S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists.
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pubmed:affiliation |
Department of Pharmacology, University of Göteborg, Sweden.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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