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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1988-3-16
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pubmed:abstractText |
Prior work in these laboratories identified (+/-)-5-hydroxy-6-methyl-2- (di-n-propylamino)tetralin as a dopaminergic agonist prodrug. The ortho methyl hydroxy aromatic substitution pattern in this molecule has now been incorporated into the aporphine ring system to give a congener of the dopaminergic agonist apomorphine in which the position 10 OH group has been replaced by methyl. Preparation of the target compound involved acid-catalyzed rearrangement of the 3-(1-phenyltetrazolyl) ether of morphine and subsequent molecular modification of the product, the 10-(1-phenyltetrazolyl) ether of (R)-(-)-apomorphine. Surprisingly, the target compound elicited no responses in any assays for effects at dopamine receptors, but rather it displayed pharmacological properties consistent with its being a serotonergic agonist with a high degree of selectivity for 5-HT1A receptors similar to the serotonergic agonist 8-hydroxy-2-(di-n-propylamino)tetralin.
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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 |
Feb
|
pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
31
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
|
pubmed:pagination |
313-8
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3339604-Animals,
pubmed-meshheading:3339604-Apomorphine,
pubmed-meshheading:3339604-Aporphines,
pubmed-meshheading:3339604-Binding Sites,
pubmed-meshheading:3339604-Cats,
pubmed-meshheading:3339604-Magnetic Resonance Spectroscopy,
pubmed-meshheading:3339604-Male,
pubmed-meshheading:3339604-Molecular Conformation,
pubmed-meshheading:3339604-Rats,
pubmed-meshheading:3339604-Rats, Inbred Strains,
pubmed-meshheading:3339604-Receptors, Serotonin,
pubmed-meshheading:3339604-Serotonin,
pubmed-meshheading:3339604-Structure-Activity Relationship
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pubmed:year |
1988
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pubmed:articleTitle |
(R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist.
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pubmed:affiliation |
Division of Medicinal and Natural Products Chemistry, College of Pharmacy, University of Iowa, Iowa City 52242.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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