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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 |
A series of (8 beta)-6-methyl-1-(1-methylethyl)ergoline-8-carboxylic acid cycloalkyl esters were prepared and examined for blockade of vascular 5HT2 receptors. The antagonist in this series that had the highest 5HT2 receptor affinity was (8 beta)-6-methyl-1-(1-methylethyl)ergoline-8-carboxylic acid cyclohexyl ester. This compound was therefore chosen as the basic backbone of a structure-activity study to determine what effect different N1-substituents, N6-substituents, and ester ring substituents had on 5HT2 receptor affinity. Maximal 5HT2 receptor affinity was obtained when the N1-substituent was isopropyl, the N6-substituent was methyl, and there was a hydroxy or keto substituent in the 4-position of the ester cyclohexyl ring.
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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
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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
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pubmed:pagination |
444-8
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:3339614-Animals,
pubmed-meshheading:3339614-Ergolines,
pubmed-meshheading:3339614-Male,
pubmed-meshheading:3339614-Rats,
pubmed-meshheading:3339614-Rats, Inbred Strains,
pubmed-meshheading:3339614-Receptors, Serotonin,
pubmed-meshheading:3339614-Serotonin Antagonists,
pubmed-meshheading:3339614-Structure-Activity Relationship
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pubmed:year |
1988
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pubmed:articleTitle |
(8 beta)-Ergoline-8-carboxylic acid cycloalkyl esters as serotonin antagonists: structure-activity study.
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pubmed:affiliation |
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.
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pubmed:publicationType |
Journal Article
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