pubmed-article:7506312 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:7506312 | lifeskim:mentions | umls-concept:C0379900 | lld:lifeskim |
pubmed-article:7506312 | lifeskim:mentions | umls-concept:C1704675 | lld:lifeskim |
pubmed-article:7506312 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
pubmed-article:7506312 | lifeskim:mentions | umls-concept:C0380600 | lld:lifeskim |
pubmed-article:7506312 | lifeskim:mentions | umls-concept:C0243072 | lld:lifeskim |
pubmed-article:7506312 | pubmed:issue | 26 | lld:pubmed |
pubmed-article:7506312 | pubmed:dateCreated | 1994-2-4 | lld:pubmed |
pubmed-article:7506312 | pubmed:abstractText | A series of 2-(dipropylamino)tetralin derivatives in which the C8 substituent is varied has been prepared and evaluated pharmacologically to explore the importance of the C8 substituent in the interaction of 2-aminotetralin-based ligands with serotonin (5-HT1A) receptors. Enantiopure derivatives were prepared by facile palladium-catalyzed reactions of the triflates of the enantiomers of 8-hydroxy-2-(dipropylamino)tetralin (8-OH-DPAT, 1). The affinity of the compounds for the 5-HT1A receptors was evaluated by competition experiments with [3H]-8-OH-DPAT in rat hippocampal and cortical tissue. In addition, the compounds were evaluated for central 5-HT and dopamine receptor stimulating activity in vivo by use of biochemical and behavioral assays in rats. With the exception of the carboxy-substituted derivative which is devoid of 5-HT1A receptor affinity, the compounds have moderate to high affinities (K(i) values range from 0.7 to 130 nM) for 5-HT1A receptors. Surprisingly, several of the derivatives do not produce any apparent effects in vivo although they have fairly high 5-HT1A receptor affinities. However, the methoxycarbonyl- and acetyl-substituted derivatives are potent 5-HT1A receptor agonists in vivo and exhibit in vitro affinities in the same range as the enantiomers of 1. | lld:pubmed |
pubmed-article:7506312 | pubmed:language | eng | lld:pubmed |
pubmed-article:7506312 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7506312 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:7506312 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7506312 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7506312 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7506312 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7506312 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7506312 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7506312 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7506312 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:7506312 | pubmed:month | Dec | lld:pubmed |
pubmed-article:7506312 | pubmed:issn | 0022-2623 | lld:pubmed |
pubmed-article:7506312 | pubmed:author | pubmed-author:LewanderTT | lld:pubmed |
pubmed-article:7506312 | pubmed:author | pubmed-author:YuHH | lld:pubmed |
pubmed-article:7506312 | pubmed:author | pubmed-author:LieII | lld:pubmed |
pubmed-article:7506312 | pubmed:author | pubmed-author:HacksellUU | lld:pubmed |
pubmed-article:7506312 | pubmed:author | pubmed-author:SvenssonB EBE | lld:pubmed |
pubmed-article:7506312 | pubmed:author | pubmed-author:CortizoLL | lld:pubmed |
pubmed-article:7506312 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:7506312 | pubmed:day | 24 | lld:pubmed |
pubmed-article:7506312 | pubmed:volume | 36 | lld:pubmed |
pubmed-article:7506312 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:7506312 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:7506312 | pubmed:pagination | 4221-9 | lld:pubmed |
pubmed-article:7506312 | pubmed:dateRevised | 2008-11-21 | lld:pubmed |
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pubmed-article:7506312 | pubmed:year | 1993 | lld:pubmed |
pubmed-article:7506312 | pubmed:articleTitle | Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors. | lld:pubmed |
pubmed-article:7506312 | pubmed:affiliation | Department of Organic Pharmaceutical Chemistry, Uppsala Biomedical Centre, Uppsala University, Sweden. | lld:pubmed |
pubmed-article:7506312 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:7506312 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:7506312 | lld:chembl |
http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:7506312 | lld:pubmed |