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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 |
1999-3-11
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pubmed:abstractText |
New dimers of known 5HT1 ligands (5HT, 1-NP or 8-OH-DPAT) have been prepared and evaluated at human cloned 5HT1B, 5HT1D and 5HT1A receptors. Binding experiments show that all these dimers have better affinities at 5HT1B/1D receptors than their corresponding monomeric ligands. Studies of inhibition of the forskolin-stimulated c-AMP formation mediated by the human 5HT1B receptor show that hetero-bivalent ligands [combining an agonist (5HT) with an antagonist (1-NP)] behave as partial agonists while the intrinsic activity of bivalent antagonists (combining two 1-NP residues) was found to be spacer dependent. Surprisingly enough, the dimer of 8-OH-DPAT 6 binds to 5HT1A, 5HT1B and 5HT1D receptors with similar high affinity.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/1-(1-naphthyl)piperazine,
http://linkedlifedata.com/resource/pubmed/chemical/8-Hydroxy-2-(di-n-propylamino)tetral...,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/HTR1B protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1B,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1D,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin, 5-HT1,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
2
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1407-12
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:9871775-8-Hydroxy-2-(di-n-propylamino)tetralin,
pubmed-meshheading:9871775-Cyclic AMP,
pubmed-meshheading:9871775-Humans,
pubmed-meshheading:9871775-Ligands,
pubmed-meshheading:9871775-Piperazines,
pubmed-meshheading:9871775-Radioligand Assay,
pubmed-meshheading:9871775-Receptor, Serotonin, 5-HT1B,
pubmed-meshheading:9871775-Receptor, Serotonin, 5-HT1D,
pubmed-meshheading:9871775-Receptors, Serotonin,
pubmed-meshheading:9871775-Receptors, Serotonin, 5-HT1,
pubmed-meshheading:9871775-Recombinant Proteins,
pubmed-meshheading:9871775-Serotonin,
pubmed-meshheading:9871775-Serotonin Agents,
pubmed-meshheading:9871775-Serotonin Antagonists,
pubmed-meshheading:9871775-Serotonin Receptor Agonists
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pubmed:year |
1998
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pubmed:articleTitle |
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes.
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pubmed:affiliation |
Medicinal Chemistry Division, Centre de Recherche Pierre FABRE, Castres, France.
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pubmed:publicationType |
Journal Article
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