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rdf:type |
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lifeskim:mentions |
umls-concept:C0012984,
umls-concept:C0021554,
umls-concept:C0036751,
umls-concept:C0205227,
umls-concept:C0449560,
umls-concept:C0530967,
umls-concept:C0675717,
umls-concept:C1522492,
umls-concept:C1554184,
umls-concept:C1704675,
umls-concept:C1948027
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pubmed:issue |
3
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pubmed:dateCreated |
2000-9-12
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pubmed:abstractText |
Molecular cloning and expression of canine (ca) serotonin 5-HT(1B) and ca 5-HT(1D) receptor subtypes showed that besides the lower binding affinity of ketanserin for the ca 5-HT(1D) receptor, the ligand binding profiles were similar to their human homologues. Site-directed mutagenesis studies suggest that a Gln(189) residue in the second extracellular loop of the ca 5-HT(1D) receptor may partially account for the lower binding affinity of ketanserin. The coupling of ca 5-HT(1B) and ca 5-HT(1D) receptor subtypes to the phospholipase C pathway was analyzed by measuring stimulation of inositol phosphate formation in COS-7 cells. Zolmitriptan potently stimulated (EC(50) = 4.9 nM) the inositol phosphate formation at ca 5-HT(1D) receptors in a fully pertussis toxin (PTX)-dependent manner, whereas only a weak PTX-resistant inositol phosphate response (26-29% at 10 microM zolmitriptan) could be detected for the ca 5-HT(1B) receptor at a similar expression level. In contrast, both ca 5-HT(1B) and ca 5-HT(1D) receptor subtypes yielded a similar maximal magnitude of inositol phosphate formation (300-340% at 10 microM zolmitriptan) upon co-expression with a mouse (m) G(alpha15) protein. PTX treatment and co-expression with a beta-adrenergic receptor kinase C-terminal polypeptide partially (20-46%) abolished the m G(alpha15) protein-dependent ca 5-HT(1B) and ca 5-HT(1D) receptor-mediated stimulation of inositol phosphate formation. This study suggests both 5-HT receptor subtypes can activate betagamma subunits of endogenous G(i/o) proteins besides their coupling to recombinant m G(alpha15) protein.
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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/G protein alpha 16,
http://linkedlifedata.com/resource/pubmed/chemical/GTP-Binding Protein alpha...,
http://linkedlifedata.com/resource/pubmed/chemical/GTP-Binding Protein alpha...,
http://linkedlifedata.com/resource/pubmed/chemical/HTR1B protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Heterotrimeric GTP-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Inositol Phosphates,
http://linkedlifedata.com/resource/pubmed/chemical/Ketanserin,
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/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-3042
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
75
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1180-9
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:10936201-Amino Acid Sequence,
pubmed-meshheading:10936201-Animals,
pubmed-meshheading:10936201-COS Cells,
pubmed-meshheading:10936201-Cloning, Molecular,
pubmed-meshheading:10936201-Dogs,
pubmed-meshheading:10936201-GTP-Binding Protein alpha Subunits, Gi-Go,
pubmed-meshheading:10936201-GTP-Binding Protein alpha Subunits, Gq-G11,
pubmed-meshheading:10936201-Heterotrimeric GTP-Binding Proteins,
pubmed-meshheading:10936201-Humans,
pubmed-meshheading:10936201-Inositol Phosphates,
pubmed-meshheading:10936201-Ketanserin,
pubmed-meshheading:10936201-Kinetics,
pubmed-meshheading:10936201-Mice,
pubmed-meshheading:10936201-Molecular Sequence Data,
pubmed-meshheading:10936201-Mutagenesis, Site-Directed,
pubmed-meshheading:10936201-Receptor, Serotonin, 5-HT1B,
pubmed-meshheading:10936201-Receptor, Serotonin, 5-HT1D,
pubmed-meshheading:10936201-Receptors, Serotonin,
pubmed-meshheading:10936201-Recombinant Proteins,
pubmed-meshheading:10936201-Sequence Alignment,
pubmed-meshheading:10936201-Sequence Homology, Amino Acid,
pubmed-meshheading:10936201-Serotonin,
pubmed-meshheading:10936201-Transfection
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pubmed:year |
2000
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pubmed:articleTitle |
Coupling of canine serotonin 5-HT(1B) and 5-HT(1D) receptor subtypes to the formation of inositol phosphates by dual interactions with endogenous G(i/o) and recombinant G(alpha15) proteins.
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pubmed:affiliation |
Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, Castres, France.
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pubmed:publicationType |
Journal Article
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