Abstract
The serotonin (5-hydroxytryptamine (5-HT)) 1B and 1D receptor subtypes share a high amino acid sequence identity and have similar ligand binding properties. In this study, we demonstrate that both receptor subtypes exist as monomers and homodimers when expressed alone and as monomers and heterodimers when co-expressed. Gene expression studies have shown that there are brain regions where the 5-HT1B and 5-HT1D receptors are co-localized and where heterodimerization may occur physiologically. This is the first direct visualization of the physical association between G protein-coupled receptors of different subtypes.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Benzamides / metabolism
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Binding, Competitive
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Cell Membrane / metabolism
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Cells, Cultured
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Dimerization
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Gene Expression
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Immunoblotting
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Ketanserin / metabolism
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Molecular Weight
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Pyridines / metabolism
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Receptor, Serotonin, 5-HT1B
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Receptor, Serotonin, 5-HT1D
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Receptors, Serotonin / chemistry*
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Receptors, Serotonin / genetics
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Receptors, Serotonin / metabolism*
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Recombinant Proteins / chemistry
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Recombinant Proteins / genetics
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Recombinant Proteins / metabolism
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Serotonin / analogs & derivatives
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Serotonin / metabolism
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Serotonin Antagonists / metabolism
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Serotonin Receptor Agonists / metabolism
Substances
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Benzamides
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N-(4-methoxy-3-(4-methylpiperazin-1-yl)phenyl)-3-methyl-4-(4-pyridyl)benzamide
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Pyridines
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Receptor, Serotonin, 5-HT1B
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Receptor, Serotonin, 5-HT1D
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Receptors, Serotonin
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Recombinant Proteins
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Serotonin Antagonists
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Serotonin Receptor Agonists
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Serotonin
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5-carboxamidotryptamine
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Ketanserin