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| Subject | Predicate | Object |
|---|---|---|
| http://purl.uniprot.org/citations/21422162 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/21422162 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/21422162 | http://www.w3.org/2000/01/rdf-schema#comment | "The 5-hydroxytryptamine (5-HT) 1E receptor is highly expressed in the human frontal cortex and hippocampus, and this distribution suggests the function of 5-HT(1E) receptors might be linked to memory. To test this hypothesis, behavioral experiments are needed. Because rats and mice lack a 5-HT(1E) receptor gene, knockout strategies cannot be used to elucidate this receptor's functions. Thus, selective pharmacological tools must be developed. The tryptamine-related agonist BRL54443 [5-hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole] is one of the few agents that binds 5-HT(1E) receptors with high affinity and some selectively; unfortunately, it binds equally well to 5-HT(1F) receptors (K(i) ≈ 1 nM). The differences between tryptamine binding requirements of these two receptor populations have never been extensively explored; this must be done to guide the design of analogs with greater selectivity for 5-HT(1E) receptors versus 5-HT(1F) receptors. Previously, we determined the receptor binding affinities of a large series of tryptamine analogs at the 5-HT(1E) receptor; we now examine the affinities of this same series of compounds at 5-HT(1F) receptors. The affinities of these compounds at 5-HT(1E) and 5-HT(1F) receptors were found to be highly correlated (r = 0.81). All high-affinity compounds were full agonists at both receptor populations. We identified 5-N-butyryloxy-N,N-dimethyltryptamine as a novel 5-HT(1F) receptor agonist with >60-fold selectivity versus 5-HT(1E) receptors. There is significant overlap between 5-HT(1E) and 5-HT(1F) receptor orthosteric binding properties; thus, identification of 5-HT(1E)-selective orthosteric ligands will be difficult. The insights generated from this study will inform future drug development and molecular modeling studies for both 5-HT(1E) and 5-HT(1F) receptors."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.org/dc/terms/identifier | "doi:10.1124/jpet.111.179606"xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.org/dc/terms/identifier | "doi:10.1124/jpet.111.179606"xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/author | "Dukat M."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/author | "Dukat M."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/author | "Glennon R.A."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/author | "Glennon R.A."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/author | "Klein M.T."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/author | "Klein M.T."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/author | "Teitler M."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/author | "Teitler M."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/date | "2011"xsd:gYear |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/date | "2011"xsd:gYear |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/name | "J. Pharmacol. Exp. Ther."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/name | "J. Pharmacol. Exp. Ther."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/pages | "860-867"xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/pages | "860-867"xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/title | "Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/title | "Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships."xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/volume | "337"xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://purl.uniprot.org/core/volume | "337"xsd:string |
| http://purl.uniprot.org/citations/21422162 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/21422162 |
| http://purl.uniprot.org/citations/21422162 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/21422162 |