http://purl.uniprot.org/citations/33156577 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/33156577 | http://www.w3.org/2000/01/rdf-schema#comment | "Association of G protein-coupled receptors into heterodimeric complexes has been reported for over 50 receptor pairs in vitro but functional in vivo validation remains a challenge. Our recent in vitro studies defined the functional fingerprint of heteromers composed of Gi -coupled melatonin MT2 receptors and Gq -coupled serotonin 5-HT2C receptors, in which melatonin transactivates phospholipase C (PLC) through 5-HT2C . Here, we identified this functional fingerprint in the mouse brain. Gq protein activation was probed by [35 S]GTPγS incorporation followed by Gq immunoprecipitation, and PLC activation by determining the inositol phosphate levels in brain lysates of animals previously treated with melatonin. Melatonin concentration-dependently activated Gq proteins and PLC in the hypothalamus and cerebellum but not in cortex. These effects were inhibited by the 5-HT2C receptor-specific inverse agonist SB-243213, and were absent in MT2 and 5-HT2C knockout mice, fully recapitulating previous in vitro data and indicating the involvement of MT2 /5-HT2C heteromers. The antidepressant agomelatine had a similar effect than melatonin when applied alone but blocked the melatonin-promoted Gq activation due to its 5-HT2C antagonistic component. Collectively, we provide strong functional evidence for the existence of MT2 /5-HT2C heteromeric complexes in mouse brain. These heteromers might participate in the in vivo effects of agomelatine."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.org/dc/terms/identifier | "doi:10.1096/fj.202000305r"xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/author | "Heisler L.K."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/author | "Gerbier R."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/author | "Jockers R."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/author | "Gbahou F."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/author | "Ndiaye-Lobry D."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/author | "Delagrange P."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/author | "Cecon E."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/author | "Martinez de Morentin P.B."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/date | "2021"xsd:gYear |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/name | "FASEB J"xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/pages | "e21161"xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/title | "Pharmacological evidence for transactivation within melatonin MT2 and serotonin 5-HT2C receptor heteromers in mouse brain."xsd:string |
http://purl.uniprot.org/citations/33156577 | http://purl.uniprot.org/core/volume | "35"xsd:string |
http://purl.uniprot.org/citations/33156577 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/33156577 |
http://purl.uniprot.org/citations/33156577 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/33156577 |
http://purl.uniprot.org/uniprot/#_B2RUD4-mappedCitation-33156577 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/33156577 |
http://purl.uniprot.org/uniprot/#_Q8BZI5-mappedCitation-33156577 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/33156577 |
http://purl.uniprot.org/uniprot/#_P34968-mappedCitation-33156577 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/33156577 |
http://purl.uniprot.org/uniprot/#_P70329-mappedCitation-33156577 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/33156577 |
http://purl.uniprot.org/uniprot/#_Q3SXF8-mappedCitation-33156577 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/33156577 |
http://purl.uniprot.org/uniprot/#_Q8CIQ6-mappedCitation-33156577 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/33156577 |
http://purl.uniprot.org/uniprot/#_Q8BUB1-mappedCitation-33156577 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/33156577 |