Novel Aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands

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dc.contributor.authorKrogsgaard-Larsen, N.
dc.contributor.authorJensen, A.
dc.contributor.authorSchrøder, T.
dc.contributor.authorChristoffersen, C.
dc.contributor.authorKehler, J.
dc.date.issued2014
dc.descriptionNiels Krogsgaard-Larsen, Anders A. Jensen, Tenna J. Schroder, Claus. T. Christoffersen and Jan Kehler
dc.description.abstractBy introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar receptor binding affinities for the dopamine D₂ and serotonin 5-HT₆ receptor subtype, respectively. While the 5-HT₆ ligands were antagonists, the D₂ ligands displayed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity. These structures could potentially be interesting for treatment of neurological diseases such as schizophrenia, Parkinson's disease, and cognitive deficits.
dc.description.statementofresponsibilityNiels Krogsgaard-Larsen, Anders A. Jensen, Tenna J. Schrøder, Claus. T. Christoffersen and Jan Kehler
dc.identifier.citationJournal of Medicinal Chemistry, 2014; 57(13):5823-5828
dc.identifier.doi10.1021/jm5003759
dc.identifier.issn0022-2623
dc.identifier.issn1520-4804
dc.identifier.urihttp://hdl.handle.net/2440/101916
dc.language.isoen
dc.publisherAmerican Chemical Society
dc.source.urihttps://doi.org/10.1021/jm5003759
dc.subjectErgolines
dc.titleNovel Aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands
dc.title.alternativeNovel Aza-analogous ergoline derived scaffolds as potent serotonin 5-HT(6) and dopamine D(2) receptor ligands
dc.typeJournal article
pubs.publication-statusPublished

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