Novel Aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands
Date
2014
Authors
Krogsgaard-Larsen, N.
Jensen, A.
Schrøder, T.
Christoffersen, C.
Kehler, J.
Editors
Advisors
Journal Title
Journal ISSN
Volume Title
Type:
Journal article
Citation
Journal of Medicinal Chemistry, 2014; 57(13):5823-5828
Statement of Responsibility
Niels Krogsgaard-Larsen, Anders A. Jensen, Tenna J. Schrøder, Claus. T. Christoffersen and Jan Kehler
Conference Name
Abstract
By 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.
School/Discipline
Dissertation Note
Provenance
Description
Niels Krogsgaard-Larsen, Anders A. Jensen, Tenna J. Schroder, Claus. T. Christoffersen and Jan Kehler