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Novel Aza-analogous Ergoline Derived Scaffolds as Potent Serotonin 5‑HT6 and Dopamine D2 Receptor Ligands.

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journal contribution
posted on 10.07.2014, 00:00 by Niels Krogsgaard-Larsen, Anders A. Jensen, Tenna J. Schrøder, Claus. T. Christoffersen, Jan Kehler
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.