Novel Aza-analogous Ergoline Derived Scaffolds as
Potent Serotonin 5‑HT<sub>6</sub> and Dopamine D<sub>2</sub> Receptor Ligands.
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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 D<sub>2</sub> and serotonin 5-HT<sub>6</sub> receptor subtype, respectively. While
the 5-HT<sub>6</sub> ligands were antagonists, the D<sub>2</sub> 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