| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370513 | Bioorganic & Medicinal Chemistry Letters | 2015 | 4 Pages |
Abstract
A group of aporphine alkaloids related to (±)-nantenine (1) and bearing a C4 phenyl and various C1 or N-substituents, was synthesized and evaluated for affinity to h5-HT receptors. In general, unlike nantenine, the analogs lack affinity for the h5-HT2A receptor and other 5-HT receptors but bind selectively to the h5-HT2B receptor. With regards to 5-HT2B affinity, there appears to be a low tolerance for bulky C1 or N-substituents when the C4 phenyl moiety is present. Compound 5a had the highest 5-HT2B affinity of the compounds tested, was found to be an antagonist and is selective vs other CNS receptors.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Nirav Kapadia, Wayne W. Harding,