ArticleBioorganic & medicinal chemistry letters2015
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.
Article in Bioorganic & medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed, 12 citations in OpenAlex.
- Regioselective Synthesis of 9‑ACS omega · 2026Article
- Total Synthesis of Aporphine Alkaloids via Photocatalytic Oxidative Phenol Coupling and Biological Evaluation at the Serotonin 5-HTJournal of medicinal chemistry · 2025Article
- Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Structure-activity profiling of alkaloid natural product pharmacophores against a Schistosoma serotonin receptor.International journal for parasitology. Drugs and drug resistance · 2018Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
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-HT(2A) receptor and other 5-HT receptors but bind selectively to the h5-HT(2B) receptor. With regards to 5-HT(2B) 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-HT(2B) affinity of the compounds tested, was found to be an antagonist and is selective vs other CNS receptors.
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