ArticleBioorganic & medicinal chemistry letters2014
Evaluation of structural effects on 5-HT(2A) receptor antagonism by aporphines: identification of a new aporphine with 5-HT(2A) antagonist activity.
Article in Bioorganic & medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 21 citations in OpenAlex.
- Regioselective Synthesis of 9‑ACS omega · 2026Article
- Synthesis and evaluation of aporphinoid 5-HTBioorganic & medicinal chemistry letters · 2025Article
- Total Synthesis of Aporphine Alkaloids via Photocatalytic Oxidative Phenol Coupling and Biological Evaluation at the Serotonin 5-HTJournal of medicinal chemistry · 2025Article
- Biological Potential of Oxoglaucine in Medicine for the Treatment of Human Disorders: An Update on Pharmacological Activities and Related Molecular Mechanism.Recent advances in anti-infective drug discovery · 2025Review
- Identification of C10 nitrogen-containing aporphines with dopamine DBioorganic & medicinal chemistry letters · 2020Article
- STarFish: A Stacked Ensemble Target Fishing Approach and its Application to Natural Products.Journal of chemical information and modeling · 2019Article
- Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HTMedChemComm · 2018Article
- Pharmacological profiling an abundantly expressed schistosome serotonergic GPCR identifies nuciferine as a potent antagonist.International journal for parasitology. Drugs and drug resistance · 2016Article
- Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.Bioorganic & medicinal chemistry letters · 2015Article
- C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.Bioorganic & medicinal chemistry letters · 2015Article
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
A set of aporphine analogs related to nantenine was evaluated for antagonist activity at 5-HT2A and α1A adrenergic receptors. With regards to 5-HT2A receptor antagonism, a C2 allyl group is detrimental to activity. The chiral center of nantenine is not important for 5-HT2A antagonist activity, however the N6 nitrogen atom is a critical feature for 5-HT2A antagonism. Compound 12b was the most potent 5-HT2A aporphine antagonist identified in this study and has similar potency to previously identified aporphine antagonists 2 and 3. The ring A and N6 modifications examined were detrimental to α1A antagonism. A slight eutomeric preference for the R enantiomer of nantenine was observed in relation to α1A antagonism.
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