ChemInform Abstract: Serotonergic and Dopaminergic Activities of Rigidified (R)‐Aporphine Derivatives.

Abstract

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Characterization of the 5-HT7Receptor. Determination of the Pharmacophore for 5-HT7Receptor Agonism and CoMFA-Based Modeling of the Agonist Binding Site

“…The most recently discovered member of the serotonin receptor family, the 5-HT 7 receptor, has received great interest over the past decade. − Four splice variants have been identified, with main differences at the C-termini, suggesting different efficiencies in G-protein coupling. However, all isoforms seem to be positively coupled to adenylyl cyclase. − Despite the fact that several series of antagonists with moderate to high affinity and selectivity for the 5-HT 7 receptor have been synthesized in the recent years, − its (patho-) physiological role still remains unclear. It has been hypothesized to be involved in the regulation of circadian rhythms, − depression, , and smooth muscle relaxation, , but this awaits further elucidation with the use of known and newly synthesized selective ligands (both agonists and antagonists) and relevant in vivo models.…”

Discovery of Aporphine Analogues as Potential Antiplatelet and Antioxidant Agents: Design, Synthesis, Structure–Activity Relationships, Biological Evaluations, and in silico Molecular Docking Studies

“…For example, natural/synthetic aporphines have been identified as antimicrobial, antiviral,, and acetyl cholinesterase inhibitors; antimalarial agents;, central nervous system receptor ligands; anti‐Alzheimer agents;–,, and potent dopamine D1/D2 agonists . Additionally, their characteristic tetracyclic motif with different levels of oxidation on both aromatic rings results in a diverse range of interesting biological activities, including antimalarial, serotonergic, anticancer, vasorelaxing and cytotoxic activities . Moreover, literature reports reveal that natural and semisynthetic aporphines 3 – 14 show excellent antioxidant and antiplatelet activities (Figure ).…”