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Your search keyword '"Ronsisvalle, Simone"' showing total 7 results
Start Over Author "Ronsisvalle, Simone" Journal journal of medicinal chemistry
7 results on '"Ronsisvalle, Simone"'

1. Novel Potent and Selective σ Ligands: Evaluation of Their Agonist and Antagonist Properties

Author

Marrazzo, Agostino, Cobos, Enrique J., Parenti, Carmela, Aricò, Giuseppina, Marrazzo, Giuseppina, Ronsisvalle, Simone, Pasquinucci, Lorella, Prezzavento, Orazio, Colabufo, Nicola A., Contino, Marialessandra, González, Luis G., Scoto, Giovanna M., and Ronsisvalle, Giuseppe

Abstract

Novel enantiomers and diastereoisomers structurally related to σ ligand (+)-MR200 were synthesized to improve σ1/σ2subtype selectivity. The selective σ1ligand (–)-8showed an antagonist profile determined by phenytoin differential modulation of binding affinity in vitro, confirmed in vivo by an increase of κ opioid analgesia. The σ2ligand (–)-9displayed agonist properties in an in vitro isolated organ bath assay and antiproliferative effects on LNCaP and PC3 prostate cancer cell lines.

Published
2024
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2. Synthesis and Resolution of cis-(±)-Methyl (1R,2S/1S,2R)-2-[(4-Hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [(±)-PPCC)]: New σ Receptor Ligands with Neuroprotective Effect

Author

Prezzavento, Orazio, Campisi, Agata, Parenti, Carmela, Ronsisvalle, Simone, Aricò, Giuseppina, Arena, Emanuela, Pistolozzi, Marco, Scoto, Giovanna M., Bertucci, Carlo, Vanella, Angelo, and Ronsisvalle, Giuseppe

Abstract

The enantiomers of cis-(±)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [1, (±)-PPCC], a selective σ ligand, were synthesized. The (+)- and (−)-enantiomers bind predominantly to σ1receptors and have a reduced σ2affinity. Both individually restore the astroglial oxidative status modified by glutamate, counteracting also transglutaminase-2 overexpression. They exhibited in vivo anti-opioid effects on κ opioid (KOP) receptor-mediated analgesia. Our findings demonstrate that the enantiomers display mainly σ1agonist activity and that they have neuroprotective effects.

Published
2024
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3. Synthesis and Biological Characterization of 3-Substituted-1H-indoles as Ligands of GluN2B-Containing N-Methyl-d-aspartate Receptors

Author

Gitto, Rosaria, primary, De Luca, Laura, additional, Ferro, Stefania, additional, Buemi, Maria Rosa, additional, Russo, Emilio, additional, De Sarro, Giovambattista, additional, Costa, Lara, additional, Ciranna, Lucia, additional, Prezzavento, Orazio, additional, Arena, Emanuela, additional, Ronsisvalle, Simone, additional, Bruno, Giuseppe, additional, and Chimirri, Alba, additional

Published
2011
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4. Novel Potent and Selective σ Ligands: Evaluation of Their Agonist and Antagonist Properties

Author

Marrazzo, Agostino, primary, Cobos, Enrique J., additional, Parenti, Carmela, additional, Aricò, Giuseppina, additional, Marrazzo, Giuseppina, additional, Ronsisvalle, Simone, additional, Pasquinucci, Lorella, additional, Prezzavento, Orazio, additional, Colabufo, Nicola A., additional, Contino, Marialessandra, additional, González, Luis G., additional, Scoto, Giovanna M., additional, and Ronsisvalle, Giuseppe, additional

Published
2011
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5. Synthesis and Resolution of cis-(±)-Methyl (1R,2S/1S,2R)-2-[(4-Hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [(±)-PPCC)]: New σ Receptor Ligands with Neuroprotective Effect

Author

Prezzavento, Orazio, primary, Campisi, Agata, additional, Parenti, Carmela, additional, Ronsisvalle, Simone, additional, Aricò, Giuseppina, additional, Arena, Emanuela, additional, Pistolozzi, Marco, additional, Scoto, Giovanna M., additional, Bertucci, Carlo, additional, Vanella, Angelo, additional, and Ronsisvalle, Giuseppe, additional

Published
2010
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6. Novel Sigma Receptor Ligands: Synthesis and Biological Profile

Author

Prezzavento, Orazio, primary, Campisi, Agata, additional, Ronsisvalle, Simone, additional, Li Volti, Giovanni, additional, Marrazzo, Agostino, additional, Bramanti, Vincenzo, additional, Cannavò, Giuseppe, additional, Vanella, Luca, additional, Cagnotto, Alfredo, additional, Mennini, Tiziana, additional, Ientile, Riccardo, additional, and Ronsisvalle, Giuseppe, additional

Published
2007
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7. Synthesis and resolution of cis-(+/-)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [(+/-)-PPCC)]: new sigma receptor ligands with neuroprotective effect.

Author

Prezzavento O, Campisi A, Parenti C, Ronsisvalle S, Aricò G, Arena E, Pistolozzi M, Scoto GM, Bertucci C, Vanella A, and Ronsisvalle G

Subjects
3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer pharmacology, Analgesics, Non-Narcotic pharmacology, Animals, Astrocytes drug effects, Astrocytes metabolism, Cells, Cultured, Cyclopropanes chemistry, Cyclopropanes pharmacology, Drug Interactions, GTP-Binding Proteins biosynthesis, Glutamic Acid pharmacology, Glutathione metabolism, Ibogaine pharmacology, Ligands, Neuroprotective Agents chemistry, Neuroprotective Agents pharmacology, Oxidative Stress, Pentazocine pharmacology, Piperidines chemistry, Piperidines pharmacology, Protein Glutamine gamma Glutamyltransferase 2, Rats, Reactive Oxygen Species metabolism, Receptors, Opioid, kappa agonists, Receptors, sigma metabolism, Stereoisomerism, Structure-Activity Relationship, Transglutaminases biosynthesis, Cyclopropanes chemical synthesis, Neuroprotective Agents chemical synthesis, Piperidines chemical synthesis, Receptors, sigma agonists
Abstract

The enantiomers of cis-(+/-)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [1, (+/-)-PPCC], a selective sigma ligand, were synthesized. The (+)- and (-)-enantiomers bind predominantly to sigma(1) receptors and have a reduced sigma(2) affinity. Both individually restore the astroglial oxidative status modified by glutamate, counteracting also transglutaminase-2 overexpression. They exhibited in vivo anti-opioid effects on kappa opioid (KOP) receptor-mediated analgesia. Our findings demonstrate that the enantiomers display mainly sigma(1) agonist activity and that they have neuroprotective effects.

Published
2010
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