| Literature DB >> 21476493 |
Agostino Marrazzo1, Enrique J Cobos, Carmela Parenti, Giuseppina Aricò, Giuseppina Marrazzo, Simone Ronsisvalle, Lorella Pasquinucci, Orazio Prezzavento, Nicola A Colabufo, Marialessandra Contino, Luis G González, Giovanna M Scoto, Giuseppe Ronsisvalle.
Abstract
Novel enantiomers and diastereoisomers structurally related to σ ligand (+)-MR200 were synthesized to improve σ(1)/σ(2) subtype selectivity. The selective σ(1) ligand (-)-8 showed an antagonist profile determined by phenytoin differential modulation of binding affinity in vitro, confirmed in vivo by an increase of κ opioid analgesia. The σ(2) ligand (-)-9 displayed agonist properties in an in vitro isolated organ bath assay and antiproliferative effects on LNCaP and PC3 prostate cancer cell lines.Entities:
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Year: 2011 PMID： 21476493 DOI： 10.1021/jm200144j
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446