1295650-35-9Relevant academic research and scientific papers
Novel potent and selective θ ligands: Evaluation of their agonist and antagonist properties
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.,Ronsisvalle, Giuseppe
, p. 3669 - 3673 (2011/06/28)
Novel enantiomers and diastereoisomers structurally related to θ ligand (+)-MR200 were synthesized to improve θ1/θ 2 subtype selectivity. The selective θ1 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 θ2 ligand (-)-9 displayed agonist properties in an in vitro isolated organ bath assay and antiproliferative effects on LNCaP and PC3 prostate cancer cell lines.
