475150-69-7Relevant articles and documents
Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4′-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide
Trapella, Claudio,Fischetti, Carmela,Pela', Michela,Lazzari, Ilaria,Guerrini, Remo,Calo', Girolamo,Rizzi, Anna,Camarda, Valeria,Lambert, David G.,McDonald, John,Regoli, Domenico,Salvadori, Severo
experimental part, p. 5080 - 5095 (2009/12/24)
Twelve derivatives of the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4′-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide (Comp 24) were synthesized and tested in binding experiments performed on CHOsu
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity
Goto, Yasuhiro,Arai-Otsuki, Sachie,Tachibana, Yukari,Ichikawa, Daisuke,Ozaki, Satoshi,Takahashi, Hiroyuki,Iwasawa, Yoshikazu,Okamoto, Osamu,Okuda, Shoki,Ohta, Hisashi,Sagara, Takeshi
, p. 847 - 849 (2007/10/03)
A focused library approach identifying novel leads to develop a potent ORL1 antagonist is described. Beginning from a compound identified by random screening, an exploratory library that exhibited a diverse display of pharmacophores was designed. After evaluating ORL1 antagonistic activity, a highly focused library was designed based on 3D-pharmacophore similarity to known actives. A novel D-proline amide class was identified in this library and was found to possess potent ORL1 antagonistic activity.