Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist.
Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist.
复制标题
鉴定 J-113397 的非手性类似物为有效的伤害感受肽/孤啡肽 FQ 受体拮抗剂。
DOI：
10.1016/j.bmc.2005.08.049
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发表时间：
2006
期刊：
影响因子：
--
通讯作者：
Salvadori,Severo
中科院分区：
文献类型：
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作者：
Trapella,Claudio;Guerrini,Remo;Piccagli,Laura;Calo',Girolamo;Carra',Giacomo;Spagnolo,Barbara;Rubini,Samantha;Fanton,Giulia;Hebbes,Christopher;McDonald,John;Lambert,DavidG;Regoli,Domenico;Salvadori,Severo
To date, J-113397 represents the most potent and selective non peptide NOP receptor antagonist widely used in pharmacological studies. However, the synthesis, purification, and enantiomer separation of this molecule, which contains two chiral centers, is rather difficult and low-yielding. Here, we synthesized and tested a series of simplified J-113397 analogues to investigate the importance of the stereochemistry and the influence of the substituents at position 3 of the piperidine nucleus and on the nitrogen atom of the benzimidazolidinone nucleus. The compound coded as Trap-101, an achiral analogue of J-113397, combines a pharmacological profile similar to that of the parent compound with a practical, high-yielding preparation.
