861445-47-8Relevant articles and documents
Structure-activity relationships of novel endomorphin-2 analogues with N-O turns induced by α-aminoxy acids
Wei, Jie,Shao, Xuan,Gong, Maozhen,Zhu, Beibei,Cui, Yuxin,Gao, Yanfeng,Wang, Rui
, p. 2986 - 2989 (2007/10/03)
Endomorphin-2 (H-Tyr-Pro-Phe-Phe-NH2, EM-2) is a putative endogenous μ-opioid receptor ligand. To study the structure-activity relationship against its receptor, we introduced N-O turns into EM-2 and got the analogues with potent affinities for μ-opioid receptor. Our results indicated that N-O turn structures at the Pro2-aminoxy-Phe 3 position of EM-2 analogues played important roles for their affinities. These novel analogues with N-O turns provided a new approach to develop potent analgesics related to EM-2.