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Conformational analysis and μ-opioid receptor affinity of short peptides, endomorphin models in a low polarity solvent

机译:低极性溶剂中短肽,内啡肽模型的构象分析和μ阿片受体亲和力

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摘要

Peptide carbamates containing the sequence H-Pro-Trp-PheNH_2 showed in CDCl_3 restricted conformations stabilized by the presence of a γ-turn. To test the reliability of the peptides as endomorphin conformational models, we measured the affinities for μ-receptors labelled with [~3H]-DAMGO. In particular, Cbz-Pro-Trp-PheNH_2 displayed a nanomolar affinity.
机译:含有序列H-Pro-Trp-PheNH_2的氨基甲酸酯肽在CDCl_3限制的构象中显示,可通过γ转角稳定化。为了测试肽作为内啡肽构象模型的可靠性,我们测量了用[〜3H] -DAMGO标记的μ受体的亲和力。特别地,Cbz-Pro-Trp-PheNH_2显示出纳摩尔亲和力。

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