对δ-阿片受体具有非凡效力和选择性的环脑啡肽类似物。
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.
作者信息
Hruby V J, Bartosz-Bechowski H, Davis P, Slaninova J, Zalewska T, Stropova D, Porreca F, Yamamura H I
机构信息
Department of Chemistry, University of Arizona, Tucson 85721, USA.
出版信息
J Med Chem. 1997 Nov 21;40(24):3957-62. doi: 10.1021/jm9704762.
Superpotent and highly delta-opioid receptor selective cyclic peptides of the general formula H-Tyr-c[D-Pen-Gly-Phe(p-X)-Pen]-Phe-OH (where X = hydrogen or halogen) have been synthesized. In the binding assays the most selective and most potent compound is the p-bromophenyl-alanine-4 analogue (IC50 value = 0.19 nM, selectivity ratio = 21,000 for delta vs mu). In the GPI and MVD bioassays the most selective and most potent analogue is the p-fluoro-substituted analogue Tyr-[D-Pen-Gly-Phe(p-F)-Pen]-Phe-OH. In the MVD assay it has an exceptionally low IC50 value of 0.016 nM and a delta vs mu selectivity ratio of 45,000.
已合成通式为H-Tyr-c[D-Pen-Gly-Phe(p-X)-Pen]-Phe-OH（其中X = 氢或卤素）的超高效且高度δ-阿片受体选择性环肽。在结合试验中，最具选择性和效力最强的化合物是对溴苯丙氨酸-4类似物（IC50值 = 0.19 nM，δ与μ的选择性比 = 21,000）。在GPI和MVD生物测定中，最具选择性和效力最强的类似物是对氟取代类似物Tyr-[D-Pen-Gly-Phe(p-F)-Pen]-Phe-OH。在MVD测定中，其IC50值极低，为0.016 nM，δ与μ的选择性比为45,000。
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