Rinaldi F, Lin M, Shapiro M J, Petersheim M
Chemistry Department, Seton Hall University, South Orange, New Jersey 07079, USA.
Biophys J. 1997 Dec;73(6):3337-48. doi: 10.1016/S0006-3495(97)78358-9.
D-Penicillamine(2,5)-enkephalin (DPDPE) is a potent opioid peptide that exhibits a high selectivity for the delta-opiate receptors. This zwitterionic peptide has been shown, by pulsed-field gradient 1H NMR diffusion studies, to have significant affinity for a zwitterionic phospholipid bilayer. The bilayer lipid is in the form of micelles composed of dihexanoylphosphatidylcholine (DHPC) and dimyristoylphosphatidylcholine (DMPC) mixtures, where the DMPC forms the bilayer structure. At high lipid concentration (25% w/w) these micelles orient in the magnetic field of an NMR spectrometer. The resulting 1H-13C dipolar couplings and chemical shift changes in the natural abundance 13C resonances for the Tyr and Phe aromatic rings were used to characterize the orientations in the bilayer micelles of these two key pharmacophores.
D-青霉胺（2,5）-脑啡肽（DPDPE）是一种强效阿片肽，对δ-阿片受体具有高度选择性。通过脉冲场梯度1H NMR扩散研究表明，这种两性离子肽对两性离子磷脂双层具有显著亲和力。双层脂质呈由二己酰磷脂酰胆碱（DHPC）和二肉豆蔻酰磷脂酰胆碱（DMPC）混合物组成的胶束形式，其中DMPC形成双层结构。在高脂质浓度（25%w/w）下，这些胶束在NMR光谱仪的磁场中取向。利用所得的Tyr和Phe芳香环的1H-13C偶极耦合以及天然丰度13C共振中的化学位移变化，来表征这两个关键药效基团在双层胶束中的取向。
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