Haaseth R C, Zalewska T, Davis P, Yamamura H I, Porreca F, Hruby V J
Department of Chemistry, University of Arizona, Tucson, USA.
J Pept Res. 1997 Sep;50(3):171-7. doi: 10.1111/j.1399-3011.1997.tb01182.x.
Several para-substituted Phe4 analogues of the delta 1-selective antagonist [L-Ala3]DPDPE (DPADPE) were prepared and evaluated for their brain-binding and in vitro pharmacological effects. Unlike the p-haloPhe4 analogues of DPDPE and the deltorphins, similar analogues of DPADPE with electron-withdrawing groups substituted at the para-position of the Phe4 aromatic ring did not all have increased potency and selectivity for delta opioid receptors, but all retained high potency and selectivity for delta opioid receptors greater than DPDPE.
制备了δ1选择性拮抗剂[L-Ala3]DPDPE（DPADPE）的几种对-取代苯丙氨酸4类似物，并评估了它们的脑结合和体外药理作用。与DPDPE和强啡肽的对-卤代苯丙氨酸4类似物不同，在苯丙氨酸4芳香环的对位取代有吸电子基团的DPADPE类似物并非都对δ阿片受体具有增强的效力和选择性，但所有这些类似物对δ阿片受体均保持了高于DPDPE的高效力和选择性。
