Slaninova J, Knapp R J, Wu J J, Fang S N, Kramer T, Burks T F, Hruby V J, Yamamura H I
Department of Pharmacology, University of Arizona Health Science Center, Tucson 85724.
Eur J Pharmacol. 1991 Jul 23;200(1):195-8. doi: 10.1016/0014-2999(91)90688-m.
Four analogues of cholecystokinin (CCK) octapeptide having analgesic activity after i.c.v. administration and high affinity for CCK-B receptors were studied for their ability to displace specific ligands, [3H]D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2. [3H][D-Pen2, 4'-Cl-Phe4,D-Pen5]enkephalin and [3H]U-69,593, for mu-, delta- and kappa-opioid receptors, respectively. None of the analogues tested have high affinity for either mu- or kappa-receptors (IC50 values greater than 0.7 microM), but their IC50 values for delta-receptors range from 29 to 1023 nM. The results suggest a relationship between the ligand requirements of CCK-B and delta-opioid receptors which further implies a possible structural relationship between these receptors.
研究了四种胆囊收缩素（CCK）八肽类似物，它们经脑室内给药后具有镇痛活性，且对CCK-B受体具有高亲和力，研究其置换特异性配体[3H]D-苯丙氨酸-半胱氨酸-酪氨酸-D-色氨酸-鸟氨酸-苏氨酸-青霉胺-苏氨酸-氨基的能力。[3H][D-青霉胺2，4'-氯苯丙氨酸4，D-青霉胺5]脑啡肽和[3H]U-69,593，分别用于μ-、δ-和κ-阿片受体。所测试的类似物对μ-或κ-受体均无高亲和力（IC50值大于0.7μM），但它们对δ-受体的IC50值范围为29至1023 nM。结果表明CCK-B和δ-阿片受体的配体需求之间存在关系，这进一步暗示了这些受体之间可能存在结构关系。
