Delay-Goyet P, Kayser V, Zajac J M, Guilbaud G, Besson J M, Roques B P
Département de Chimie Organique, U 266 I.N.S.E.R.M., UA 498 C.N.R.S., U.E.R. des Sciences Pharmaceutiques et Biologiques, Paris, France.
Neuropharmacology. 1989 Dec;28(12):1341-8. doi: 10.1016/0028-3908(89)90008-7.
The possible changes in neutral endopeptidase EC 3.4.24.11 ("enkephalinase", NEP), mu and delta opioid binding sites, were investigated using in vitro quantitative radioautography in various regions of the central nervous system of the Freund's adjuvant-induced arthritic rat, a model of chronic pain. Enkephalinase was labeled by a specific tritiated inhibitor, [3H]N-[(2RS)-3-hydroxyaminocarbonyl-2-benzyl-1-oxopropyl]glycine ([3H]HACBO-Gly), while mu and delta opioid binding sites were selectively labelled with [3H]Tyr-D-Ala-Gly-(Me)Phe-Gly-ol ([3H]DAGO) and [3H]Tyr-D-Thr-Gly-Phe-Leu-Thr ([3H]DTLFT), respectively. As compared to controls, no significant modifications were found in NEP, mu or delta binding sites at both supraspinal and spinal levels of arthritic rats. These results suggest that the enhanced efficiency of exogenous opioids or endogenous enkephalins, reported to occur in this model of chronic inflammatory pain, are not directly related to changes in mu and delta opioid binding sites or steady state levels of NEP.
利用体外定量放射自显影技术，在弗氏完全佐剂诱导的关节炎大鼠（一种慢性疼痛模型）的中枢神经系统各个区域，研究中性内肽酶EC 3.4.24.11（“脑啡肽酶”，NEP）、μ和δ阿片样物质结合位点可能发生的变化。脑啡肽酶用一种特异性氚标记抑制剂[3H]N-[(2RS)-3-羟基氨基羰基-2-苄基-1-氧代丙基]甘氨酸（[3H]HACBO-Gly）标记，而μ和δ阿片样物质结合位点分别用[3H]酪氨酸-D-丙氨酸-甘氨酸-（甲基）苯丙氨酸-甘醇（[3H]DAGO）和[3H]酪氨酸-D-苏氨酸-甘氨酸-苯丙氨酸-亮氨酸-苏氨酸（[3H]DTLFT）选择性标记。与对照组相比，在关节炎大鼠的脊髓上和脊髓水平，NEP、μ或δ结合位点均未发现明显改变。这些结果表明，据报道在这种慢性炎症性疼痛模型中发生的外源性阿片类药物或内源性脑啡肽效率增强，与μ和δ阿片样物质结合位点的变化或NEP的稳态水平没有直接关系。
