Bowen W D, Pert C B, Pert A
Life Sci. 1982;31(16-17):1679-82. doi: 10.1016/0024-3205(82)90184-9.
We have investigated the effect of nigral 6-hydroxydopamine (6-OHDA) lesions on binding of the mu receptor ligand dihydromorphine (DHM) and the delta receptor ligand [D-Ala2, D-Leu5]-enkephalin (DADLE) to sections of rat striatum under conditions which yield mu-like and delta-like ligand selectivities at discrete receptor patches (Type 1 receptor). 3H-DHM binding was decreased 43% while 3H-DADLE was decreased 22%. However, when the contribution of diffuse binding (Type 2) which is not affected by 6-OHDA is subtracted from the patch, the decrease is approximately 49% for both ligands. These data support the hypothesis that the Type 1 receptor of striatal patches is a conformationally malleable receptor entity which can exist in states having high affinities for various classes of opiate ligands.
我们研究了黑质6-羟基多巴胺（6-OHDA）损伤对μ受体配体二氢吗啡（DHM）和δ受体配体[D-Ala2，D-Leu5]-脑啡肽（DADLE）与大鼠纹状体切片结合的影响，实验条件是在离散的受体斑块（1型受体）处产生类似μ和类似δ的配体选择性。3H-DHM结合减少了43%，而3H-DADLE减少了22%。然而，当从斑块中减去不受6-OHDA影响的弥散结合（2型）的贡献时，两种配体的减少约为49%。这些数据支持这样的假设，即纹状体斑块的1型受体是一种构象可塑性受体实体，它可以以对各种阿片类配体具有高亲和力的状态存在。
