Glasel J A, Bradbury W M, Venn R F, Reese J H, Cooper J R
Life Sci. 1984 Jan 23;34(4):345-51. doi: 10.1016/0024-3205(84)90622-2.
Binding of 3H-etorphine and 3H-D-Ala2-D-Leu5-enkephalin to opiate receptors in synaptosomal and microsomal fractions prepared from guinea pig ileum homogenates has been studied. It is found that the dissociation constants for etorphine from all fractions are the same. The binding capacity for etorphine for the purified synaptosomal fraction is greater than for other fractions by a factor of 5. For the enkephalin derivative binding to the microsomal fraction the dissociation constant is greater than for etorphine while the binding capacity is a factor of 3 lower. These results are in contrast to the case for binding to central nervous system subcellular fractions.
对从豚鼠回肠匀浆制备的突触体和微粒体部分中3H-埃托啡和3H-D-丙氨酸2-D-亮氨酸5-脑啡肽与阿片受体的结合进行了研究。发现埃托啡从所有部分的解离常数相同。纯化的突触体部分对埃托啡的结合能力比其他部分大5倍。对于脑啡肽衍生物与微粒体部分的结合,解离常数大于埃托啡,而结合能力低3倍。这些结果与结合到中枢神经系统亚细胞部分的情况相反。