Durieux C, Pham H, Charpentier B, Roques B P
Département de Chime Organique, U 266 INSERM, UA 498 CNRS, Faculté de Pharmacie, Paris, France.
Biochem Biophys Res Commun. 1988 Aug 15;154(3):1301-7. doi: 10.1016/0006-291x(88)90281-1.
The properties of high affinity CCK8 binding sites of guinea-pig and rat brain cortex were compared using [3H]pCCK8. Large differences were observed, with the KD value being significantly higher in the rat (KD = 1.25 nM) than in guinea-pig brain (KD = 0.18 nM). Both sites exhibited different specificities for various CCK8 analogues, the selectivity factors KI rat/KI guinea-pig varied from 0.9 for CCK4 to 64 for cyclic CCK8-related compounds. Significant differences in the inhibition of [3H]pCCK8 binding by monovalent and nucleotides cations were also observed. These results could be explained by a difference in receptor environment or by a species difference in the proportion of CCK8 receptor-subtypes.
使用[3H]pCCK8比较了豚鼠和大鼠脑皮质高亲和力CCK8结合位点的特性。观察到了很大差异，大鼠的KD值（KD = 1.25 nM）显著高于豚鼠脑（KD = 0.18 nM）。两个位点对各种CCK8类似物表现出不同的特异性，选择性因子KI大鼠/KI豚鼠从CCK4的0.9到环CCK8相关化合物的64不等。还观察到单价和核苷酸阳离子对[3H]pCCK8结合抑制的显著差异。这些结果可以通过受体环境的差异或CCK8受体亚型比例的物种差异来解释。
