Zarbin M A, Innis R B, Wamsley J K, Snyder S H, Kuhar M J
J Neurosci. 1983 Apr;3(4):877-906. doi: 10.1523/JNEUROSCI.03-04-00877.1983.
Cholecystokinin (CCK) receptor binding sites have been localized by autoradiography in the guinea pig and rat central nervous system. [125I]CCK-triacontatriapeptide labeled the sites in brain slices with an observed association constant equal to 0.041 min-1 and a dissociation constant equal to 0.008 min-1. CCK-triacontatriapeptide (CCK-33) and the C-terminal octapeptide of CCK-33 (CCK-8) potently inhibited [125I]CCK-33 binding with Ki's of 2 nM, whereas desulfated CCK-8 (CCK8-ds) and the C-terminal tetrapeptide of CCK-33 (CCK-4) were much weaker. Receptors were concentrated in the olfactory bulb, in the superficial laminae of the primary olfactory cortex, in the deep laminae of the cerebral cortex, and in the pretectal area. Substantial numbers of sites were also found in the basal ganglia, in the amygdala, and in the hippocampal formation. [125I]CCK-33 binding sites appear to be located on fibers of the optic tract and probably on olfactory tract fibers as well. These results are discussed in terms of physiological functions associated with CCK, presynaptic receptors, and axonal flow of CCK receptors.
通过放射自显影法已将胆囊收缩素（CCK）受体结合位点定位在豚鼠和大鼠的中枢神经系统中。[125I]CCK-三十烷三肽标记脑切片中的位点，观察到的缔合常数等于0.041分钟-1，解离常数等于0.008分钟-1。CCK-三十烷三肽（CCK-33）和CCK-33的C末端八肽（CCK-8）能有效抑制[125I]CCK-33结合，其抑制常数（Ki）为2 nM，而硫酸化缺失的CCK-8（CCK8-ds）和CCK-33的C末端四肽（CCK-4）的抑制作用则弱得多。受体集中在嗅球、初级嗅觉皮层的浅层、大脑皮层的深层以及顶盖前区。在基底神经节、杏仁核和海马结构中也发现了大量的位点。[125I]CCK-33结合位点似乎位于视束纤维上，可能也位于嗅束纤维上。将根据与CCK、突触前受体和CCK受体轴浆运输相关的生理功能来讨论这些结果。
