Mori H, Shiba K, Matsuda H, Tsuji S, Hisada K
Radioisotope Centre, School of Medicine, Kanazawa University, Japan.
Nucl Med Commun. 1990 Apr;11(4):327-31. doi: 10.1097/00006231-199004000-00012.
N-isopropyl-p-[125I]iodoamphetamine (125I-IMP) binding to crude synaptosomal membranes of rat brain was saturable and pharmacologically displacable. Scatchard analysis of binding data revealed an apparent dissociation constant, KD of 56.2 +/- 5.2 microM, and the estimated maximum number of binding sites, Bmax of 7.5 +/- 1.1 nmoles mg-1 protein; and competition studies demonstrated structure activity relationships among structural analogues of arylalkylamines. These findings suggest that the retention mechanism of IMP in the brain is probably associated with saturable binding of IMP to extreme high-density, relatively low-affinity binding sites rather than any of the well-known amine receptors.
N-异丙基-p-[¹²⁵I]碘安非他明（¹²⁵I-IMP）与大鼠脑粗突触体膜的结合具有饱和性且可被药理学方法置换。对结合数据进行Scatchard分析显示，其表观解离常数KD为56.2±5.2微摩尔，估计的最大结合位点数Bmax为7.5±1.1纳摩尔/毫克蛋白质；竞争研究表明芳基烷基胺结构类似物之间存在构效关系。这些发现提示，IMP在脑中的潴留机制可能与IMP与极高密度、相对低亲和力结合位点的饱和性结合有关，而非与任何已知的胺受体有关。
