Barabé J, Babiuk C, Regoli D
Can J Physiol Pharmacol. 1982 Dec;60(12):1551-5. doi: 10.1139/y82-229.
Binding studies of [3H]des-Arg9-BK have been performed on pieces of rabbit anterior mesenteric veins. Kinetic studies have permitted us to evaluate an affinity constant of 1.04 X 10(-7) M, which is not so different from the apparent affinity constant determined by bioassay (1.6 X 10(-7) M). Furthermore, inhibition of the binding of [3H]des-Arg9-BK with various kinins results in an order of potency of kinins very similar to that observed in the bioassay. Taken together, these results suggest that we are dealing with binding sites which might be the same as those subserving the biological action of des-Arg9-BK (pharmacological receptors). The preincubation of tissues in Krebs' solution brings about an increase of the specific binding from 0.06 pmol/mg of wet weight at time 0 to 0.75 pmol after 24 h; cycloheximide inhibits this increase for at least 6 h. Veins taken from animals treated with LPS, which have shown an increase in sensitivity compared with veins extracted from untreated animals, have a higher number of specific binding sites for [3H]des-Arg9-BK. The results support the hypothesis that the increased response of tissues to des-Arg9-BK is due to the de novo synthesis of receptors for kinins in some experimental and pathological conditions.
已对兔肠系膜前静脉片段进行了[3H]去-精氨酸9-缓激肽的结合研究。动力学研究使我们能够评估其亲和常数为1.04×10(-7) M，这与通过生物测定法确定的表观亲和常数（1.6×10(-7) M）并无太大差异。此外，用各种激肽抑制[3H]去-精氨酸9-缓激肽的结合，所得到的激肽效力顺序与生物测定中观察到的非常相似。综上所述，这些结果表明我们所研究的结合位点可能与那些介导去-精氨酸9-缓激肽生物作用的位点（药理受体）相同。将组织在Krebs溶液中预孵育，会使特异性结合从时间0时的0.06 pmol/毫克湿重增加到24小时后的0.75 pmol；环己酰亚胺至少在6小时内抑制这种增加。从用脂多糖处理过的动物身上取出的静脉，与从未经处理的动物身上取出的静脉相比，对去-精氨酸9-缓激肽的敏感性有所增加，其对[3H]去-精氨酸9-缓激肽的特异性结合位点数量更多。这些结果支持了以下假设：在某些实验和病理条件下，组织对去-精氨酸9-缓激肽反应性增加是由于激肽受体的重新合成。
