Weissman B A, Elson H F, Kaplan D, Newman A H
Department of Applied Biochemistry, Walter Reed Army Institute of Research, Washington, DC 20307.
Eur J Pharmacol. 1990 Oct 23;187(3):369-75. doi: 10.1016/0014-2999(90)90364-c.
Employing [3H]Ro5-4864 as a radioligand, the existence of peripheral benzodiazepine binding sites in rat hind limb skeletal fibroblasts was explored. Saturable, high affinity binding of this ligand is described for fibroblasts and cell membrane preparations, demonstrating a pharmacological profile characteristic for such receptors. The binding of [3H]Ro5-4864 exhibited higher affinity and density in fibroblasts compared to membrane preparations. A quaternaryamine derivative of PK 11195 showed a similar potency as a displacer of [3H]Ro5-4864 in both preparations. The data suggest that peripheral benzodiazepine receptors are present in the plasma membrane of primary mammalian fibroblasts.
以[3H]Ro5-4864作为放射性配体，研究了大鼠后肢骨骼肌成纤维细胞中周围型苯二氮䓬结合位点的存在情况。描述了该配体在成纤维细胞和细胞膜制剂中的饱和、高亲和力结合，证明了此类受体具有药理学特征。与细胞膜制剂相比，[3H]Ro5-4864在成纤维细胞中的结合表现出更高的亲和力和密度。PK 11195的季铵衍生物在两种制剂中作为[3H]Ro5-4864的置换剂显示出相似的效力。数据表明，周围型苯二氮䓬受体存在于原代哺乳动物成纤维细胞的质膜中。
