Burstein S H, Audette C A, Charalambous A, Doyle S A, Guo Y, Hunter S A, Makriyannis A
Department of Biochemistry and Molecular Biology, University of Massachusetts Medical School, Worcester 01655.
Biochem Biophys Res Commun. 1991 Apr 15;176(1):492-7. doi: 10.1016/0006-291x(91)90951-3.
A novel [125I]-labelled photoaffinity ligand designed to detect cannabinoid binding sites has been used in mouse brain preparations and in cultured S49 mouse lymphoma cells. The ligand, 2-iodo-5'-azido-delta 8-THC, shows a high affinity for sites in both brain (Kd = 5.60 pM) and whole cell (Kd = 9.38 pM) systems. Photolabelling studies with brain samples revealed the existence of four ligand-protein adducts, of estimated molecular weights 85.5, 62.1, 30.0 and 25.5 kDa, that were diminished by prior exposure to 8 microM THC. A similar study with S49 cells gave adducts with apparent molecular weights of 62.1, 34.4, 16.9 and 13.5 kDa. The ligand produces a typical cannabinoid cataleptic response in mice suggesting that possibly one or more of the binding sites may be involved in some of the receptor mediated actions of THC.
一种设计用于检测大麻素结合位点的新型[125I]标记光亲和配体已用于小鼠脑组织和培养的S49小鼠淋巴瘤细胞。该配体2-碘-5'-叠氮基-δ8-四氢大麻酚在脑（Kd = 5.60 pM）和全细胞（Kd = 9.38 pM）系统中对位点均显示出高亲和力。对脑样本的光标记研究揭示了存在四种配体-蛋白质加合物，估计分子量分别为85.5、62.1、30.0和25.5 kDa，预先暴露于8 microM四氢大麻酚会使其减少。对S49细胞的类似研究得到了表观分子量为62.1、34.4、16.9和13.5 kDa的加合物。该配体在小鼠中产生典型的大麻素僵住反应，表明可能一个或多个结合位点可能参与了四氢大麻酚的一些受体介导的作用。
