Kotzyba-Hibert F, Lagenbuch-Cachat J, Jaganathen J, Goeldner M, Hirth C
FEBS Lett. 1985 Mar 25;182(2):297-301. doi: 10.1016/0014-5793(85)80319-7.
Several aryldiazonium salts are described as irreversible blockers of the phencyclidine binding site of the nicotinic cholinergic receptor. A partial hydrophobic character increases the affinity of these salts for the phencyclidine binding site. Photoaffinity labelling with a tritiated diazonium salt in the presence of either carbamylcholine or alpha-bungarotoxin leads to incorporation of radioactivity into the 4 subunits of the receptor. Among these diazonium salts, an imidazole derivative is unique in that the photoinduced irreversible blocking in only effective when the receptor is in a desensitised state.
几种芳基重氮盐被描述为烟碱型胆碱能受体苯环利定结合位点的不可逆阻滞剂。部分疏水特性增加了这些盐对苯环利定结合位点的亲和力。在氨甲酰胆碱或α-银环蛇毒素存在的情况下，用氚标记的重氮盐进行光亲和标记会导致放射性掺入受体的4个亚基中。在这些重氮盐中，一种咪唑衍生物的独特之处在于，只有当受体处于脱敏状态时，光诱导的不可逆阻断才有效。
