Aryldiazonium salts as photoaffinity labels of the nicotinic acetylcholine receptor PCP binding site

FEBS Letters

Hirth, Christian¹  Goeldner, Maurice¹  Kotzyba-Hibert, Florence¹  Jaganathen, Jensen¹  Langenbuch-Cachat, Jocelyne¹ 

[1] Centre de Neurochimie, 5 rue Blaise Pascal, 67084 Strasbourg Cedex, France

关键词: Aryldiazonium salt;    Acetylcholine receptor;    Phencyclidine binding site;    Photoaffinity labelling;    Non-competitive blocker;    carb;    carbamylcholine;    α Bgtx;    α-bungarotoxin;    PCP;    phencyclidine;    NCB;    non-competitive blocker;    AcHR;    acetylcholine receptor;    DDF;    p-(N;    N-dimethylamino)benzenediazonium fluoroborate;   

DOI  :  10.1016/0014-5793(85)80319-7

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 α-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.

【 授权许可】

Unknown