Aryldiazonium salts as photoaffinity labels of the nicotinic acetylcholine receptor PCP binding site
- 25 March 1985
- journal article
- Published by Wiley in FEBS Letters
- Vol. 182 (2) , 297-301
- https://doi.org/10.1016/0014-5793(85)80319-7
Abstract
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.Keywords
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