Aryldiazonium salts as photoaffinity labels of the nicotinic acetylcholine receptor PCP binding site |
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Authors: | F Kotzyba-Hibert J Lagenbuch-Cachat J Jaganathen M Goeldner C Hirth |
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Affiliation: | Centre de Neurochimie, 5 rue Blaise Pascal, 67084 Strasbourg Cedex, France |
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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 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. |
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