title: Aryldiazonium salts as photoaffinity labels of the nicotinic acetylcholine receptor PCP binding site.
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.
mesh_terms: D000345:Affinity Labels / Q000378:metabolism; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D002038:Bungarotoxins / Q000494:pharmacology; D002217:Carbachol / Q000494:pharmacology; D003979:Diazonium Compounds / Q000378:metabolism* / Q000494:pharmacology; D004557:Electric Organ / Q000378:metabolism*; D010622:Phencyclidine / Q000378:metabolism*; D010777:Photochemistry; D011978:Receptors, Nicotinic / Q000187:drug effects / Q000378:metabolism*; D014101:Torpedo
chemical_list: D000345:Affinity Labels; D002038:Bungarotoxins; D003979:Diazonium Compounds; D011978:Receptors, Nicotinic; D002217:Carbachol; D010622:Phencyclidine