| 2422792 |
Aronstam RS, Hong JS: Interactions of chlordecone (kepone) and mirex with the nicotinic acetylcholine receptor--ion channel complex. Toxicol Lett. 1986 Mar;30(3):247-51.
Interactions of chlordecone (kepone) and mirex with nicotinic acetylcholine (ACh) receptor complexes from Torpedo californica electric organs were studied using biochemical probes for ACh and ion-channel binding sites. Neither compound inhibited the binding of [125I] alpha-bungarotoxin (BGT) to the receptor; chlordecone, however, enhanced carbamylcholine affinity for the receptor 5-fold. Chlordecone, but not mirex, also inhibited the binding of [3H] perhydrohistrionicotoxin and [3H] phencyclidine to sites associated with the receptor-gated ion channel. Ion-channel inhibition by chlordecone was enhanced in the presence of carbamylcholine. These results indicate that chlordecone, but not mirex, interacts with the ion-translocation mechanism associated with nicotinic ACh receptors, where it may sterically block ion flux as well as stabilize a desensitized conformation of the receptor complex. |
81(1,1,1,1) |