| 6292640 |
Abbassy MA, Eldefrawi ME, Eldefrawi AT: Allethrin interactions with the nicotinic acetylcholine receptor channel. Life Sci. 1982 Oct 11;31(15):1547-52.
Interactions of the synthetic pyrethroid allethrin with the nicotinic acetylcholine (ACh) receptor/channel were studied in membranes from Torpedo electric organ. Allethrin did not inhibit binding of [3H] ACh to the receptor sites, but inhibited noncompetitively binding of [3H] perhydrohistrionicotoxin ([3H] H12-HTX) to the ionic channel sites in a dose-dependent manner. The inhibition constant (Ki) of [3H] H12-HTX binding in absence of receptor agonist was 30 micro M, while in presence of 100 micro M carbamylcholine it was 4 micro M. This inhibitory effect of allethrin had a negative temperature coefficient. The high affinity binding of allethrin to the channel sites of the nicotinic ACh-receptor may be indicative of a postsynaptic site of action for pyrethroids, in addition to their known action on the sodium channel. |
81(1,1,1,1) |