Effects of calcium on the binding of phencyclidine to acetylcholine receptor-rich membrane fragments from Torpedo californica electroplaque.
The influence of calcium on the binding of phencyclidine (PCP) to acetylcholine (ACh) receptor-rich membrane fragments was investigated. Calcium decreased the equilibrium affinity for PCP in the presence, but not in the absence, of the cholinergic agonist carbamylcholine. The effect of calcium was rapidly reversible by EGTA, indicating that it was not attributable to a calcium-activated protease or a phospholipase. Following detergent solubilization of the nicotinic ACh receptor, the calcium effect on PCP remained, suggesting that calcium may interact directly with the receptor to exert its effect. Other divalent cations (Mn2+, La2+, Co2+, Mg2+) had similar effects. A correlate of "desensitization" of the ACh receptor can be observed using PCP binding, and a two-step "desensitization" process can be observed. Calcium seemed to increase the amplitude of a rapid component of receptor "desensitization." The results presented in this paper suggest that calcium may play a role in the modulation of the nicotinic ACh receptor.
D000818:Animals; D002118:Calcium / Q000494:pharmacology*; D002217:Carbachol / Q000494:pharmacology; D002413:Cations, Divalent; D002462:Cell Membrane / Q000378:metabolism; D004533:Egtazic Acid / Q000494:pharmacology; D004557:Electric Organ / Q000187:drug effects / Q000378:metabolism*; D010622:Phencyclidine / Q000378:metabolism*; D011950:Receptors, Cholinergic / Q000187:drug effects / Q000378:metabolism*; D014101:Torpedo / Q000378:metabolism*
D002413:Cations, Divalent; D011950:Receptors, Cholinergic; D004533:Egtazic Acid; D002217:Carbachol; D010622:Phencyclidine; D002118:Calcium