The desensitizing interaction of hexafluorenium with the cholinergic receptor in the diaphragm of the rat.
1. The interaction of hexafluorenium with acetylcholine, carbachol and suxamethonium with regard to the depolarization of the end-plate of rat diaphragm was studied. The depolarization was measured with the moving meniscus technique of Fatt. The competitive antagonist d-tubocurarine was included in the studies. 2. Hexafluorenium inhibited acetylcholinesterase in the end-plate. 3. The receptors in the end-plate were desensitized by carbachol and suxamethonium. Hexafluorenium enhanced the desensitization by suxamethonium. d-Tubocurarine had no direct influence on desensitization 4. The desensitization of the receptors in rat diaphragm is compatible with a cyclic model of desensitization. 5. The desensitizing interaction of hexafluorenium with the receptors may explain the non-competitive antagonism with depolarizing drugs with regard to the depolarization of the end-plate and the synergism with these drugs with regard to the paralysis of the indirectly stimulated muscle reported earlier. 6. The affinities of carbachol, suxamethonium and d-tubocurarine to the sensitive receptors are 4.9, 5.2 and 6.8, respectively.
D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D002217:Carbachol / Q000494:pharmacology; D003964:Diaphragm / Q000187:drug effects; D005449:Fluorenes; D006584:Hexamethonium Compounds / Q000494:pharmacology*; D066298:In Vitro Techniques; D009045:Motor Endplate / Q000187:drug effects; D009467:Neuromuscular Depolarizing Agents; D051381:Rats; D011950:Receptors, Cholinergic / Q000187:drug effects*; D013390:Succinylcholine / Q000494:pharmacology
D005449:Fluorenes; D006584:Hexamethonium Compounds; D009467:Neuromuscular Depolarizing Agents; D011950:Receptors, Cholinergic; C005034:hexafluorenium; D002217:Carbachol; D013390:Succinylcholine; D000109:Acetylcholine