Reference

Acetylcholine receptor

Acetylcholine receptor. Responses to drug binding. Maelicke, Alfred; Fulpius, Bernard W.; Klett, Robert P.; Reich, E.; Dumaguing, Emmanuel (Rockefeller Univ., New York, N. Y., USA). J. Biol. Chem., 252(14), 4811-30 (English) 1977. CODEN: JBCHA3. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) Section cross-reference(s): 1 Benzoquinonium chloride [311-09-1], dimethyl-d-tubocurarine iodide [518-26-3], alloferin [15180-03-7], bis-methonium compds., carbamylcholine chloride [51-83-2], nicotine [54-11-5], acetylcholine chloride [60-31-1], and bis(3-aminopyridnium)alkanes competed with cobra .alpha.-neurotoxin for binding sites on the nicotinic acetylcholine recpetor purified from the elec. organ of Electrophorus electricus. Receptor binding of neurotoxin and ligands was mutually exclusive at equil. The ratio of ligand to neurotoxin binding sites was 0.Chemical with cas number 19213-73-1 also plays role.5. All cholinergic antagonists bound to a single class of noninteracting sites whose affinity was independent of concn.; whereas, all cholinergic agonists bound to sites whose affinity was concn. dependent. Large reaction entropies accompanied the binding of all ligands. When high concns. of competing small ligands were added to a soln. of receptor-toxin complexes, there was a transient increase in the rate of complex dissocn. After the new equil. value was reached, the dissocn. rate of the recetor-toxin complex was the same as that obsd. in the absence of ligands. The nicotinic cholinergic receptor may have a high degree of conformation plasticity. .

The action of cholinergic antagonists on the effect of acetylcholine, nicotine and benzoylcholine applied iontophoretically onto two identified neurons in the brain of Helix aspersa

The action of cholinergic antagonists on the effect of acetylcholine, nicotine and benzoylcholine applied iontophoretically onto two identified neurons in the brain of Helix aspersa. Kiss, I.; Walker, R. J. (Dep. Physiol. Biochem., Southampton Univ., Southampton, Engl.). Comp. Biochem. Physiol. C, 60C(1), 89-99 (English) 1978. CODEN: CBPCBB. ISSN: 0306-4492. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Section cross-reference(s): 12 The cholinolytic potencies of 13 compds. were tested against acetylcholine chloride [60-31-1] on 2 H. aspersa neurons, cell E4 and cell F1. Scopolamine-HBr [114-49-8], decamethonium iodide [1420-40-2], and suxamethonium chloride [71-27-2] blocked only acetylcholine inhibition on cell E4, with no cholinolytic action on cell F1. Strychnine sulfate [60-41-3], atropine sulfate [55-48-1], pancuronium bromide [15500-66-0], gallamine triethiodide [65-29-2], and benzoylcholine chloride [2964-09-2] were more potent as antagonists on cell E4 than on cell F1. Hexamethonium bromide [55-97-0] and tubocurarine chloride [57-94-3] were slightly more potent as antagonists on cell F1 than cell E4. Mecamylamine-HCl [826-39-1], pentolinium tartrate [52-62-0], and benzoquinonium chloride [311-09-1] were equally potent on both cells. Atropine, tubocurarine, and hexamethonium blocked the action of both nicotine hydrogen tartrate [65-31-6] and benzoylcholine in both cells, whereas strychnine only blocked the action of benzoylcholine on cell E4.