title: Reversible and irreversible inhibition by anesthetics of the calcium-induced luminescence of aequorin.
abstract: The actions of various kinds of so-called membrane-stabilizing drugs on Ca2+-induced flash intensity of purified aequorin, a photoprotein obtained from Aequorea aequorea, were examined. All drugs used in this experiment, including inhalational anesthetics, tetracaine, chlorpromazine, and morphine, depressed flash intensity, and the inhibition increased with time. The inhibition followed a mixture of reversible and irreversible kinetics. A method of analyzing irreversible kinetics is presented. The dissociation constants for reversible inhibition and the rate constants for irreversible inhibition are presented for each agent.
mesh_terms: D000331:Aequorin; D000768:Anesthesia, General; D000779:Anesthetics, Local / Q000494:pharmacology*; D002118:Calcium / Q000037:antagonists & inhibitors*; D002746:Chlorpromazine / Q000494:pharmacology; D006221:Halothane / Q000494:pharmacology; D007700:Kinetics; D008163:Luminescent Measurements; D008733:Methoxyflurane / Q000494:pharmacology; D009020:Morphine / Q000494:pharmacology; D011506:Proteins; D013748:Tetracaine / Q000494:pharmacology
chemical_list: D000779:Anesthetics, Local; D011506:Proteins; D013748:Tetracaine; D008733:Methoxyflurane; D000331:Aequorin; D009020:Morphine; D002118:Calcium; D002746:Chlorpromazine; D006221:Halothane
references.citation: Biochemistry. 1969 Oct;8(10):3991-7
references.pmid: 4390576
references.citation: Can J Physiol Pharmacol. 1967 Jul;45(4):587-96
references.pmid: 4382487
references.citation: Pharmacol Rev. 1972 Dec;24(4):583-655
references.pmid: 4565956
references.citation: Anesthesiology. 1974 Dec;41(6):576-9
references.pmid: 4433057
references.citation: Anesthesiology. 1976 Mar;44(3):211-5
references.pmid: 1267888
references.citation: Biochem Pharmacol. 1969 Feb;18(2):339-46
references.pmid: 5778151