Disease relevance of Syncurine

• A rapid and sensitive radioimmunological method is described, using decamethonium (DC), which revealed antibodies which blocked alpha-bungarotoxin (alpha-Bgt) binding to human acetylcholine receptor (AChR) in 98% of myasthenia gravis (MG) patients' sera tested [1].
• Decamethonium bromide caused generalized edema and high mortality with treated embryos rarely surviving beyond day 16 of incubation [2].
• Tubocurarine, succinylcholine and decamethonium exhibited their typical action when tested with spermatic nerve-cremaster muscle preparation; the latter two drugs also produced muscle spasm [3].
• In order to examine the applicability of this method, we chose the excitatory type of acetylcholine-induced responses of the ganglion cells in Aplysia, and analyzed the mode of inhibition by decamethonium (Deca) and tetraethylammonium (TEA) [4].

High impact information on Syncurine

• Decamethonium efficiently blocked alkylation by DPA in all three investigated peptides [5].
• At -130 mV membrane potential and 13 degrees, the mean open time of decamethonium-activated channels is 2.8 msec [6].
• Miniature endplate currents, endplate current fluctuations ("membrane noise"), and voltage-jump current relaxations were studied in voltage-clamped frog muscle fibers during decamethonium action [6].
• The voltage-sensitive component has the relative amplitudes acetylcholine less than carbamoylcholine less than decamethonium, and for each agonist equals the closing rate determined from "noise" measurements at neuromuscular junctions [7].
• The pharmacological profile of agents which inhibit 125I-alpha BuTx binding to Aplysia ganglia was similar to the profile of vertebrate ganglionic and brain preparations; d-tubocurarine, nicotine, and carbamylcholine effectively and competitively inhibit binding, whereas hexamethonium and decamethonium are less effective and noncompetitive [8].

Biological context of Syncurine

• The antagonists dihydro-beta-erythroidine, methyllycaconitine, d-tubocurarine, hexamethonium, decamethonium, and mecamylamine either failed to up-regulate [3H]epibatidine binding sites or up-regulated mildly at high concentrations [9].
• A comparison of the alpha(2)S10'A beta T10'A gamma delta mutant to WT receptors revealed faster desensitization kinetics, increased sensitivity to ACh, a higher efficacy for activation by the partial nicotinic agonist decamethonium, and a greater number of openings per burst [10].
• Maximal finger muscle contractions were also weakened by partial neuromuscular blockade with either decamethonium or tubocurarine [11].
• 2. Injection of tetrapentylammonium, nonyl-triethylammonium and decamethonium all reversibly blocked transmission evoked by presynaptic action potentials [12].
• (1) The activators of neural transmission, decamethonium and carbamylcholine, occupy overlapping binding sites [13].

Anatomical context of Syncurine

• Decamethonium induced a detectable depolarization of the chromaffin cells [14].
• In human subjects sustained static contractions of the quadriceps femoris in one leg were performed with the same absolute and the same relative intensity before and after partial neuromuscular blockade with either decamethonium or tubocurarine which reduced strength to about 50% of the control value [15].
• 4 On the frog rectus abdominis the alkylating agent, decamethonium mustard, does not produce any 'parallel shift' of the dose-response curve for carbachol, the only result of alkylation being a decrease in maximal response, which is more pronounced in isometric than in isotonic conditions [16].
• 3. Chick embryos were treated in ovo during the early period of nerve-muscle interactions with d-tubocurarine (dTC; a competitive neuromuscular blocking agent) or with decamethonium (dMET; a depolarizing agent) [17].
• D-Tubocurarine, nicotine, decamethonium and atropine displaced [125]alpha-BuTX from sciatic nerve sections with affinities comparable to those previously reported for the toxin binding component of rat brain [18].

Associations of Syncurine with other chemical compounds

• Alkylation of the AChR by N-(1-pyrene)maleimide is pH-dependent with an apparent pKa of 7.5 and is unaffected by preincubation with carbamylcholine, alpha-bungarotoxin, tubocurarine, or decamethonium [19].
• Edrophonium, decamethonium, and propidium, three quaternary AChE ligands of different types, were tested as potential accelerators [20].
• 1. Depolarization caused by carbachol or decamethonium is followed by spontaneous recovery of membrane potential in the presence of the drug [21].
• 1. Tritium-labelled decamethonium accumulated in diaphragm muscles of the rat in vitro with a peak at the end-plate region and the distributions were fitted by Gaussian curves [22].
• An unsymmetrical decamethonium spin label (XVIII) in which one of the quaternary methyl groups had been replaced by the 4-(2,2,6,6-tetramethyl-1-piperidinyloxy) moiety was 13 times more potent as an inhibitor of Torpedo californica acetylcholinesterase than the parent drug [23].

Gene context of Syncurine

• Unlike curare, pretreatment of the preparation with enterotoxin did not antagonize the neuromuscular block by decamethonium [24].
• With this band as a probe, the bound tacrine could be displaced by edrophonium or decamethonium, both of which are known to bind to the anionic site at the active center of AChE, but not by propidium, which binds to the peripheral site of the enzyme [25].
• Human Tf was found to be resolved in an uncoated capillary equilibrated with a borate buffer containing millimolar concentrations of decamethonium bromide as a buffer additive [26].
• The Y337 (F330) in mammalian acetylcholinesterase, which is replaced by A328 in human butyrylcholinesterase, is implicated in the binding of ligands such as huperzine A, edrophonium, and acridines and one end of bisquaternary compounds such as BW284C51 and decamethonium [27].
• BACKGROUND: Of the polymethylene bismethonium congeners (C5-C12 and C18), decamethonium (C10) is the most potent neuromuscular blocking agent [28].

Analytical, diagnostic and therapeutic context of Syncurine

• After elution from the immunoadsorbent with pH 11 buffer, the preparation was purified further by affinity chromatography on phenyltrimethylammonium-Sepharose 4B with decamethonium elution [29].
• The purified enzyme eluted from the column by decamethonium bromide migrated as a single band of 500 kD on nondenaturing polyacrylamide gel electrophoresis (PAGE), whether stained for proteins or for enzymatic activity [30].
• 4 Scintillation counting showed that during infusion of labelled decamethonium the radioactivity of the muscles increased progressively with time [31].
• 5 The labelled drug was localized by autoradiography of frozen sections of leg muscles following intra-arterial injection of decamethonium [31].
• Here, we demonstrate how patch clamp recording during rapid perfusion of agonists to outside-out patches from BC3H-1 cells can be used to provide an unambiguous estimate of the efficacy of decamethonium [32].

References