tubocurarine

Summary

Summary: A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.

Top Publications

  1. Hibbs R, Radic Z, Taylor P, Johnson D. Influence of agonists and antagonists on the segmental motion of residues near the agonist binding pocket of the acetylcholine-binding protein. J Biol Chem. 2006;281:39708-18 pubmed
    ..decay of anisotropy were assessed for one agonist (epibatidine) and two antagonists (alpha-bungarotoxin and d-tubocurarine)...
  2. Alyautdin R, Tezikov E, Ramge P, Kharkevich D, Begley D, Kreuter J. Significant entry of tubocurarine into the brain of rats by adsorption to polysorbate 80-coated polybutylcyanoacrylate nanoparticles: an in situ brain perfusion study. J Microencapsul. 1998;15:67-74 pubmed
    ..b>Tubocurarine (a quaternary ammonium salt) does not penetrate the normal intact blood-brain barrier...
  3. Hogue C, Ward J, Itani M, Martyn J. Tolerance and upregulation of acetylcholine receptors follow chronic infusion of d-tubocurarine. J Appl Physiol (1985). 1992;72:1326-31 pubmed
    ..Chronic antagonism of the nAChR was achieved in rats by an infusion of d-tubocurarine (dTC) via subcutaneously placed osmotic pumps...
  4. Rossokhin A, Teodorescu G, Grissmer S, Zhorov B. Interaction of d-tubocurarine with potassium channels: molecular modeling and ligand binding. Mol Pharmacol. 2006;69:1356-65 pubmed
    ..3 using the X-ray structures of MthK and Kv1.2, respectively, and simulated the binding of d-tubocurarine in the inner pore of the channels...
  5. O Leary M, Filatov G, White M. Characterization of d-tubocurarine binding site of Torpedo acetylcholine receptor. Am J Physiol. 1994;266:C648-53 pubmed
    d-Tubocurarine (curare) is a well-characterized competitive antagonist of nicotinic acetylcholine receptors (AChRs), and it is usually assumed that curare and agonists share a common binding site...
  6. Ibebunjo C, Donati F, Fox G, Eshelby D, Tchervenkov J. The effects of chronic tacrine therapy on d-tubocurarine blockade in the soleus and tibialis muscles of the rat. Anesth Analg. 1997;85:431-6 pubmed
    ..We determined the magnitude and time course of the effects of chronic oral THA and of intravenous (IV) THA on d-tubocurarine (dTC) blockade at the soleus and tibialis muscles...
  7. Wenningmann I, Dilger J. The kinetics of inhibition of nicotinic acetylcholine receptors by (+)-tubocurarine and pancuronium. Mol Pharmacol. 2001;60:790-6 pubmed
    ..Previous determinations of the dissociation rate of (+)-tubocurarine have produced inconsistent results ranging from 0.1 to 4000/s...
  8. Sheiner L, Stanski D, Vozeh S, Miller R, Ham J. Simultaneous modeling of pharmacokinetics and pharmacodynamics: application to d-tubocurarine. Clin Pharmacol Ther. 1979;25:358-71 pubmed
    ..The model is demonstrated on two different sets of Cp and effect data for the drug d-tubocurarine (dTC)...
  9. Nyce H, Stober S, Abrams C, White M. Mapping spatial relationships between residues in the ligand-binding domain of the 5-HT3 receptor using a molecular ruler. Biophys J. 2010;98:1847-55 pubmed publisher
    ..that are expressed on the cell surface, but decreases receptor affinity for the competitive antagonist d-tubocurarine (dTC) 5-35-fold...

More Information

Publications62

  1. Yan D, White M. Interaction of d-tubocurarine analogs with mutant 5-HT(3) receptors. Neuropharmacology. 2002;43:367-73 pubmed
    d-Tubocurarine is a potent competitive antagonist of both the muscle-type nicotinic acetylcholine receptor (AChR) and the serotonin type-3 receptor (5HT(3)R)...
  2. Brams M, Pandya A, Kuzmin D, van Elk R, Krijnen L, Yakel J, et al. A structural and mutagenic blueprint for molecular recognition of strychnine and d-tubocurarine by different cys-loop receptors. PLoS Biol. 2011;9:e1001034 pubmed publisher
    ..Strychnine and d-tubocurarine (d-TC) are neurotoxins that have been highly instrumental in decades of research on glycine receptors (GlyR) ..
  3. Gao F, Bern N, Little A, Wang H, Hansen S, Talley T, et al. Curariform antagonists bind in different orientations to acetylcholine-binding protein. J Biol Chem. 2003;278:23020-6 pubmed
    ..of competitive antagonists at the atomic structural level, we studied binding of the curare derivatives d-tubocurarine (d-TC) and metocurine to AChBP using computational methods, mutagenesis, and ligand binding measurements...
  4. Zhang R, Wen X, Militante J, Hester B, Rhubottom H, Sun H, et al. The role of loop F residues in determining differential d-tubocurarine potencies in mouse and human 5-hydroxytryptamine 3A receptors. Biochemistry. 2007;46:1194-204 pubmed
    The competitive antagonist d-tubocurarine (curare) has greater potency at mouse than at human 5-hydroxytryptamine 3A (5-HT3A) receptors, despite 84% amino acid sequence identity between the receptors...
  5. Sine S. Molecular dissection of subunit interfaces in the acetylcholine receptor: identification of residues that determine curare selectivity. Proc Natl Acad Sci U S A. 1993;90:9436-40 pubmed
    ..The determinants lie on either side of a disulfide loop found within the major extracellular domain of the subunits. This loop is common to all acetylcholine, gamma-aminobutyrate, and glycine receptor subunits...
  6. Yan D, Meyer J, White M. Mapping residues in the ligand-binding domain of the 5-HT(3) receptor onto d-tubocurarine structure. Mol Pharmacol. 2006;70:571-8 pubmed
    ..of the binding site to tyrosine (F226Y) has no effect on the apparent affinity of the competitive antagonist d-tubocurarine (dTC) for the receptor...
  7. Nguyen Huu T, Dobbertin A, Barbier J, Minic J, Krejci E, Duvaldestin P, et al. Cholinesterases and the resistance of the mouse diaphragm to the effect of tubocurarine. Anesthesiology. 2005;103:788-95 pubmed
    ..Because of the competitive mechanism of action of tubocurarine, the rate of hydrolysis of acetylcholine at the neuromuscular junction may modulate its neuromuscular blocking ..
  8. Basu S, Chaudhuri T, Chauhan S, Das Gupta A, Chaudhury L, Vedasiromoni J. The theaflavin fraction is responsible for the facilitatory effect of black tea at the skeletal myoneural junction. Life Sci. 2005;76:3081-8 pubmed
    ..Tfs completely antagonized the submaximal paralytic effect of d- tubocurarine and decamethonium bromide...
  9. Stojan J, Pavlic M. On the inhibition of cholinesterase by D-tubocurarine. Biochim Biophys Acta. 1991;1079:96-102 pubmed
    Some investigation in this laboratory pointed to an unexpectedly slow inhibition of cholinesterase by D-tubocurarine, occurring in addition to a typically instantaneous inhibition...
  10. Nakamura S, Saitoh M, Yamazaki M, Nishimura M, Kurashige Y, Arakawa T, et al. Nicotine induces upregulated expression of beta defensin-2 via the p38MAPK pathway in the HaCaT human keratinocyte cell line. Med Mol Morphol. 2010;43:204-10 pubmed publisher
    ..Both nAChR inhibitors also abolished the upregulation of hBD-2 by nicotine. The present study demonstrated that nicotine causes upregulated expression of hBD-2 via the p38MAP kinase pathway in keratinocytes...
  11. Turner G, Williams J, Baker D. Train-of-four fade during onset and recovery of neuromuscular block: a study in non-anaesthetized subjects. Br J Anaesth. 1989;62:279-86 pubmed
    The actions of alcuronium, vecuronium and tubocurarine have been studied in the isolated forearms of six healthy, non-anaesthetized volunteers...
  12. Wu M, Hajszan T, Leranth C, Alreja M. Nicotine recruits a local glutamatergic circuit to excite septohippocampal GABAergic neurons. Eur J Neurosci. 2003;18:1155-68 pubmed
    ..The discovery of a local glutamatergic circuit within the septum may provide another avenue for restoring septohippocampal GABAergic functions in neurodegenerative disorders associated with a loss of septohippocampal cholinergic neurons...
  13. Puura A, Baer G, Rorarius M. Neuromuscular blocking characteristics of vecuronium after tubocurarine-induced "fade". An experimental double-blind clinical study. Eur J Clin Pharmacol. 1999;55:173-6 pubmed
    ..During onset of the neuromuscular block (NMB) tubocurarine (TC) causes more fade in the TOF responses than vecuronium (VEC)...
  14. Psaridi Linardaki L, Mamalaki A, Tzartos S. Future therapeutic strategies in autoimmune myasthenia gravis. Ann N Y Acad Sci. 2003;998:539-48 pubmed
    ..1 +/- 2.4 nM), and this binding was blocked by unlabeled d-tubocurarine and gallamine...
  15. Hakki A, Friedman H, Pross S. Nicotine modulation of apoptosis in human coronary artery endothelial cells. Int Immunopharmacol. 2002;2:1403-9 pubmed
    ..This decrease was blocked by the addition of d-tubocurarine chloride (d-TC), a general nicotinic receptor antagonist, providing evidence that this action of nicotine was ..
  16. Magloire V, Streit J. Intrinsic activity and positive feedback in motor circuits in organotypic spinal cord slice cultures. Eur J Neurosci. 2009;30:1487-97 pubmed publisher
    ..By contrast, the uncorrelated muscle activity is fully suppressed by the muscular nicotinic antagonist D-tubocurarine. Together, these findings confirm the previous finding that motoneurons drive muscle fibres in this preparation ..
  17. Kimura I, Okazaki M, Uwano T, Kobayashi S, Kimura M. Succinylcholine-induced acceleration and suppression of electrically evoked acetylcholine release from mouse phrenic nerve-hemidiaphragm muscle preparation. Jpn J Pharmacol. 1991;57:397-403 pubmed
    ..b>Tubocurarine (5 microM) prevented the enhancing effect of [3H]-ACh release induced by 1 microM, but not the decreasing ..
  18. Erkola O. Effects of precurarisation on suxamethonium-induced postoperative myalgia during the first trimester of pregnancy. Acta Anaesthesiol Scand. 1990;34:63-7 pubmed
    ..Either alcuronium (0.03 mg/kg), atracurium (0.04 mg/kg), tubocurarine (0.05 mg/kg), vecuronium (0...
  19. Chiara D, Dangott L, Eckenhoff R, Cohen J. Identification of nicotinic acetylcholine receptor amino acids photolabeled by the volatile anesthetic halothane. Biochemistry. 2003;42:13457-67 pubmed
    ..Labeling of deltaTyr-212 in the extracellular domain was inhibited >90% by d-tubocurarine, whereas addition of either carbamylcholine or isoflurane had no effect...
  20. Shiina T, Shimizu Y, Boudaka A, Wörl J, Takewaki T. Tachykinins are involved in local reflex modulation of vagally mediated striated muscle contractions in the rat esophagus via tachykinin NK1 receptors. Neuroscience. 2006;139:495-503 pubmed
    ..Electrical stimulation of the vagus nerve evoked twitch contractile responses that were abolished by d-tubocurarine (5 microM)...
  21. Yeoman M, Parish D, Benjamin P. A cholinergic modulatory interneuron in the feeding system of the snail, Lymnaea. J Neurophysiol. 1993;70:37-50 pubmed
    ..8. The evidence suggests that ACh is the main neurochemical involved in allowing the SO to initiate and control the frequency of the Lymnaea feeding CPG...
  22. Dewael Y, Mallefet J. Luminescence in ophiuroids (Echinodermata) does not share a common nervous control in all species. J Exp Biol. 2002;205:799-806 pubmed
    ..In this species, the involvement of both muscarinic and nicotinic receptors is proposed, since atropine and tubocurarine (at 10(-3) mol l(-1)) inhibited 99 % and 71 %, respectively, of the light emitted...
  23. Zouridakis M, Zisimopoulou P, Eliopoulos E, Poulas K, Tzartos S. Design and expression of human alpha7 nicotinic acetylcholine receptor extracellular domain mutants with enhanced solubility and ligand-binding properties. Biochim Biophys Acta. 2009;1794:355-66 pubmed publisher
    ..nM) compared to the wild-type-ECD (K(d)=70 nM), the binding being inhibited by unlabelled alpha-bungarotoxin, d-tubocurarine or nicotine (K(i) of 21.5 nM, 127 microM and 17.5 mM, respectively)...
  24. Woo R, Park E, Shin M, Jeong M, Zhao R, Shin B, et al. Mechanism of nicotine-evoked release of 3H-noradrenaline in human cerebral cortex slices. Br J Pharmacol. 2002;137:1063-70 pubmed
    ..5. Mecamylamine (10 micro M), dihydro-beta-erythroidine (10 micro M) and d-tubocurarine (30 micro M), but not alpha-bungarotoxin (alpha-BTX, 0...
  25. Buznego M, Pérez Saad H. Acute effect of an extract of Ambrosia paniculata (Willd.) O. E. Schultz (mugwort) in several models of experimental epilepsy. Epilepsy Behav. 2004;5:847-51 pubmed
    ..penicillin-agar-saline mixture and recorded in sensorimotor and occipital cortices, in rats immobilized with d-tubocurarine. The plant decoction reduced significantly the spike amplitude in both sites...
  26. Geertsen S, Afar R, Trifaro J, Quik M. Regulation of alpha-bungarotoxin sites in chromaffin cells in culture by nicotinic receptor ligands, K+, and cAMP. Mol Pharmacol. 1988;34:549-56 pubmed
    Previous work had shown that incubation with the nicotinic antagonist d-tubocurarine resulted in a marked increase in alpha-bungarotoxin (alpha-BGT) binding in adrenal medullary chromaffin cells in culture; the possible molecular ..
  27. Prisco S, Natoli S, Bernardi G, Mercuri N. Group I metabotropic glutamate receptors activate burst firing in rat midbrain dopaminergic neurons. Neuropharmacology. 2002;42:289-96 pubmed
    ..burst firing when exposed to the Group I metabotropic glutamate receptor (mGluR) agonist DHPG (30 microM) and d-tubocurarine (500 microM) (d-TC), whereas they all fired in bursts during NMDA (20 microM) plus d-TC application...
  28. Bonaventure N, Jardon B, Wioland N, Yucel H, Rudolf G. On cholinergic mechanisms in the optokinetic nystagmus of the frog: antagonistic effects of muscarinic and nicotinic systems. Behav Brain Res. 1988;27:59-71 pubmed
    ..Similar results were obtained with ACh nicotinic antagonists (D-tubocurarine, alpha-bungarotoxin, hexamethonium and gallamine)...
  29. Chang C, Chen S, Hong S. Reversals of the neostigmine-induced tetanic fade and endplate potential run-down with respect to the autoregulation of transmitter release. Br J Pharmacol. 1988;95:1255-61 pubmed
    ..more light on the role of presynaptic cholinoceptors in the modulation of transmitter release, the effects of tubocurarine, choline and hexamethonium on neostigmine-induced tetanic fade and run-down of endplate potentials (e.p...
  30. Wallis D, Dun N. A comparison of fast and slow depolarizations evoked by 5-HT in guinea-pig coeliac ganglion cells in vitro. Br J Pharmacol. 1988;93:110-20 pubmed
    ..They were reduced in amplitude by tubocurarine (10-100 microM, pIC50 4.4), MDL 72222 (1-5 microM, pIC50 5...
  31. Albanese C, Nour B, Rowe M. Anesthesia blocks nonshivering thermogenesis in the neonatal rabbit. J Pediatr Surg. 1994;29:983-6 pubmed
    ..However, cessation of anesthesia (halothane) in a cold environment results in a marked increase in metabolic activity...
  32. Gonzalez Forero D, Alvarez F. Differential postnatal maturation of GABAA, glycine receptor, and mixed synaptic currents in Renshaw cells and ventral spinal interneurons. J Neurosci. 2005;25:2010-23 pubmed
    ..As a result, charge transfer in GABA, glycine, or mixed mPSCs was larger in mature RCs than in non-RCs, suggesting RCs receive potent inhibitory synapses...
  33. Oron L, Sarne Y, Michaelson D. Nonopioid effect of morphine on electrically evoked acetylcholine release from Torpedo electromotor neurons. J Neurochem. 1992;58:416-20 pubmed
    ..stimulation was modulated by morphine, by the muscarinic antagonist atropine, and by the nicotinic antagonist tubocurarine. Addition of either atropine or tubocurarine in the presence of the acetylcholinesterase inhibitor phospholine ..
  34. Bal R, Erdogan S, Theophilidis G, Baydas G, Naziroglu M. Assessing the effects of the neonicotinoid insecticide imidacloprid in the cholinergic synapses of the stellate cells of the mouse cochlear nucleus using whole-cell patch-clamp recording. Neurotoxicology. 2010;31:113-20 pubmed publisher
    ..IMI decreased the membrane input resistance and the membrane time constants. Bath application of 50 microM d-tubocurarine (d-TC) reversibly blocked the depolarizing shift of the resting membrane potential and the spontaneous firing ..
  35. Kumamoto E, Nohmi M, Shinnick Gallagher P. Fast hyperpolarization following an excitatory postsynaptic potential in cat bladder parasympathetic neurons. Neuroscience. 1989;30:671-81 pubmed
    ..potential sequence was blocked completely and reversibly by nicotinic receptor antagonists (hexamethonium and D-tubocurarine)...
  36. Kapur A, Davies M, Dryden W, Dunn S. Tryptophan 86 of the alpha subunit in the Torpedo nicotinic acetylcholine receptor is important for channel activation by the bisquaternary ligand suberyldicholine. Biochemistry. 2006;45:10337-43 pubmed
    ..wild type with respect to the concentration dependence of channel activation, receptor desensitization, or d-tubocurarine inhibition...
  37. Lovenberg T, Roth R, Nichols D, Mailman R. D1 dopamine receptors of NS20Y neuroblastoma cells are functionally similar to rat striatal D1 receptors. J Neurochem. 1991;57:1563-9 pubmed
    ..The present results indicate that NS20Y neuroblastoma cells have D1 receptors that are coupled to adenylate cyclase, and that these receptors have a pharmacological profile similar to that of the D1 receptor(s) found in rat striatum...
  38. Røed A. Effects of chlorhexidine on the isolated rat phrenic nerve-diaphragm preparation. Pharmacol Toxicol. 1994;74:10-6 pubmed
    ..It could not be inhibited by the excitation-contraction uncoupler dantrolene, but it was dependent on extracellular Ca2+. Chlorhexidine-induced influx of Ca2+ might thus cause the contracture...
  39. Fieber L, Adams D. Acetylcholine-evoked currents in cultured neurones dissociated from rat parasympathetic cardiac ganglia. J Physiol. 1991;434:215-37 pubmed
    ..Kd = 37 nM) and hexamethonium (IC50 approximately 1 microM), as well as by the neuromuscular relaxant, d-tubocurarine (Kd = 3 microM)...
  40. Bossa R, Chiericozzi M, Efstathiu G, Galatulas I, Ninci M. The effect of famotidine on neuromuscular transmission. In Vivo. 1991;5:53-5 pubmed
    ..Famotidine, administered by I.V. injection, potentiates the neuromuscular blockade induced by d-tubocurarine, pancuronium and aminoglycoside antibiotics...
  41. Pawelczyk J, Pawelczyk R, Warberg J, Mitchell J, Secher N. Cardiovascular and catecholamine responses to static exercise in partially curarized humans. Acta Physiol Scand. 1997;160:23-8 pubmed
  42. Jüttner R, Henneberger C, Grantyn R, Rothe T. Early onset of glutamatergic and GABAergic synaptic activity in the visual layers of the rodent superior colliculus. Int J Dev Neurosci. 2001;19:255-61 pubmed
    ..The early function of glutamatergic and GABAergic synaptic transmission in the visual layers of SC suggests that SC neurons are able to process information originating from retinal axons immediately after birth...
  43. Murashov A, Haq I, Hill C, Park E, Smith M, Wang X, et al. Crosstalk between p38, Hsp25 and Akt in spinal motor neurons after sciatic nerve injury. Brain Res Mol Brain Res. 2001;93:199-208 pubmed
    ..Together, our observations implicate Hsp25 as a central player in a complex system of signaling that may both promote regeneration of nerve fibers and prevent neuronal cell death in the injured spinal cord...
  44. Chiao C, Masland R. Starburst cells nondirectionally facilitate the responses of direction-selective retinal ganglion cells. J Neurosci. 2002;22:10509-13 pubmed
    ..This seems to place a constraint on models of the directional discrimination in which the starburst cells participate, namely, that their cholinergic synapses be nondirectional in their effects on the ganglion cells...
  45. Yanagita M, Kobayashi R, Kojima Y, Mori K, Murakami S. Nicotine modulates the immunological function of dendritic cells through peroxisome proliferator-activated receptor-? upregulation. Cell Immunol. 2012;274:26-33 pubmed publisher
    ..Expression of PPAR ? and PPAR ?-target genes was significantly inhibited by pretreatment with d-tubocurarine, antagonist of non-selective nicotinic acetylcholine receptors (nAChR)...
  46. Heier T. [Muscle relaxants]. Tidsskr Nor Laegeforen. 2010;130:398-401 pubmed publisher
    ..The purpose of this article is to provide an overview of the history of muscle relaxants, their mode of action and their role in current anaesthetic practice...
  47. Nguyen Huu T, Molgo J, Servent D, Duvaldestin P. Resistance to D-tubocurarine of the rat diaphragm as compared to a limb muscle: influence of quantal transmitter release and nicotinic acetylcholine receptors. Anesthesiology. 2009;110:1011-5 pubmed publisher
    ..The basis of this difference may be a higher concentration of acetylcholine released or higher number of postsynaptic nicotinic acetylcholine receptors in diaphragmatic neuromuscular junctions...
  48. Meretoja O, Brown T, Clare D. Dose response of alcuronium and d-tubocurarine in infants, children and adolescents. Anaesth Intensive Care. 1990;18:449-51 pubmed
    ..to create an individual dose-response curve for the long-acting neuromuscular blocking agents, alcuronium and d-tubocurarine. The mean (SEM) ED95 of alcuronium was 196 (9), 271 (13) and 243 (8) micrograms/kg in infants, children and ..
  49. Niel J, Clerc N, Jule Y. Patterns of fast synaptic cholinergic activation of neurons in the celiac ganglia of cats. Am J Physiol. 1988;255:G759-66 pubmed
    ..The existence of the mechanisms described in this study reflects the complexity of the integrative processes at work in neurons of the cat celiac ganglia that involve fast synaptic cholinergic activation...
  50. Narimatsu E, Niiya T, Kawamata M, Namiki A. Sepsis stage dependently and differentially attenuates the effects of nondepolarizing neuromuscular blockers on the rat diaphragm in vitro. Anesth Analg. 2005;100:823-9, table of contents pubmed
    ..1 Hz were evaluated. Rocuronium, pancuronium, and d-tubocurarine dose-dependently decreased the twitch tensions of the nonseptic, early septic, and late septic diaphragms (P &..
  51. Stensløkken K, Sundin L, Renshaw G, Nilsson G. Adenosinergic and cholinergic control mechanisms during hypoxia in the epaulette shark (Hemiscyllium ocellatum), with emphasis on branchial circulation. J Exp Biol. 2004;207:4451-61 pubmed
    ..3 mg l(-1)) using antagonists against muscarinic (atropine 2 mg kg(-1)) and nicotinic (tubocurarine 5 mg kg(-1)) receptors...
  52. Nikolsky E, Vyskocil F, Bukharaeva E, Samigullin D, Magazanik L. Cholinergic regulation of the evoked quantal release at frog neuromuscular junction. J Physiol. 2004;560:77-88 pubmed
    ..The effects of CCh and nicotine on quantal dispersion were reduced substantially by 5 x 10(-7) M (+)tubocurarine (TC)...
  53. Fairclough R, Twaddle G, Gudipati E, Lin M, Richman D. Differential surface accessibility of alpha(187-199) in the Torpedo acetylcholine receptor alpha subunits. J Mol Biol. 1998;282:317-30 pubmed
    ..binding by alpha-bungarotoxin selectively directed to the alpha subunit correlated with the high-affinity d-tubocurarine binding site, along with a lack of inhibition by alpha-bungarotoxin directed to the alpha subunit correlated ..