• binds
  • These results suggest that tetracaine binds to closed states of CNG channels with approximately three orders of magnitude higher affinity than to open states. (rupress.org)
  • 3 H]Tetracaine binds at equilibrium to a single site with a K eq value of 0.5 μM in the absence of agonist or presence of α-bungarotoxin and with a K eq value of 30 μM in the presence of agonist (i.e., for nAChR in the desensitized state). (aspetjournals.org)
  • subunit
  • When applied to the intracellular side of wild-type rod CNG channels expressed in Xenopus oocytes from the α subunit, the local anesthetic tetracaine exhibits state-dependent block, binding with much higher affinity to closed states than to open states. (rupress.org)
  • The pharmacological specificity of nAChR subunit photolabeling as well as its dependence on [ 3 H]tetracaine concentration establish that the observed photolabeling is at the high-affinity [ 3 H]tetracaine-binding site. (aspetjournals.org)
  • dependence
  • Here we show that neutralization of a glutamic acid in the conserved P region (E363G) eliminated this state dependence of tetracaine block. (rupress.org)
  • This voltage dependence is consistent with the hypothesis that tetracaine blocks the pore of CNG channels. (rupress.org)
  • channel
  • These results suggest that E363 is accessible to internal tetracaine in the closed but not the open configuration of the pore and that the conformational change that accompanies channel opening includes a change in the conformation or accessibility of E363. (rupress.org)
  • Under these conditions, tetracaine is more effective at blocking the rod channel than the olfactory channel. (rupress.org)
  • With all four subunits contributing to [ 3 H]tetracaine site, the site in the closed channel state of the nAChR is most likely within the central ion channel domain. (aspetjournals.org)
  • Conditions
  • Neo-Predef with Tetracaine Powder is indicated in the treatment of certain ear and skin conditions in dogs, cats and horses. (valleyvet.com)
  • Tetracaine becomes more effective at blocking CNG channels under conditions that permit the channels to spend more time in closed states, such as low concentrations of cGMP or saturating concentrations of cAMP. (rupress.org)
  • release
  • In biomedical research, tetracaine is used to alter the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. (wikipedia.org)
  • similar
  • Irradiation at 302 nm of nAChR-rich membranes equilibrated with [ 3 H]tetracaine resulted in covalent incorporation with similar efficiency into nAChR α, β, γ, and δ subunits. (aspetjournals.org)
  • children
  • A systematic review investigated tetracaine for use in emergency departments, especially for starting intravenous lines in children, in view of its analgesic and cost-saving properties. (wikipedia.org)