• Sodium channels are important proteins in modulating neuronal membrane excitability. (aspetjournals.org)
  • Genetic studies from patients and animals have indicated neuronal sodium channels play key roles in pain sensitization. (aspetjournals.org)
  • NKTR-171 is a new molecular entity that is specifically designed to treat neuropathic pain by blocking hyperactive neuronal sodium channels associated with damaged nerves in the peripheral nervous system.Chronic neuropathic pain arises from nerves injured or damaged by systemic disease, infection, toxins, or physical trauma that are in a continuous state of hyper-excitability, often due to aberrant sodium channel firing. (bio-medicine.org)
  • We demonstrated that WB4101 inhibited both Nav1.7 and Nav1.8 channels with similar levels of potency. (aspetjournals.org)
  • WB4101 induced a hyperpolarizing shift in the voltage-dependent inactivation for both Nav1.7 (15 mV) and Nav1.8 (20 mV) channels. (aspetjournals.org)
  • Consistent with the state-dependent block, the drug also displayed use-dependent inhibitory properties on both wild-type Nav1.7 and Nav1.8 channels, which were removed by the local anesthetic-insensitive mutations but still existed in the inactivation-deficient channels. (aspetjournals.org)
  • These results support the hypothesis that TTX-sensitive sodium channels at axonal nodes of Ranvier play a significant role in the secondary injury of WM after SCI. (jneurosci.org)
  • The results indicate that acute axonal pathology is significantly reduced with TTX treatment, supporting the hypothesis that axonal Na + channels contribute to secondary injury of WM after SCI. (jneurosci.org)
  • NKTR-171 is designed to be a peripherally-restricted molecule which selectively blocks hyper-excitable sodium channels without causing the CNS side effects that limit usage of existing therapies. (bio-medicine.org)
  • LQT3 mutations in the LQTS Registry will be studied using in vitro expression studies to determine whether ranolazine causes a decrease in late sodium current, slower recovery from inactivation and/or changes in time course of inactivation, ameliorating the causative functional effect of each individual mutation. (clinicaltrials.gov)
  • 4 provide evidence for the safety and analgesic potential of neosaxitoxin, a site-1 sodium channel blocker. (asahq.org)
  • 5 The separation in neosaxitoxin affinities for sodium channel isoforms is at least an order of magnitude greater than that for any conventional local anesthetic. (asahq.org)
  • As we have learned more about the sub-types of sodium channels and their distribution, new therapeutic opportunities have suggested themselves. (eurekaselect.com)
  • Effects of the sodium channel blocker amitriptyline on the spontaneous and stimulus-evoked activity of corneal cold-sensitive nerve terminals in intact and tear-deficient guinea-pig eyes. (arvojournals.org)
  • Na + -channel blocker amitriptyline attenuates the spontaneous activity and cooling response of cold nerve terminals in intact corneas and less efficiently in DE corneas. (arvojournals.org)