[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs

J Med Chem. 1985 Mar;28(3):381-8. doi: 10.1021/jm00381a019.


[3H]Batrachotoxinin A benzoate ( [3H]BTX-B) binds with high affinity to sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex. In this preparation, local anesthetics competitively antagonize the binding of [3H]BTX-B. The potencies of some 40 classical local anesthetics and a variety of catecholamine, histamine, serotonin, adenosine, GABA, glycine, acetylcholine, and calcium antagonists, tranquilizers, antidepressants, barbiturates, anticonvulsants, steroids, vasodilators, antiinflammatories, anticoagulants, analgesics, and other agents have been determined. An excellent correlation with the known local anesthetic activity of many of these agents indicate that antagonism of binding of [3H]BTX-B binding provides a rapid, quantitative, and facile method for the screening and investigation of local anesthetic activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology
  • Adrenergic beta-Antagonists / pharmacology
  • Anesthetics, Local / pharmacology*
  • Animals
  • Batrachotoxins / metabolism*
  • Calcium Channel Blockers / pharmacology
  • Cyclic AMP / biosynthesis
  • Guinea Pigs
  • Histamine H1 Antagonists / pharmacology
  • In Vitro Techniques
  • Ion Channels / metabolism*
  • Neurotoxins / metabolism*
  • Sodium / metabolism*
  • Tranquilizing Agents / pharmacology
  • Tritium


  • Adrenergic alpha-Antagonists
  • Adrenergic beta-Antagonists
  • Anesthetics, Local
  • Batrachotoxins
  • Calcium Channel Blockers
  • Histamine H1 Antagonists
  • Ion Channels
  • Neurotoxins
  • Tranquilizing Agents
  • Tritium
  • batrachotoxinin A 20-alpha-benzoate
  • Sodium
  • Cyclic AMP