(/sup 3/H)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
(/sup 3/H)Batrachotoxinin A benzoate ((/sup 3/H)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 (/sup 3/H)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 (/sup 3/H)BTX-B binding provides a rapid, quantitative, and facile method for the screening and investigation of local anesthetic activity.
- Research Organization:
- National Institute of Arthritis, Bethesda, MD
- OSTI ID:
- 5553891
- Journal Information:
- J. Med. Chem.; (United States), Vol. 28:3
- Country of Publication:
- United States
- Language:
- English
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ANESTHETICS
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GUINEA PIGS
SYMPATHOLYTICS
TOXINS
TRACER TECHNIQUES
TRANQUILIZERS
TRITIUM COMPOUNDS
ALKALI METAL COMPOUNDS
ANIMALS
ANTIGENS
AUTONOMIC NERVOUS SYSTEM AGENTS
CENTRAL NERVOUS SYSTEM AGENTS
CENTRAL NERVOUS SYSTEM DEPRESSANTS
DRUGS
ELECTRICITY
ISOTOPE APPLICATIONS
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LABELLED COMPOUNDS
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MATERIALS
NUCLEOTIDES
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RODENTS
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550501* - Metabolism- Tracer Techniques