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Binding sites for [3H]tetracaine in synaptosomal sodium channel preparations from mouse brain.

Abstract：

:The present study was an attempt to answer the question whether the local anesthetic [3H]tetracaine labels sodium channels in mouse brain synaptosomes. Binding of [3H]tetracaine had a Kd of 0.19 microM and a Bmax ranging from 3.7 to 5.2 pmol/mg of protein. Local anesthetics other than tetracaine and cocaine-related compounds inhibited [3H]tetracaine binding with Hill numbers between 0.3 and 0.6. Initiation of the dissociation of [3H]tetracaine binding by an excess of unlabeled tetracaine resulted in non-linear curves. These results are consonant with site heterogeneity, negative cooperativity, or complexities arising from the use of synaptosomal preparations instead of broken membranes. There were important differences between the absolute values of the potency of various local anesthetic drugs and cocaine-related compounds in inhibiting binding of [3H]tetracaine and those in inhibiting binding of [3H]batrachotoxinin A 20-alpha-benzoate. Although there were some effects of manipulating the state of the channel with activating toxins on the apparent rate of association and dissociation of [3H]tetracaine binding, the equilibrium binding was not much affected by the toxins. The results indicate that further characterization is necessary before accepting [3H]tetracaine binding as a valid tool for studying sodium channels.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Reith ME,Kim SS,Lajtha A

doi

10.1016/0014-2999(87)90530-9

subject

Has Abstract

pub_date

1987-11-10 00:00:00

pages

171-8

issue

2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(87)90530-9

journal_volume

143

pub_type

杂志文章

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