Binding of omega-conotoxin to receptor sites associated with the voltage-sensitive calcium channel.

Abstract:

:The binding of radioiodinated omega-conotoxin GVIA, a probable Ca channel antagonist, to synaptic plasma membranes of rat brain was examined. Two kinds of specific binding sites were found with apparent dissociation constants of 10 pM and 0.5 nM and maximum binding capacities of 0.5 and 3.4 pmol/mg prot., respectively. The binding of the toxin was not affected by high concentrations of Ca antagonists or an agonist, indicating distinct binding sites of the toxin from those of these drugs. Divalent and trivalent metal ions strongly inhibited the binding. The order of their inhibitory potencies was similar to that for inhibition of the Ca current through certain Ca channels. These results suggest that the binding sites of omega-conotoxin GVIA are functionally related to the Ca2+-binding site postulated to be in the pore of the Ca channel.

journal_name

Neurosci Lett

journal_title

Neuroscience letters

authors

Abe T,Koyano K,Saisu H,Nishiuchi Y,Sakakibara S

doi

10.1016/0304-3940(86)90559-8

subject

Has Abstract

pub_date

1986-11-11 00:00:00

pages

203-8

issue

2

eissn

0304-3940

issn

1872-7972

pii

0304-3940(86)90559-8

journal_volume

71

pub_type

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