Binding of the nonpeptide antagonist, SB 209670, to endothelin receptors on cultured neurons

We studied the binding characteristics of a novel, nonpeptide endothelin antagonist, SB 209670, to two subtypes of endothelin (ET) receptor in cultured rat cerebellar granule cell neurons. Displacement binding studies of [ 125I]ET-1 performed in the presence of the ET B receptor-selective agonist, s...

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Bibliographic Details
Published in:Peptides (New York, N.Y. : 1980) N.Y. : 1980), 1995, Vol.16 (7), p.1279-1282
Main Authors: Lysko, Paul G., Webb, Christine L., Feuerstein, Giora
Format: Article
Language:English
Subjects:
Animals
Binding, Competitive
Cells, Cultured
Cerebellar granule cell
Cerebellum - cytology
Cerebellum - metabolism
Dose-Response Relationship, Drug
Endothelin Receptor Antagonists
Endothelin receptors
Endothelins - metabolism
Indans - metabolism
Neurons - cytology
Neurons - metabolism
Nonpeptide antagonist
Rats
Receptors, Endothelin - metabolism
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Summary:We studied the binding characteristics of a novel, nonpeptide endothelin antagonist, SB 209670, to two subtypes of endothelin (ET) receptor in cultured rat cerebellar granule cell neurons. Displacement binding studies of [ 125I]ET-1 performed in the presence of the ET B receptor-selective agonist, sarafotoxin 6c (S6c), allowed us to measure a K i of 4.0 ± 1.5 n M for (±)SB 209670 at the ET A receptor ( n = 4). Similarly, binding studies in the presence of the ET A receptor-selective antagonist, BQ123, allowed us to measure a K i of 46 ± 14 n M for (±)SB 209670 at the ET B receptor ( n = 4). These studies indicate that the novel endothelin antagonist, SB 209670, has high affinity for both types of neuronal endothelin receptor.
ISSN:0196-9781
1873-5169
DOI:10.1016/0196-9781(95)00096-3