Properties of an endothelin-3-sensitive Eta-like endothelin receptor in brain capillary endothelial cells
| Autor: | Denis Guedin, Paul Vigne, Christian Frelin, Julien Desmarets |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
Sodium-Hydrogen Exchangers
Eta receptor Biophysics Capillary endothelial cells Biochemistry Binding Competitive Animals Binding site education Receptor Molecular Biology Volume concentration Etb receptor education.field_of_study Binding Sites Chemistry Receptors Endothelin Endothelins Brain Cell Biology Molecular biology Endothelin 3 Capillaries Rats Kinetics Endothelium Vascular Endothelin receptor |
| Zdroj: | Biochemical and biophysical research communications. 220(3) |
| ISSN: | 0006-291X |
| Popis: | [125I]Et-1 binding experiments showed the presence in rat brain capillary endothelial cells of typical ETA receptors that recognized Et-1, BQ-123 and FR139317 but not IRL1620, [Ala1,3,11,15]Et-1 or Et-3. [125I]Et-3 binding experiments showed that the same cells expressed high affinity Et-3 binding sites (Kd = 1 nM) that recognized Et-1 (Kd = 1 nM), BQ-123 (Kd = 5 nM) and FR139317 (Kd = 2 nM) but not low concentrations of IRL1620 or of [Ala1,3,11,15]Et-1. Et-3 activated Na+/H+exchange activity in a manner that was sensitive to BQ-123 (Ki = 6 nM) and FR 139317 (Ki = 0.6 nM). The results suggest the existence of a high affinity Et-3 receptor that is insensitive to ETB receptor agonists and sensitive to ETA receptor antagonists and that is functionally coupled to Na+/H+exchange activity. |
| Databáze: | OpenAIRE |
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