Characterization of endothelin-A receptors in the cerebral circulation
- 1 April 1993
- journal article
- research article
- Published by Wolters Kluwer Health in NeuroReport
- Vol. 4 (4) , 441-443
- https://doi.org/10.1097/00001756-199304000-00026
Abstract
ENDOTHELIN-1 (ET-1), a 21-amino acid peptide produced by the vascular endothelium, mediates contraction. In the present study we demonstrate that both ET-1 (Emax: 238 × 29% of potassium contraction) and ET-2 (Emax: 231 × 36%) produce strong concentration-dependent contractions of circular segments of guinea-pig middle cerebral artery, whereas ET-3 has only weak effects (Emax: 32 × 13%). FR 139317 (10–6 M), a selective endothelinA (ETA) receptor antagonist, shifted the ET-1 response curve to the right (pD2:7.86 × 0.09 with and 8.76 × 0.09 without the antagonist) in a competitive manner (pA2 = 6.83). These findings are the first to show the presence of ETA receptors in cerebral vessels.Keywords
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