PMID: 8959749Jan 1, 1996Paper

Pharmacological characterization of the ETA receptor in the vascular smooth muscle comparing its analogous distribution in the rat mesenteric artery and in the arterial mesenteric bed

Peptides
M Veronica DonosoJ P Huidobro-Toro

Abstract

The potency of ET-1, ET-2, and ET-3 to contract the isolated perfused rat arterial mesenteric bed was 2.73 +/- 0.57, 1.63 +/- 0.32, and 144 +/- 30 nM, respectively. The vasomotor effect of the ETs was slow in onset, persistent but reversible. Sarafotoxin S6b mimicked the ETs with a potency twofold lower than ET-1; sarafotoxin S6c and the C-terminal hexapeptide of ET-1 was inactive. ETH agonists such as IRL-1620 and AGETB-89 were inactive as vasoconstrictors within the range of concentrations examined. Minor chemical modifications of ET-1 amino acids residues in position 7 or 21 decreased significantly the peptide potency; ET-1 analogues with one or none of the disulfide bonds resulted inactive. The vasomotor effect of ETs was blocked in a competitive, reversible, and selective manner by FR 139317 and BQ-123, the latter being about threefold less potent than the former antagonist. The potency of FR 139317 was 20-fold higher to antagonize ET-3 than ET-1, and threefold higher to block ET-2 than ET-1. In strict analogy to FR 139317, BQ-123 was 12-fold more potent to antagonize ET-3 than ET-1, and fourfold more potent to antagonize ET-2 than ET-1. Upon removal of the endothelial cell layer, the vasomotor potency of ET-1 or the antag...Continue Reading

References

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Citations

Oct 30, 2001·British Journal of Pharmacology·X F FigueroaJ P Huidobro-Toro
Jul 12, 2002·British Journal of Pharmacology·Sonja BuvinicJ Pablo Huidobro-Toro
Feb 14, 2012·British Journal of Pharmacology·M G CompeerJ G R De Mey
Mar 13, 2012·Life Sciences·Matthijs G CompeerJo G R De Mey
Mar 4, 2000·The Journal of Laryngology and Otology·S A MonemM C Frampton
Sep 14, 1999·The American Journal of Physiology·M P BoricJ P Huidobro-Toro
Jul 28, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Camila Calfío, Juan Pablo Huidobro-Toro
Jun 9, 2005·The Journal of Experimental Biology·B McNeill, S F Perry

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