Differential effects of BQ‐123 against endothelin‐1 and endothelin‐3 on the rat vas deferens: evidence for an atypical endothelin receptor
Open Access
- 19 July 1993
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 109 (3) , 736-738
- https://doi.org/10.1111/j.1476-5381.1993.tb13635.x
Abstract
1 Endothelin-1 and endothelin-3 enhanced concentration-dependently the rat vas deferens twitch response to electrical stimulation, endothelin-1 being three times more potent. Sarafotoxin S6c was at least 200 times less active than endothelin-1. 2 The response to endothelin was antagonized in a competitive manner by the supposedly selective ETA receptor antagonist, BQ-123 (pA2:7.0 ± 0.1). In contrast, the endothelin-1 concentration-response curve was only shifted two fold in the presence of 10 μm BQ-123, while no effect was observed at 1 μm. 3 This evidence suggests the rat vas deferens contains an endothelin receptor not conforming to the ETA/ETB receptor subtype classification so far proposed.Keywords
This publication has 11 references indexed in Scilit:
- Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptorLife Sciences, 1992
- BQ-123, cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu), is a non-competitive antagonist of the actions of endothelin-1 in SK-N-MC human neuroblastoma cellsBiochemical and Biophysical Research Communications, 1992
- Human big‐endothelin‐1 and endothelin‐1 release prostacyclin via the activation of ET1 receptors in the rat perfused lungBritish Journal of Pharmacology, 1992
- Heterogeneity of endothelin‐sarafotoxin receptors mediating contraction of pig coronary arteryBritish Journal of Pharmacology, 1992
- Sarafotoxin S6c: An agonist which distinguishes between endothelin receptor subtypesBiochemical and Biophysical Research Communications, 1991
- Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptorNature, 1990
- Cloning and expression of a cDNA encoding an endothelin receptorNature, 1990
- Specific receptors for endothelin‐3 in cultured bovine endothelial cells and its cellular mechanism of actionFEBS Letters, 1990
- The activity of peptides of the endothelin family in various mammalian smooth muscle preparationsEuropean Journal of Pharmacology, 1989