Functional endothelin/sarafotoxin receptors in the rat uterus

D. Bousso-Mittler, Y. Kloog, Z. Wollberg, A. Bdolah, E. Kochva, M. Sokolovsky*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

54 Scopus citations


Functional receptors for the peptides of the endothelin (ET) and sarafotoxin (SRTX) families were detected in the rat uterus. These receptors specifically bind 125I-SRTX-b (Bmax = 220 fmol/mg protein), as well as ET-1, ET-3 and SRTX-c (IC50's 10, 5, 300 and 780 nM, respectively). Activation of the uterine ET/SRTX receptors induced dose-dependent phosphoinositide (PI) hydrolysis and three typical contractile responses: 1) increase in the muscle tonic tension; 2) increase in frequency of the spontaneous rhythmic contractions; 3) decrease of relaxation in each spontaneous rhythmic cycle. All three effects appeared at doses as low as 0.5-1 nM. Dose responses yield ED50 values of 5.5, 30 and 680 nM for ET-1, SRTX-b and ET-3, respectively. SRTX-c was the least effective peptide in achieving decrease in relaxation. In view of these results, and since the uterine responses to the peptides were almost immediate and reversible, we suggest that the functional ET/SRTX receptor of the rat uterus that is coupled to PI hydrolysis may be of physiological significance.

Original languageEnglish
Pages (from-to)952-957
Number of pages6
JournalBiochemical and Biophysical Research Communications
Issue number3
StatePublished - 15 Aug 1989


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