Endothelin receptors in human and guinea-pig gallbladder muscle

Shih Che Huang, Ming Che Lee, Chang Kao Wei, Shih Ming Huang

Research output: Contribution to journalArticlepeer-review

24 Citations (Scopus)

Abstract

We measured contraction of muscle strips caused by endothelin (ET) isopeptides and binding of 125I-ET-1 to muscle cell membranes prepared from human and guinea-pig gallbladders. Visualization of 125I-ET-1 binding sites in tissue was performed by autoradiography. Results in human were similar to those in guinea-pig. ET-1 caused tetrodotoxin and atropine-insensitive contraction. The relative potencies for ET isopeptides to cause contraction were ET-1 = ET-2 > ET-3. ET-1 caused contraction was only slightly inhibited by BQ-123 (potent ETA receptor antagonist) and not by BQ-788 (potent ETB receptor antagonist). It was inhibited by the combination of both. Autoradiography localized 125I-ET-1 binding to the smooth muscle layer. Binding of 125I-ET-1 to muscle cell membranes was saturable and specific. Analysis of dose-inhibition curves demonstrated the presence of two classes of receptors. One class (ETA receptor) had a high affinity for ET-1 and ET-2 but a low affinity for ET-3, and the other (ETB receptor) a high affinity for ET-1, ET-2 and ET-3. These results demonstrate that similar to guinea-pig, human gallbladder possesses both ETA and ETB receptors cooperating to mediate muscle contraction.

Original languageEnglish
Pages (from-to)145-153
Number of pages9
JournalRegulatory Peptides
Volume98
Issue number3
DOIs
Publication statusPublished - Apr 20 2001
Externally publishedYes

Keywords

  • Autoradiography
  • Binding
  • Contraction
  • ET
  • Motility

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Clinical Biochemistry
  • Cellular and Molecular Neuroscience

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