Multiple subtypes of endothelin receptors in porcine tissues

characterization by ligand binding, affinity labeling and regional distribution

Ryoichi Takayanagi, Ohnaka Keizo, Chikahisa Takasaki, Masao Ohashi, Hajime Nawata

Research output: Contribution to journalArticle

49 Citations (Scopus)

Abstract

To clarify the existence and the distribution of endothelin (ET) receptor subtypes, we have examined the pharmacological properties and the molecular weight (Mr) of 125I-ET-1 and 125I-ET-3 binding sites in various tissues of pigs. ET-1 and ET-2 showed almost identical potencies in displacing the bound 125I-ET-1 in all the tissues examined. ET-3, sarafotoxin S6b (SRT-b) and sarafotoxin S6c (SRT-c) displaced the 125I-ET-1 with the same sensitivity as ET-1 (IC50 = 0.1-1.4 nM) in brain, kidney, liver and adrenal, whereas the three peptides showed very weak competition (IC50 = 40-500 nM) against 125I-ET-1 binding in cardiac atria, aorta, lung, stomach and uterus. The computer analyses of the binding data suggested the presence of high (Kd1 = 0.04-0.29 nM) and low (Kd2 = 60-190 nM) affinity binding sites for ET-3 and SRT-b in lung and stomach. 125I-ET-3 bound to the high affinity sites in lung and stomach was displaced by ET/SRT isopeptides almost equipotently. Two proteins with Mr of 47,000 and 35,000 were affinity-labeled with 125I-ET-1 in cerebellum, while a protein with Mr of 123,000, in addition to the two proteins, was predominantly labeled in lung. The above findings indicated that two distinct subclasses of ET receptors, namely, ET-1-specific and ET/SRT family-common receptors were distributed in various proportions in mammalian tissues, and suggested that their molecular forms are also different.

Original languageEnglish
Pages (from-to)23-37
Number of pages15
JournalRegulatory Peptides
Volume32
Issue number1
DOIs
Publication statusPublished - Jan 1 1991

Fingerprint

Endothelin Receptors
Endothelin-1
Labeling
Swine
Endothelin-3
Tissue
Ligands
Lung
Stomach
Endothelins
Inhibitory Concentration 50
Binding Sites
Endothelin-2
Proteins
Liver
Cerebellum
Uterus
Aorta
Brain
Molecular Weight

All Science Journal Classification (ASJC) codes

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

Cite this

Multiple subtypes of endothelin receptors in porcine tissues : characterization by ligand binding, affinity labeling and regional distribution. / Takayanagi, Ryoichi; Keizo, Ohnaka; Takasaki, Chikahisa; Ohashi, Masao; Nawata, Hajime.

In: Regulatory Peptides, Vol. 32, No. 1, 01.01.1991, p. 23-37.

Research output: Contribution to journalArticle

Takayanagi, Ryoichi ; Keizo, Ohnaka ; Takasaki, Chikahisa ; Ohashi, Masao ; Nawata, Hajime. / Multiple subtypes of endothelin receptors in porcine tissues : characterization by ligand binding, affinity labeling and regional distribution. In: Regulatory Peptides. 1991 ; Vol. 32, No. 1. pp. 23-37.
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