Two types of endothelin B receptors mediating relaxation in the guinea pig ileum

Masatoshi Hori; Sri Agus Sudjarwo; Kyoko Oda; Yoshihiro Urade; Hideaki Karaki

doi:10.1016/0024-3205(94)00547-8

Two types of endothelin B receptors mediating relaxation in the guinea pig ileum

Masatoshi Hori, Sri Agus Sudjarwo, Kyoko Oda, Yoshihiro Urade, Hideaki Karaki

Research output: Contribution to journal › Article › peer-review

31 Citations (Scopus)

Abstract

In guinea pig ileum, binding assays showed the existence of endothelin (ET) receptors of ET_A (isopeptide-selective) and ET_B (nonselective) subtypes. ETs induced relaxation followed by contraction. ET-1 induced greater contraction at lower concentrations than ET-3. An ET_A antagonist, BQ-123, shifted the concentration-response curves for ETs to the right. An ET_B antagonist, IRL 1038, shifted the concentration-response curve for ET-3 to the right and downwards with little effect on the curve for ET-1. In contrast, ET-1 and ET-3 induced relaxation at similar concentrations. The relaxation induced by ETs was composed of an initial transient relaxation followed by sustained relaxation. Only the transient phase was inhibited by IRL 1038 in a concentration-dependent manner. These results suggest that the ET-induced relaxation is mediated by two types of ET_B receptor; transient and sustained relaxations are mediated respectively by IRL 1038-sensitive and IRL 1038-insensitive subtypes of ET_B receptor. In contrast, the contractile effect seems to be mediated mainly by the ET_A receptor and partially by an IRL 1038-sensitive subtype of ET_B receptor.

Original language	English
Pages (from-to)	645-652
Number of pages	8
Journal	Life Sciences
Volume	54
Issue number	10
DOIs	https://doi.org/10.1016/0024-3205(94)00547-8
Publication status	Published - 1994
Externally published	Yes

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@article{b9eb841ac6b3498681ca8e780c7465e4,

title = "Two types of endothelin B receptors mediating relaxation in the guinea pig ileum",

abstract = "In guinea pig ileum, binding assays showed the existence of endothelin (ET) receptors of ETA (isopeptide-selective) and ETB (nonselective) subtypes. ETs induced relaxation followed by contraction. ET-1 induced greater contraction at lower concentrations than ET-3. An ETA antagonist, BQ-123, shifted the concentration-response curves for ETs to the right. An ETB antagonist, IRL 1038, shifted the concentration-response curve for ET-3 to the right and downwards with little effect on the curve for ET-1. In contrast, ET-1 and ET-3 induced relaxation at similar concentrations. The relaxation induced by ETs was composed of an initial transient relaxation followed by sustained relaxation. Only the transient phase was inhibited by IRL 1038 in a concentration-dependent manner. These results suggest that the ET-induced relaxation is mediated by two types of ETB receptor; transient and sustained relaxations are mediated respectively by IRL 1038-sensitive and IRL 1038-insensitive subtypes of ETB receptor. In contrast, the contractile effect seems to be mediated mainly by the ETA receptor and partially by an IRL 1038-sensitive subtype of ETB receptor.",

author = "Masatoshi Hori and Sudjarwo, {Sri Agus} and Kyoko Oda and Yoshihiro Urade and Hideaki Karaki",

note = "Funding Information: We are grateful to Drs. T. Okada and A. F. James, Ciba-Geigy Japan, for helpful discussion and critical reading of the manuscript. This work was supported by Grant-in-Aid for Scientific Research from the Ministry of Education, Science and Culture, Japan.",

year = "1994",

doi = "10.1016/0024-3205(94)00547-8",

language = "English",

volume = "54",

pages = "645--652",

journal = "Life Sciences",

issn = "0024-3205",

publisher = "Elsevier Inc.",

number = "10",

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TY - JOUR

T1 - Two types of endothelin B receptors mediating relaxation in the guinea pig ileum

AU - Hori, Masatoshi

AU - Sudjarwo, Sri Agus

AU - Oda, Kyoko

AU - Urade, Yoshihiro

AU - Karaki, Hideaki

N1 - Funding Information: We are grateful to Drs. T. Okada and A. F. James, Ciba-Geigy Japan, for helpful discussion and critical reading of the manuscript. This work was supported by Grant-in-Aid for Scientific Research from the Ministry of Education, Science and Culture, Japan.

PY - 1994

Y1 - 1994

N2 - In guinea pig ileum, binding assays showed the existence of endothelin (ET) receptors of ETA (isopeptide-selective) and ETB (nonselective) subtypes. ETs induced relaxation followed by contraction. ET-1 induced greater contraction at lower concentrations than ET-3. An ETA antagonist, BQ-123, shifted the concentration-response curves for ETs to the right. An ETB antagonist, IRL 1038, shifted the concentration-response curve for ET-3 to the right and downwards with little effect on the curve for ET-1. In contrast, ET-1 and ET-3 induced relaxation at similar concentrations. The relaxation induced by ETs was composed of an initial transient relaxation followed by sustained relaxation. Only the transient phase was inhibited by IRL 1038 in a concentration-dependent manner. These results suggest that the ET-induced relaxation is mediated by two types of ETB receptor; transient and sustained relaxations are mediated respectively by IRL 1038-sensitive and IRL 1038-insensitive subtypes of ETB receptor. In contrast, the contractile effect seems to be mediated mainly by the ETA receptor and partially by an IRL 1038-sensitive subtype of ETB receptor.

AB - In guinea pig ileum, binding assays showed the existence of endothelin (ET) receptors of ETA (isopeptide-selective) and ETB (nonselective) subtypes. ETs induced relaxation followed by contraction. ET-1 induced greater contraction at lower concentrations than ET-3. An ETA antagonist, BQ-123, shifted the concentration-response curves for ETs to the right. An ETB antagonist, IRL 1038, shifted the concentration-response curve for ET-3 to the right and downwards with little effect on the curve for ET-1. In contrast, ET-1 and ET-3 induced relaxation at similar concentrations. The relaxation induced by ETs was composed of an initial transient relaxation followed by sustained relaxation. Only the transient phase was inhibited by IRL 1038 in a concentration-dependent manner. These results suggest that the ET-induced relaxation is mediated by two types of ETB receptor; transient and sustained relaxations are mediated respectively by IRL 1038-sensitive and IRL 1038-insensitive subtypes of ETB receptor. In contrast, the contractile effect seems to be mediated mainly by the ETA receptor and partially by an IRL 1038-sensitive subtype of ETB receptor.

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U2 - 10.1016/0024-3205(94)00547-8

DO - 10.1016/0024-3205(94)00547-8

M3 - Article

C2 - 8107509

AN - SCOPUS:0028333642

SN - 0024-3205

VL - 54

SP - 645

EP - 652

JO - Life Sciences

JF - Life Sciences

IS - 10

ER -

Two types of endothelin B receptors mediating relaxation in the guinea pig ileum

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