Effect of endothelin receptor antagonist, BQ-123, on Ca2+ signaling in cultured rat mesangial cells

Koji Yokokawa; Masakazu Kohno; Machiko Johchi; Takeshi Horio; Koh ichi Murakawa; Kenichi Yasunari; Masashi Yanagisawa; Tadanao Takeda

doi:10.1016/0024-3205(93)90187-8

Effect of endothelin receptor antagonist, BQ-123, on Ca²⁺ signaling in cultured rat mesangial cells

Koji Yokokawa, Masakazu Kohno, Machiko Johchi, Takeshi Horio, Koh ichi Murakawa, Kenichi Yasunari, Masashi Yanagisawa, Tadanao Takeda

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

17 Scopus citations

Abstract

Endothelin (ET)-1 causes mesangial cell contraction and proliferation. The present study was designed to evaluate the functional ET receptor subtype in cultured rat mesangial cells by measuring intracellular Ca²⁺ signaling with the use of a newly synthesized ET receptor type A selective antagonist-BQ123. The ET-1, ET-2 and ET-3 increased intracellular Ca²⁺ level in a dose-dependent manner. BQ-123 suppressed intracellular Ca²⁺ elevation in response to ET-1 in a dose-dependent manner with its half maximal inhibition value of 28 nM. BQ-123 (10^-6 M) did not affect ET-3 (10^-7 M)-induced Ca²⁺ response. The peak Ca²⁺ levels after addition of ET-3 without BQ-123 were similar to those in response to ET-1, ET-2 and ET-3 in the presence of BQ-123. Northern bolt analysis showed that cultured mesangial cells expressed both ET_A and ET_B receptor mRNA. These results suggest that cultured mesangial cells have, at least, two types of functional receptors, one of which is an ET_A receptor.

Original language	English (US)
Pages (from-to)	1631-1641
Number of pages	11
Journal	Life Sciences
Volume	53
Issue number	21
DOIs	https://doi.org/10.1016/0024-3205(93)90187-8
State	Published - 1993

ASJC Scopus subject areas

General Pharmacology, Toxicology and Pharmaceutics
General Biochemistry, Genetics and Molecular Biology

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10.1016/0024-3205(93)90187-8

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@article{c8766c7826be48b1883da81d6bee1d10,

title = "Effect of endothelin receptor antagonist, BQ-123, on Ca2+ signaling in cultured rat mesangial cells",

abstract = "Endothelin (ET)-1 causes mesangial cell contraction and proliferation. The present study was designed to evaluate the functional ET receptor subtype in cultured rat mesangial cells by measuring intracellular Ca2+ signaling with the use of a newly synthesized ET receptor type A selective antagonist-BQ123. The ET-1, ET-2 and ET-3 increased intracellular Ca2+ level in a dose-dependent manner. BQ-123 suppressed intracellular Ca2+ elevation in response to ET-1 in a dose-dependent manner with its half maximal inhibition value of 28 nM. BQ-123 (10-6 M) did not affect ET-3 (10-7 M)-induced Ca2+ response. The peak Ca2+ levels after addition of ET-3 without BQ-123 were similar to those in response to ET-1, ET-2 and ET-3 in the presence of BQ-123. Northern bolt analysis showed that cultured mesangial cells expressed both ETA and ETB receptor mRNA. These results suggest that cultured mesangial cells have, at least, two types of functional receptors, one of which is an ETA receptor.",

author = "Koji Yokokawa and Masakazu Kohno and Machiko Johchi and Takeshi Horio and Murakawa, {Koh ichi} and Kenichi Yasunari and Masashi Yanagisawa and Tadanao Takeda",

note = "Funding Information: We greatly express our gratitude to Dr. Fumihiko Ikemoto, PhD. and Dr. Mitsuo Yano, PhD. of New Drug Discovery Research Laboratories, Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan for their advice and gifting BQ-123. We also greatly thanks to Dr. Michael Simonson, Division of Nephrology, Department of Medicine, Case Western Reserve University, University Hospitals of Cleveland, Ohio, for his valuable advice for Northern analysis. This study was supported by a grant of Osaka Heart Club and Uehara Memorial Foundation.",

year = "1993",

doi = "10.1016/0024-3205(93)90187-8",

language = "English (US)",

volume = "53",

pages = "1631--1641",

journal = "Life Sciences",

issn = "0024-3205",

publisher = "Elsevier Inc.",

number = "21",

}

TY - JOUR

T1 - Effect of endothelin receptor antagonist, BQ-123, on Ca2+ signaling in cultured rat mesangial cells

AU - Yokokawa, Koji

AU - Kohno, Masakazu

AU - Johchi, Machiko

AU - Horio, Takeshi

AU - Murakawa, Koh ichi

AU - Yasunari, Kenichi

AU - Yanagisawa, Masashi

AU - Takeda, Tadanao

N1 - Funding Information: We greatly express our gratitude to Dr. Fumihiko Ikemoto, PhD. and Dr. Mitsuo Yano, PhD. of New Drug Discovery Research Laboratories, Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan for their advice and gifting BQ-123. We also greatly thanks to Dr. Michael Simonson, Division of Nephrology, Department of Medicine, Case Western Reserve University, University Hospitals of Cleveland, Ohio, for his valuable advice for Northern analysis. This study was supported by a grant of Osaka Heart Club and Uehara Memorial Foundation.

PY - 1993

Y1 - 1993

N2 - Endothelin (ET)-1 causes mesangial cell contraction and proliferation. The present study was designed to evaluate the functional ET receptor subtype in cultured rat mesangial cells by measuring intracellular Ca2+ signaling with the use of a newly synthesized ET receptor type A selective antagonist-BQ123. The ET-1, ET-2 and ET-3 increased intracellular Ca2+ level in a dose-dependent manner. BQ-123 suppressed intracellular Ca2+ elevation in response to ET-1 in a dose-dependent manner with its half maximal inhibition value of 28 nM. BQ-123 (10-6 M) did not affect ET-3 (10-7 M)-induced Ca2+ response. The peak Ca2+ levels after addition of ET-3 without BQ-123 were similar to those in response to ET-1, ET-2 and ET-3 in the presence of BQ-123. Northern bolt analysis showed that cultured mesangial cells expressed both ETA and ETB receptor mRNA. These results suggest that cultured mesangial cells have, at least, two types of functional receptors, one of which is an ETA receptor.

AB - Endothelin (ET)-1 causes mesangial cell contraction and proliferation. The present study was designed to evaluate the functional ET receptor subtype in cultured rat mesangial cells by measuring intracellular Ca2+ signaling with the use of a newly synthesized ET receptor type A selective antagonist-BQ123. The ET-1, ET-2 and ET-3 increased intracellular Ca2+ level in a dose-dependent manner. BQ-123 suppressed intracellular Ca2+ elevation in response to ET-1 in a dose-dependent manner with its half maximal inhibition value of 28 nM. BQ-123 (10-6 M) did not affect ET-3 (10-7 M)-induced Ca2+ response. The peak Ca2+ levels after addition of ET-3 without BQ-123 were similar to those in response to ET-1, ET-2 and ET-3 in the presence of BQ-123. Northern bolt analysis showed that cultured mesangial cells expressed both ETA and ETB receptor mRNA. These results suggest that cultured mesangial cells have, at least, two types of functional receptors, one of which is an ETA receptor.

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SN - 0024-3205

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JO - Life Sciences

JF - Life Sciences

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ER -

Effect of endothelin receptor antagonist, BQ-123, on Ca²⁺ signaling in cultured rat mesangial cells

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