Effect of YM471, a nonpeptide AVP receptor antagonist, on human coronary artery smooth muscle cells

Atsuo Tahara; Junko Tsukada; Yuichi Tomura; Koh Ichi Wada; Toshiyuki Kusayama; Noe Ishii; Takeyuki Yatsu; Wataru Uchida; Nobuaki Taniguchi; Akihiro Tanaka

doi:10.1016/S0196-9781(02)00138-9

Effect of YM471, a nonpeptide AVP receptor antagonist, on human coronary artery smooth muscle cells

Atsuo Tahara, Junko Tsukada, Yuichi Tomura, Koh Ichi Wada, Toshiyuki Kusayama, Noe Ishii, Takeyuki Yatsu, Wataru Uchida, Nobuaki Taniguchi, Akihiro Tanaka

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

7 Citations (Scopus)

Abstract

The antagonistic properties of YM471, a potent nonpeptide vasopressin (AVP) V_1A and V₂ receptor antagonist, were characterized using human coronary artery smooth muscle cells (CASMC). YM471 potently inhibited specific binding of ³H-AVP to V_1A receptors on human CASMC, exhibiting a K_i value of 0.49 nM. Furthermore, YM471 inhibited the AVP-induced increase in intracellular free Ca²⁺ concentration with an IC₅₀ value of 1.42 nM, but exerted no agonistic activity on CASMC. Additionally, while AVP concentration-dependently induced hyperplasia and hypertrophy in CASMC, YM471 prevented these AVP-induced growth effects, exhibiting IC₅₀ values of 0.93 and 2.64 nM, respectively. These results indicate that YM471 has high affinity for V_1A receptors on, and high potency in inhibiting AVP-induced physiologic responses of, human CASMC.

Original language	English
Pages (from-to)	1809-1816
Number of pages	8
Journal	Peptides
Volume	23
Issue number	10
DOIs	https://doi.org/10.1016/S0196-9781(02)00138-9
Publication status	Published - 2002 Oct 1
Externally published	Yes

Keywords

Coronary artery
Hyperplasia
Hypertrophy
Smooth muscle cells
V receptor
Vasopressin
YM471

ASJC Scopus subject areas

Biochemistry
Physiology
Endocrinology
Cellular and Molecular Neuroscience

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10.1016/S0196-9781(02)00138-9

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title = "Effect of YM471, a nonpeptide AVP receptor antagonist, on human coronary artery smooth muscle cells",

abstract = "The antagonistic properties of YM471, a potent nonpeptide vasopressin (AVP) V1A and V2 receptor antagonist, were characterized using human coronary artery smooth muscle cells (CASMC). YM471 potently inhibited specific binding of 3H-AVP to V1A receptors on human CASMC, exhibiting a Ki value of 0.49 nM. Furthermore, YM471 inhibited the AVP-induced increase in intracellular free Ca2+ concentration with an IC50 value of 1.42 nM, but exerted no agonistic activity on CASMC. Additionally, while AVP concentration-dependently induced hyperplasia and hypertrophy in CASMC, YM471 prevented these AVP-induced growth effects, exhibiting IC50 values of 0.93 and 2.64 nM, respectively. These results indicate that YM471 has high affinity for V1A receptors on, and high potency in inhibiting AVP-induced physiologic responses of, human CASMC.",

keywords = "Coronary artery, Hyperplasia, Hypertrophy, Smooth muscle cells, V receptor, Vasopressin, YM471",

author = "Atsuo Tahara and Junko Tsukada and Yuichi Tomura and Wada, {Koh Ichi} and Toshiyuki Kusayama and Noe Ishii and Takeyuki Yatsu and Wataru Uchida and Nobuaki Taniguchi and Akihiro Tanaka",

year = "2002",

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doi = "10.1016/S0196-9781(02)00138-9",

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T1 - Effect of YM471, a nonpeptide AVP receptor antagonist, on human coronary artery smooth muscle cells

AU - Tahara, Atsuo

AU - Tsukada, Junko

AU - Tomura, Yuichi

AU - Wada, Koh Ichi

AU - Kusayama, Toshiyuki

AU - Ishii, Noe

AU - Yatsu, Takeyuki

AU - Uchida, Wataru

AU - Taniguchi, Nobuaki

AU - Tanaka, Akihiro

PY - 2002/10/1

Y1 - 2002/10/1

N2 - The antagonistic properties of YM471, a potent nonpeptide vasopressin (AVP) V1A and V2 receptor antagonist, were characterized using human coronary artery smooth muscle cells (CASMC). YM471 potently inhibited specific binding of 3H-AVP to V1A receptors on human CASMC, exhibiting a Ki value of 0.49 nM. Furthermore, YM471 inhibited the AVP-induced increase in intracellular free Ca2+ concentration with an IC50 value of 1.42 nM, but exerted no agonistic activity on CASMC. Additionally, while AVP concentration-dependently induced hyperplasia and hypertrophy in CASMC, YM471 prevented these AVP-induced growth effects, exhibiting IC50 values of 0.93 and 2.64 nM, respectively. These results indicate that YM471 has high affinity for V1A receptors on, and high potency in inhibiting AVP-induced physiologic responses of, human CASMC.

AB - The antagonistic properties of YM471, a potent nonpeptide vasopressin (AVP) V1A and V2 receptor antagonist, were characterized using human coronary artery smooth muscle cells (CASMC). YM471 potently inhibited specific binding of 3H-AVP to V1A receptors on human CASMC, exhibiting a Ki value of 0.49 nM. Furthermore, YM471 inhibited the AVP-induced increase in intracellular free Ca2+ concentration with an IC50 value of 1.42 nM, but exerted no agonistic activity on CASMC. Additionally, while AVP concentration-dependently induced hyperplasia and hypertrophy in CASMC, YM471 prevented these AVP-induced growth effects, exhibiting IC50 values of 0.93 and 2.64 nM, respectively. These results indicate that YM471 has high affinity for V1A receptors on, and high potency in inhibiting AVP-induced physiologic responses of, human CASMC.

KW - Coronary artery

KW - Hyperplasia

KW - Hypertrophy

KW - Smooth muscle cells

KW - V receptor

KW - Vasopressin

KW - YM471

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JO - Peptides

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ER -

Effect of YM471, a nonpeptide AVP receptor antagonist, on human coronary artery smooth muscle cells

Abstract

Keywords

ASJC Scopus subject areas

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