Antianginal effects of YM430, a novel calcium entry-blocking and β-adrenoceptor-blocking agent in several experimental angina models

Kumiko Shibasaki; Yukinori Arai; Wataru Uchida; Toshio Okazaki; Masaharu Asano; Toichi Takenaka

doi:10.1016/S0306-3623(96)00567-8

Antianginal effects of YM430, a novel calcium entry-blocking and β-adrenoceptor-blocking agent in several experimental angina models

Kumiko Shibasaki, Yukinori Arai, Wataru Uchida, Toshio Okazaki, Masaharu Asano, Toichi Takenaka

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

5 Citations (Scopus)

Abstract

1. We evaluated the antianginal effects of YM430 in several experimental models in vitro and in vivo. 2. In isolated dog. coronary artery, YM430 (10^-8-10^-6 M) inhibited 3,4 diaminopyridine induced rhythmic contractions with an IC₅₀ value of 59.2 nM. 3. In anesthetized rats, YM430 (10-100 mg/kg PO) inhibited arginine vasopressin-induced ST-segment depression with an IC₅₀ value of 36.6 mg/kg PO. 4. In anesthetized dogs, YM430 (0.3 mg/kg IV) significantly inhibited ST-segment elevation induced by coronary artery occlusion. 5. These findings suggest that YM430 may be of value in the treatment of various types of angina pectoris such as variant and stable angina.

Original language	English
Pages (from-to)	545-550
Number of pages	6
Journal	Vascular Pharmacology
Volume	29
Issue number	4
DOIs	https://doi.org/10.1016/S0306-3623(96)00567-8
Publication status	Published - 1997 Oct
Externally published	Yes

Keywords

β-blocker
Antianginal
Calcium antagonist
ST-segment
Vasospasm

ASJC Scopus subject areas

Pharmacology

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10.1016/S0306-3623(96)00567-8

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title = "Antianginal effects of YM430, a novel calcium entry-blocking and β-adrenoceptor-blocking agent in several experimental angina models",

abstract = "1. We evaluated the antianginal effects of YM430 in several experimental models in vitro and in vivo. 2. In isolated dog. coronary artery, YM430 (10-8-10-6 M) inhibited 3,4 diaminopyridine induced rhythmic contractions with an IC50 value of 59.2 nM. 3. In anesthetized rats, YM430 (10-100 mg/kg PO) inhibited arginine vasopressin-induced ST-segment depression with an IC50 value of 36.6 mg/kg PO. 4. In anesthetized dogs, YM430 (0.3 mg/kg IV) significantly inhibited ST-segment elevation induced by coronary artery occlusion. 5. These findings suggest that YM430 may be of value in the treatment of various types of angina pectoris such as variant and stable angina.",

keywords = "β-blocker, Antianginal, Calcium antagonist, ST-segment, Vasospasm",

author = "Kumiko Shibasaki and Yukinori Arai and Wataru Uchida and Toshio Okazaki and Masaharu Asano and Toichi Takenaka",

year = "1997",

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language = "English",

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T1 - Antianginal effects of YM430, a novel calcium entry-blocking and β-adrenoceptor-blocking agent in several experimental angina models

AU - Shibasaki, Kumiko

AU - Arai, Yukinori

AU - Uchida, Wataru

AU - Okazaki, Toshio

AU - Asano, Masaharu

AU - Takenaka, Toichi

PY - 1997/10

Y1 - 1997/10

N2 - 1. We evaluated the antianginal effects of YM430 in several experimental models in vitro and in vivo. 2. In isolated dog. coronary artery, YM430 (10-8-10-6 M) inhibited 3,4 diaminopyridine induced rhythmic contractions with an IC50 value of 59.2 nM. 3. In anesthetized rats, YM430 (10-100 mg/kg PO) inhibited arginine vasopressin-induced ST-segment depression with an IC50 value of 36.6 mg/kg PO. 4. In anesthetized dogs, YM430 (0.3 mg/kg IV) significantly inhibited ST-segment elevation induced by coronary artery occlusion. 5. These findings suggest that YM430 may be of value in the treatment of various types of angina pectoris such as variant and stable angina.

AB - 1. We evaluated the antianginal effects of YM430 in several experimental models in vitro and in vivo. 2. In isolated dog. coronary artery, YM430 (10-8-10-6 M) inhibited 3,4 diaminopyridine induced rhythmic contractions with an IC50 value of 59.2 nM. 3. In anesthetized rats, YM430 (10-100 mg/kg PO) inhibited arginine vasopressin-induced ST-segment depression with an IC50 value of 36.6 mg/kg PO. 4. In anesthetized dogs, YM430 (0.3 mg/kg IV) significantly inhibited ST-segment elevation induced by coronary artery occlusion. 5. These findings suggest that YM430 may be of value in the treatment of various types of angina pectoris such as variant and stable angina.

KW - β-blocker

KW - Antianginal

KW - Calcium antagonist

KW - ST-segment

KW - Vasospasm

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DO - 10.1016/S0306-3623(96)00567-8

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SN - 1537-1891

VL - 29

SP - 545

EP - 550

JO - Vascular Pharmacology

JF - Vascular Pharmacology

IS - 4

ER -

Antianginal effects of YM430, a novel calcium entry-blocking and β-adrenoceptor-blocking agent in several experimental angina models

Abstract

Keywords

ASJC Scopus subject areas

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