In vitro and in vivo effects of endothelin-1 and YM598, a selective endothelin ET(A) receptor antagonist, on the lower urinary tract.

In vitro and in vivo effects of endothelin-1 and YM598, a selective endothelin ET(A) receptor antagonist, on the lower urinary tract. Research Abstract Details 

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In vitro and in vivo effects of endothelin-1 and YM598, a selective endothelin ET(A) receptor antagonist, on the lower urinary tract. Abstract Text:

Masashi Ukai,Hironori Yuyama,Akira Fujimori,Akiko Koakutsu,Masanao Sanagi,Akiyoshi Ohtake,Shuichi Sato,Katsumi Sudoh,Masao Sasamata,Keiji Miyata,

We investigated the contractile response of the lower urinary tract to endothelin-1 in vitro (rabbits) and in vivo (dogs). We also assessed the effects of a selective endothelin ET(A) receptor antagonist, (E)-N-[6-methoxy-5-(2-methoxyphenoxy)[2, 2'-bipyrimidin]-4-yl]-2-phenylethenesulfonamide monopotassium salt (YM598), on endothelin-1-induced contractile responses. In the in vitro study, endothelin-1 induced contractile responses in isolated rabbit bladder base, urethra, and prostate tissues. YM598 (10(-7)-10(-5) M) antagonized these endothelin-1-induced contractile responses without affecting the maximal responses. In the in vivo study, endothelin-1 induced the elevation of non-prostatic urethral pressure as well as prostatic urethral pressure even in the presence of tamsulosin (10 mug/kg, i.v.) in anesthetized male dogs. YM598 (0.1-3 mg/kg, i.v.) inhibited these endothelin-1-induced contractile responses in a dose-dependent fashion. These results suggest that endothelin ET(A) receptors play an important role in the lower urinary tract contraction, and that the selective endothelin ET(A) receptor antagonist YM598 has ameliorating effects on various urinary dysfunctions, including benign prostatic hyperplasia.

In vitro and in vivo effects of endothelin-1 and YM598, a selective endothelin ET(A) receptor antagonist, on the lower urinary tract. Publishing Authors By Initials

M Ukai,H Yuyama,A Fujimori,A Koakutsu,M Sanagi,A Ohtake,S Sato,K Sudoh,M Sasamata,K Miyata,

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In vitro and in vivo effects of endothelin-1 and YM598, a selective endothelin ET(A) receptor antagonist, on the lower urinary tract. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: European journal of pharmacology

VOLUME: 580

Page Numbers: 394-400

Journal Abbreviation: Eur. J. Pharmacol.

ISSN: 0014-2999

DAY: 23

MONTH: 11

YEAR: 2007

In vitro and in vivo effects of endothelin-1 and YM598, a selective endothelin ET(A) receptor antagonist, on the lower urinary tract. Information

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LANGUAGE: eng

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AFFILIATION: Applied Pharmacology II, Pharmacology Research Labs., Institute for Drug Discovery Research, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.

Country: Netherlands

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MEDLINETA: Eur J Pharmacol

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