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• W2024092604 abstract "Abstract The effects of an endothelin (ET)-receptor B-specific antagonist, RES−701−1, on ET-induced contraction of guinea-pig trachea and on ET-induced bronchoconstriction in anaesthetized guinea-pigs were investigated. In the epithelium-removed tracheal preparation, 1 times 10−5 M RES−701−1 inhibited contractions induced by the ETB-specific agonist sarafotoxin S6c (pKB = 6&#x006d;̇10). In the epithelium-intact tracheal preparation, RES−701−1 (1 times 10−5 M) inhibited the ET−3−induced contraction (pKB = 5&#x006d;̇27), but enhanced the ET−1−induced contraction significantly and shifted the concentration-response curve to the left. The maximal responses of ET−1- and ET−3−induced contraction were augmented by epithelium removal by 1&#x006d;̇5 and 1&#x006d;̇8−fold, respectively. Against ET−3−induced contraction in the tracheal preparation without epithelium, RES−701−1 (0&#x006d;̇3−10 times 10−6 M) antagonized the contraction in a concentration-dependent manner (pA2 = 5&#x006d;̇9). On the other hand, RES−701−1 (1 times 10−5 M) did not affect ET−1−evoked responses in the trachea without epithelium. The intravenous administration of ET−1 (1&#x006d;̇5nmol kg−1) or ET−3 (1&#x006d;̇5 nmol kg−1) evoked a biphasic, fast and sustained bronchoconstriction in anaesthetized guinea-pigs pretreated with propranolol (1&#x006d;̇0 mg kg−1). When administered intravenously, RES−701−1 (0&#x006d;̇3 or 1&#x006d;̇0 mg kg−1) showed significant reduction in both phases of bronchoconstriction induced by ET−3. As in the case of ET−1−induced bronchoconstriction, RES−701−1 augmented the sustained phase although a significant reduction of the fast phase was observed. These results indicate that RES−701−1 can inhibit the ET−3−induced airway responses not only in-vitro but also in-vivo." @default.
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• W2024092604 date "1996-01-01" @default.
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• W2024092604 title "Effects of Endothelin B Antagonist RES−701−1 on Endothelin-induced Contractile Responses In-vivo and In-vitro in Guinea-pigs" @default.
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• W2024092604 doi "https://doi.org/10.1111/j.2042-7158.1996.tb05886.x" @default.
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