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- W2005071795 abstract "The effects of the endothelin receptor antagonist TAK-044 (cyclo[d-α-aspartyl-3-[(4-phenylpiperazin-1-yl)carbonyl]-l-alanyl-l-α-aspartyl-d-2-(2-thienyl)glycyl-l-leucyl-d-tryptop (cyclo[d-Asp-Pro-d-Val-Leu-d-Trp]) were studied in the rat heart to characterize the receptor subtypes responsible for the cardiovascular actions of endothelin-1. Endothelin-1 induced a transient decrease and subsequent increase in perfusion pressure in perfused rat hearts, and increased left ventricular developed pressure. TAK-044 diminished these endothelin-1-induced responses (100 pmol/heart) with IC50 values of 140, 57 and 1.3 nM, respectively. BQ-123 (1–30 μM) partially inhibited the endothelin-1-induced hypertension (30–40%) in the rat heart, and failed to inhibit the hypotension. The positive inotropic effect of endothelin-1 was abolished by BQ-123. Neither indomethacin (10 μM) nor Nω-nitro-l-arginine methyl ester (100 μM) attenuated the endothelin-1-induced hypotension. TAK-044 and BQ-123 attenuated the positive inotropic effect of endothelin-1 in rat papillary muscles. In rat cardiac membrane fractions, TAK-044 and BQ-123 inhibited [125I]endothelin-1 binding to endothelin ETA receptors with IC50 values of 0.39 ± 0.6 and 36 ± 9 nM, respectively, whereas only TAK-044 potently blocked the endothelin ETB receptor subtype (IC50 value: 370 ± 180 nM). These results suggest that endothelin-1 modulates cardiovascular functions in the rat heart by activating both endothelin ETA and endothelin ETB receptors, all of which are sensitive to TAK-044." @default.
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- W2005071795 date "1996-01-01" @default.
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- W2005071795 title "Pharmacological characterization of cardiovascular responses induced by endothelin-1 in the perfused rat heart" @default.
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- W2005071795 doi "https://doi.org/10.1016/0014-2999(95)00680-x" @default.
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