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- W2001897914 abstract "An in vitro preparation of rabbit thoracic aorta was tested in order to determine whether isometric contractile force induced by endothelin-1 (ET-1) in this preparation is changed when the tissue is exposed to ultraviolet (UV) light. After constriction of an aortic segment to a steady-state level of tension with ET-1, a flash of UV light induced a transient decrease in tension that returned exponentially to equilibrium. This response was endothelium-independent and sensitive to the extracellular sodium concentration. The rate of return to the baseline tension after photorelaxation increased with increasing concentrations of ET-1. UV light had only a slight photorelaxing effect at very low and very high ET-1 concentrations and a much larger effect at concentrations near the A50 value of ET-1. Since an irreversible antagonist does not yet exist for ET-1, the partial irreversible blockade method for getting the dissociation constant (KD) functionally was not possible. The relaxation method, using UV light as a perturbation of ligand-receptor equilibrium, was used instead to obtain KD as well as the forward (k1) and reverse (k2) rate constants of ET-1 in this tissue." @default.
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- W2001897914 date "1993-01-01" @default.
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- W2001897914 title "Determination of the drug-receptor dissociation constant of endothelin-1 using photorelaxation of rabbit isolated thoracic aorta" @default.
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- W2001897914 doi "https://doi.org/10.1016/0024-3205(93)90682-s" @default.
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