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.
journal_name
Life Scijournal_title
Life sciencesauthors
Nordberg LO,Raffa RB,Tallarida RJdoi
10.1016/0024-3205(93)90682-ssubject
Has Abstractpub_date
1993-01-01 00:00:00pages
PL33-8issue
3eissn
0024-3205issn
1879-0631pii
0024-3205(93)90682-Sjournal_volume
53pub_type
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