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Identification of leukotriene D4 receptor binding sites in guinea pig lung homogenates using [3H]leukotriene D4
Authors:J B Cheng  R G Townley
Institution:1. Allergic Disease Center, Creighton University, Omaha, Nebraska 68127 USA;2. the Department of Medicine, Creighton University, Omaha, Nebraska 68127 USA;3. the Department of Pharmacology, Creighton University, Omaha, Nebraska 68127 USA
Abstract:We have characterized 3H]leukotriene D4 binding to guinea pig lung homogenates. Both biphasic dissociation kinetics and curvilinear Scatchard plots indicated the presence of 3H]leukotriene high and low affinity states of the binding sites. The rank order of potency for the competition study was leukotriene C4 = leukotriene D4 greater than leukotriene E4 much greater than arachidonic acid, and for their contractile effect on lung strips was leukotriene C4 = leukotriene D4 = leukotriene E4 much greater than arachidonic acid. FPL-55712 was the only other agent tested that inhibited binding. These results suggest that binding of 3H]leukotriene D4 to the homogenate is consistent with its binding to specific leukotriene D4 receptor sites.
Keywords:LT  leukotriene  DMPP  dimethyl-4-phenylpiperazinium  TMB-8  8-(N  N-diethylamino)octyl-2  4  5-trimethoxybenzoate  AA  arachidonic acid
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