Dopamine Receptor Binding in Bovine Intermediate Lobe Pituitary Membranes
作者： DAVID R. SIBLEY , IAN CREESE
关键词: Stereochemistry 、 Membrane 、 Antagonist 、 Endocrinology 、 Dopamine receptor binding 、 Dissociation constant 、 Agonist 、 Dopamine receptor 、 Internal medicine 、 Chemistry 、 GTP' 、 Binding site
摘要: [3H]Spiroperidol ([3H]SPIRO) and [3H]N-n-propylnorapomorphine ([3H]NPA), a dopamine antagonist agonist, respectively, were found to bind stereospecifically bovine intermediate lobe pituitary membranes. The specific binding was saturable ([3H]SPIRO maximum number of sites, 11.2 pmol/g tissue; [3H]NPA 5.0 tissue) high affinity dissociation constant, 0.17 nM; 0.35 M). rank order catecholamines, phenothiazines, related drugs in competing for [3H]SPIRO is consistent with interactions at receptor. Guanine nucleotides selectively decrease agonist but not affinities these sites. With the addition 0.1 mM GTP, ability agonists displace decreased 5 7-fold, while constant increased 0.8 nM.
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