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Opiate receptors and their interactions with agnoists and antagonists.
Authors:E J Simon  J M Hiller  I Edelman  J Groth  K D Stahl
Abstract:Independent evidence, derived from studies of the kinetics of receptor inactivation by sulfhydryl reagents, is presented in support of a previously postulated allosteric model of the opiate receptor, in which sodium ions act as effectors. Scatchard analysis provides evidence for cooperative binding, a characteristic of allosteric systems. Both new and old evidence is cited which is consistent with the hypothesis that agonists and antagonists bind to the same receptor sites. These sites can exist in alternative conformations that differ in their relative affinities for agonists and antagonists.
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