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Recently two tetrapeptide ligands that bind preferentially to the μ-opioid receptor were identified and named endomorphin-1 and endomorphin-2. We examined the ability of these peptides to stimulate G protein activation in human μ-opioid receptor transfected B82 fibroblasts as measured by [ 35 S]GTPγS binding to cell membranes. Both endomorphin-1 and -2 act as partial agonists in this...
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