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As part of ongoing work aimed at generating proteolytically stable, readily applicable, radiolabeled endomorphin-2 (EM-2) analogs for elucidation of the topological requirements of peptide binding to μ-opioid receptors, we report here on the synthesis, radiolabeling, binding kinetics and binding site distribution of an EM-2 analog in which Pro 2 is replaced by 2-aminocyclohexanecarboxylic...
[ 3 H]Tyr-Tic-(2S,3R)-β-MePhe-Phe-OH (where Tic: 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) with a specific radioactivity of 53.7 Ci/mmol was synthesized and characterized in receptor binding assays at 25°C in rat brain membranes. The specific binding was saturable and displayed high affinity, with a K D of 0.16±0.005nM and B max of 85.9±6.3fmol/mg protein. NaCl increased...
Previously, we have shown that substitution of Pro 2 for cis-2-aminocyclopentanecarboxylic acid, ACPC in endomorphin-2 results in an analogue with greatly augmented proteolytic stability, high μ-opioid receptor affinity and selectivity. We now report the synthesis and biochemical characterization of [ 3 H][(1S,2R)ACPC 2 ]endomorphin-2 with a specific activity of 1.41TBq/mmol...
Naturally occurring isoforms of the decapeptide gonadotropin-releasing hormone (GnRH) share residues 1–4 and 9–10. lGnRH-III, the third isoform isolated in the sea lamprey has no endocrine effect in mammals but shows a direct antiproliferative effect on human breast, prostate and endometrial cancer cell lines. To investigate these features, residues 5–8 of lGnRH-III were systematically replaced with...
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