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• W2022196306 abstract "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 Pro2 is replaced by 2-aminocyclohexanecarboxylic acid, ACHC. [3H][(1S,2R)ACHC]2EM-2 (specific activity 63.49 Ci × mmol−1) bound specifically to its binding sites with high affinity (KD = 0.55 ± 0.06 nM) and saturably, yielding a receptor density, Bmax of 151 ± 4 fmol × mg protein−1 in rat brain membranes. A similar affinity value was obtained in kinetic assays. Both Na+ and Gpp(NH)p decreased the affinity, proving the agonist character of the radioligand. Specific μ-opioid ligands displaced the radioligand with much higher affinities than did δ- and κ-ligands. The autoradiographic distribution of the binding sites of [3H][(1S,2R)ACHC]2EM-2 agreed well with the known locations of the μ-opioid receptors in the rat brain. In consequence of its high affinity, selectivity and enzymatic resistance [19], the new radioligand will be a good tool in studies of the topographical requirements of μ-opioid-specific peptide binding." @default.
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• W2022196306 date "2011-04-01" @default.
• W2022196306 modified "2023-10-17" @default.
• W2022196306 title "Pharmacology of a new tritiated endomorphin-2 analog containing the proline mimetic cis-2-aminocyclohexanecarboxylic acid" @default.
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• W2022196306 doi "https://doi.org/10.1016/j.peptides.2011.01.017" @default.
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