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The neuroendocrine and behavioral effects of Tyr-d-Ala-Gly-Phe-d-Nle-Arg-Phe (DADN), a more stable derivative of the endogenous opiate Met-enkephalin related peptide Met 5 -enkephalin-Arg 6 -Phe 7 were investigated in mice. The behavioral experiments consisted of monitoring the horizontal (square crossing) and vertical (rearing) locomotion in the open field system. To evaluate...
Morphiceptin (Tyr-Pro-Phe-Pro-NH 2 ), a tetrapeptide present in the enzymatic digest of bovine β-casein, is a selective ligand of the μ-opioid receptor. In the present study, we describe the synthesis of a series of novel morphiceptin analogs modified in positions 1–3. Two of the obtained analogs, [Dmt 1 , d-Ala 2 , d-1-Nal 3 ]morphiceptin and [Dmt 1 , d-NMeAla...
A novel opioid peptide antagonist analogue, [ 3 H]Dmt-Tic-(2S,3R)βMePhe-Phe, derived from the potent, δ-receptor selective TIPP tetrapeptide (Tyr-Tic-Phe-Phe) series was synthesized and radiolabeled by catalytic tritiation of its iodinated precursor peptide. The purified radioprobe exhibited a specific activity of 2.15TBq/mmol (58Ci/mmol). The novelty of this compound is that it contains structurally...
Substitution of the Phe 3 aromatic ring in H-Tyr-Ticψ[CH 2 -NH]Phe-Phe-OH with cyclohexylalanine (Cha) has been reported to result in a compound, H-Tyr-Ticψ[CH 2 -NH]Cha-Phe-OH (TICP[ψ]), showing substantially increased δ-opioid antagonist potency and high δ selectivity. TICP[ψ] was radiolabeled by catalytic tritiation of its precursor Tyr(3',5'-I 2 ) 1 TICP[ψ]...
Opioid receptor binding properties of [ 3 H]Tyr-d-Ala-Phe-Phe-NH 2 (TAPP) were characterized in rat brain and Chinese hamster ovary (CHO) cells expressing the rat μ-receptor. In rat brain, [ 3 H]TAPP labeled a single class of opioid sites with a dissociation constant (K d ) of 0.31 nM and maximal number of binding sites (B max ) of 119 fmol/mg protein...
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