Rapid communicationInverse agonism by Dmt–Tic analogues and HS 378, a naltrindole analogue
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Cited by (28)
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists
2015, Bioorganic and Medicinal Chemistry LettersOpioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic
2011, European Journal of Medicinal ChemistryCitation Excerpt :iii) Finally, compounds 4 and 5 are made up of an ester linkage between pharmacophores (cleavable bivalent ligands), that after administration can be metabolized to the single pharmacophores [morphine and Dmt-Tic-(β-Ala)] characterized by a different pharmacological profile in comparison to the bifunctional ligands 4 and 5. For this reason, such ligands could be of potential utility in the opioid receptor trafficking and related pharmacological studies [19–21]. Crude peptides and pseudopeptides were purified by preparative reversed-phase HPLC [Waters Delta Prep 4000 system with Waters Prep LC 40 mm Assembly column C18 (30 cm × 4 cm, 15 μm particle)] and eluted at a flow rate of 20 mL/min with mobile phase solvent A (10% acetonitrile + 0.1% TFA in H2O, v/v), and a linear gradient from 10 to 60% B (60%, acetonitrile + 0.1% TFA in H2O, v/v) in 25 min.
Non-peptidic δ-opioid receptor antagonists suppress mitogen-induced tryptophan degradation in peripheral blood mononuclear cells in vitro
2008, Immunology LettersCitation Excerpt :Using genetic tools, it was demonstrated that the immunosuppressive actions of the δ-opioid receptor antagonist in murine spleen cells are not mediated by any of the three μ-, δ- or κ-opioid receptors [21]. Two analogues of NTI, HS-378 (17-cyclopropylmethyl-4,5α-epoxy-14β-ethoxy-5β-methylindolo[2′,3′:6,7]morphinan-3-ol hydrochloride) and HS-459 (17-cyclopropylmethyl-4,5α-epoxy-14β-methoxy-5β-methylindolo[2′,3′:6,7]morphinan-3-ol hydrochloride (Fig. 1) have been described to display greater selectivity toward the δ-opioid receptor than NTI and mediate high antagonistic activity [23–27]. In vitro and in vivo studies have demonstrated the ability of HS-378 to selectively antagonize δ-opioid receptor agonist-induced effects [28–30].
Study of disabling T-cell activation and inhibiting T-cell-mediated immunopathology reveals a possible inverse agonist activity of CD4 peptidomimetics
2002, Experimental and Molecular Pathology