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Asymmetric synthesis and in vitro and in vivo activity of tetrahydroquinolines featuring a diverse set of polar substitutions at the 6 position as mixed-efficacy μ opioid receptor/δ opioid receptor ligands.
Bender AM, Griggs NW, Anand JP, Traynor JR, Jutkiewicz EM, Mosberg HI. Bender AM, et al. Among authors: mosberg hi. ACS Chem Neurosci. 2015 Aug 19;6(8):1428-35. doi: 10.1021/acschemneuro.5b00100. Epub 2015 May 13. ACS Chem Neurosci. 2015. PMID: 25938166 Free PMC article.
Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.
Harland AA, Yeomans L, Griggs NW, Anand JP, Pogozheva ID, Jutkiewicz EM, Traynor JR, Mosberg HI. Harland AA, et al. Among authors: mosberg hi. J Med Chem. 2015 Nov 25;58(22):8952-69. doi: 10.1021/acs.jmedchem.5b01270. Epub 2015 Nov 13. J Med Chem. 2015. PMID: 26524472 Free PMC article.
Synthesis and Pharmacological Evaluation of Novel C-8 Substituted Tetrahydroquinolines as Balanced-Affinity Mu/Delta Opioid Ligands for the Treatment of Pain.
Nastase AF, Griggs NW, Anand JP, Fernandez TJ, Harland AA, Trask TJ, Jutkiewicz EM, Traynor JR, Mosberg HI. Nastase AF, et al. Among authors: mosberg hi. ACS Chem Neurosci. 2018 Jul 18;9(7):1840-1848. doi: 10.1021/acschemneuro.8b00139. Epub 2018 May 2. ACS Chem Neurosci. 2018. PMID: 29677442 Free PMC article.
Novel Dimethyltyrosine-Tetrahydroisoquinoline Peptidomimetics with Aromatic Tetrahydroisoquinoline Substitutions Show in Vitro Kappa and Mu Opioid Receptor Agonism.
Montgomery D, Anand JP, Griggs NW, Fernandez TJ, Hartman JG, Sánchez-Santiago AA, Pogozheva ID, Traynor JR, Mosberg HI. Montgomery D, et al. Among authors: mosberg hi. ACS Chem Neurosci. 2019 Aug 21;10(8):3682-3689. doi: 10.1021/acschemneuro.9b00250. Epub 2019 Jul 1. ACS Chem Neurosci. 2019. PMID: 31199621 Free PMC article.
Aromatic-Amine Pendants Produce Highly Potent and Efficacious Mixed Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Peptidomimetics with Enhanced Metabolic Stability.
Henry S, Anand JP, Twarozynski JJ, Brinkel AC, Pogozheva ID, Sears BF, Jutkiewicz EM, Traynor JR, Mosberg HI. Henry S, et al. Among authors: mosberg hi. J Med Chem. 2020 Feb 27;63(4):1671-1683. doi: 10.1021/acs.jmedchem.9b01818. Epub 2020 Feb 10. J Med Chem. 2020. PMID: 31986033 Free PMC article.
168 results