Low-Efficacy Mu Opioid Agonists as Candidate Analgesics: Effects of Novel C-9 Substituted Phenylmorphans on Pain-Depressed Behavior in Mice.

Autor: Santos EJ; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Akbarali HI; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Bow EW; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Chambers DR; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Gutman ES; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Jacobson AE; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Kang M; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Lee YK; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Lutz JA; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Rice KC; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Sulima A; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.)., Negus SS; Department of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.) sidney.negus@vcuhealth.org.

Publikováno v: The Journal of pharmacology and experimental therapeutics [J Pharmacol Exp Ther] 2024 Oct 18; Vol. 391 (2), pp. 138-151. Date of Electronic Publication: 2024 Oct 18.

Enhancing Protective Antibodies against Opioids through Antigen Display on Virus-like Particles.

Autor: Shafieichaharberoud F; Department of Chemistry, Michigan State University, 578 S. Shaw Lane, East Lansing, Michigan 48824, United States.; Institute for Quantitative Health Science and Engineering, Michigan State University, East Lansing, Michigan 48824, United States., Lang S; Department of Chemistry, Michigan State University, 578 S. Shaw Lane, East Lansing, Michigan 48824, United States.; Institute for Quantitative Health Science and Engineering, Michigan State University, East Lansing, Michigan 48824, United States., Whalen C; Laboratory of Adjuvant and Antigen Research, U.S. Military HIV Research Program, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States., Rivera Quiles C; Department of Physiology and Neuroscience Program, Michigan State University, East Lansing, Michigan 48824, United States., Purcell L; Department of Chemistry, Michigan State University, 578 S. Shaw Lane, East Lansing, Michigan 48824, United States., Talbot C; Department of Chemistry, Michigan State University, 578 S. Shaw Lane, East Lansing, Michigan 48824, United States.; Institute for Quantitative Health Science and Engineering, Michigan State University, East Lansing, Michigan 48824, United States., Wang P; Department of Chemistry, University of Alabama at Birmingham, Birmingham, Alabama 35294, United States., Norton EB; Department of Microbiology & Immunology, Tulane University School of Medicine, New Orleans, Louisiana 70112, United States., Mazei-Robison M; Department of Physiology and Neuroscience Program, Michigan State University, East Lansing, Michigan 48824, United States., Sulima A; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland 20892, United States., Jacobson AE; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland 20892, United States., Rice KC; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland 20892, United States., Matyas GR; Laboratory of Adjuvant and Antigen Research, U.S. Military HIV Research Program, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States., Huang X; Department of Chemistry, Michigan State University, 578 S. Shaw Lane, East Lansing, Michigan 48824, United States.; Institute for Quantitative Health Science and Engineering, Michigan State University, East Lansing, Michigan 48824, United States.; Department of Biomedical Engineering, Michigan State University, East Lansing, Michigan 48824, United States.

Publikováno v: Bioconjugate chemistry [Bioconjug Chem] 2024 Feb 21; Vol. 35 (2), pp. 164-173. Date of Electronic Publication: 2023 Dec 19.

Role of efficacy as a determinant of locomotor activation by mu-opioid receptor (MOR) ligands in female and male mice. II. Effects of novel MOR-selective phenylmorphans with high-to-low MOR efficacy.

Autor: Santos EJ; Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA., Nassehi N; Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA., Bow EW; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA., Chambers DR; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA., Gutman ES; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA., Jacobson AE; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA., Lutz JA; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA., Marsh SA; Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA., Rice KC; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA., Sulima A; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA., Selley DE; Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA., Negus SS; Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA.

Publikováno v: Pharmacology research & perspectives [Pharmacol Res Perspect] 2023 Aug; Vol. 11 (4), pp. e01111.

Discovery of a Potent Highly Biased MOR Partial Agonist among Diastereomeric C9-Hydroxyalkyl-5-phenylmorphans.

Autor: Lutz JA; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892-3373, USA., Sulima A; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892-3373, USA., Gutman ES; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892-3373, USA., Bow EW; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892-3373, USA., Luo D; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone Street, Lexington, KY 40536, USA., Kaska S; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone Street, Lexington, KY 40536, USA., Prisinzano TE; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone Street, Lexington, KY 40536, USA., Paronis CA; McLean Hospital/Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA., Bergman J; McLean Hospital/Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA., Imler GH; Center for Biomolecular Science and Engineering, Naval Research Laboratory, Washington, DC 20375-0001, USA., Kerr AT; Center for Biomolecular Science and Engineering, Naval Research Laboratory, Washington, DC 20375-0001, USA., Jacobson AE; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892-3373, USA., Rice KC; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892-3373, USA.

Publikováno v: Molecules (Basel, Switzerland) [Molecules] 2023 Jun 15; Vol. 28 (12). Date of Electronic Publication: 2023 Jun 15.

A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists.

Autor: Chambers DR; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892, USA., Sulima A; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892, USA., Luo D; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone Street, Lexington, KY 40536, USA., Prisinzano TE; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone Street, Lexington, KY 40536, USA., Goldberg A; Computational Chemistry and Molecular Biophysics Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, 333 Cassell Drive, Baltimore, MD 21224, USA., Xie B; Computational Chemistry and Molecular Biophysics Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, 333 Cassell Drive, Baltimore, MD 21224, USA., Shi L; Computational Chemistry and Molecular Biophysics Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, 333 Cassell Drive, Baltimore, MD 21224, USA., Paronis CA; McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA., Bergman J; McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA., Nassehi N; Department of Pharmacology and Toxicology, Virginia Commonwealth University, 1112 East Clay Street, Richmond, VA 23298, USA., Selley DE; Department of Pharmacology and Toxicology, Virginia Commonwealth University, 1112 East Clay Street, Richmond, VA 23298, USA., Imler GH; Naval Research Laboratory, Center for Biomolecular Science and Engineering, Washington, DC 20375, USA., Jacobson AE; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892, USA., Rice KC; Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892, USA.

Publikováno v: Molecules (Basel, Switzerland) [Molecules] 2022 Sep 30; Vol. 27 (19). Date of Electronic Publication: 2022 Sep 30.