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.

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.

Novel Vaccine That Blunts Fentanyl Effects and Sequesters Ultrapotent Fentanyl Analogues.

Autor: Barrientos RC; Laboratory of Adjuvant and Antigen Research, U.S. Military HIV Research Program, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.; U.S. Military HIV Research Program, Henry M. Jackson Foundation for the Advancement of Military Medicine, 6720A Rockledge Drive, Bethesda, Maryland 20817, United States., 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, Department of Health and Human Services, National Institutes of Health, 9800 Medical Center Drive, Bethesda, Maryland 20892-3373, United States., Whalen C; Laboratory of Adjuvant and Antigen Research, U.S. Military HIV Research Program, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States., Torres OB; Laboratory of Adjuvant and Antigen Research, U.S. Military HIV Research Program, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.; U.S. Military HIV Research Program, Henry M. Jackson Foundation for the Advancement of Military Medicine, 6720A Rockledge Drive, Bethesda, Maryland 20817, 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, Department of Health and Human Services, National Institutes of Health, 9800 Medical Center Drive, Bethesda, Maryland 20892-3373, United States., Beck Z; Laboratory of Adjuvant and Antigen Research, U.S. Military HIV Research Program, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.; U.S. Military HIV Research Program, Henry M. Jackson Foundation for the Advancement of Military Medicine, 6720A Rockledge Drive, Bethesda, Maryland 20817, 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, Department of Health and Human Services, National Institutes of Health, 9800 Medical Center Drive, Bethesda, Maryland 20892-3373, 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, Department of Health and Human Services, National Institutes of Health, 9800 Medical Center Drive, Bethesda, Maryland 20892-3373, United States., Matyas GR; Laboratory of Adjuvant and Antigen Research, U.S. Military HIV Research Program, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.

Publikováno v: Molecular pharmaceutics [Mol Pharm] 2020 Sep 08; Vol. 17 (9), pp. 3447-3460. Date of Electronic Publication: 2020 Aug 13.