Research ArticleSpecial Section on Clinical Pharmacology
Initial Pharmacological Characterization of a Major Hydroxy Metabolite of PF-5190457: Inverse Agonist Activity of PF-6870961 at the Ghrelin Receptor
Sara L. Deschaine, Morten A. Hedegaard, Claire L. Pince, Mehdi Farokhnia, Jacob E. Moose, Ingrid A. Stock, Sravani Adusumalli, Fatemeh Akhlaghi, James L. Hougland, Agnieszka Sulima, Kenner C. Rice, George F. Koob, Leandro F. Vendruscolo, Birgitte Holst and Lorenzo Leggio
Journal of Pharmacology and Experimental Therapeutics August 2023, 386 (2) 117-128; DOI: https://doi.org/10.1124/jpet.122.001393
Sara L. Deschaine
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Morten A. Hedegaard
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Claire L. Pince
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Mehdi Farokhnia
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Jacob E. Moose
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Ingrid A. Stock
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Sravani Adusumalli
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Fatemeh Akhlaghi
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
James L. Hougland
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Agnieszka Sulima
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Kenner C. Rice
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
George F. Koob
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Leandro F. Vendruscolo
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Birgitte Holst
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Lorenzo Leggio
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Article Information
vol. 386 no. 2 117-128
PubMed
Print ISSN
Online ISSN
History
- Received July 23, 2022
- Accepted December 9, 2022
- Published online July 17, 2023.
Article Versions
- Earlier version (January 11, 2023 - 13:44).
- Earlier version (February 22, 2023 - 11:36).
- You are viewing the most recent version of this article.
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Author Information
- Sara L. Deschaine,
- Morten A. Hedegaard,
- Claire L. Pince,
- Mehdi Farokhnia,
- Jacob E. Moose,
- Ingrid A. Stock,
- Sravani Adusumalli,
- Fatemeh Akhlaghi,
- James L. Hougland,
- Agnieszka Sulima,
- Kenner C. Rice,
- George F. Koob,
- Leandro F. Vendruscolo,
- Birgitte Holst, and
- Lorenzo Leggio
- Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
- Address correspondence to:
Dr. Lorenzo Leggio, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Biomedical Research Center, Room 04A511, 251 Bayview Boulevard, Baltimore, MD 21224. E-mail: lorenzo.leggio{at}nih.gov
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In this issue
Research ArticleSpecial Section on Clinical Pharmacology
PF-5190457 Metabolite Activity at the Ghrelin Receptor
Sara L. Deschaine, Morten A. Hedegaard, Claire L. Pince, Mehdi Farokhnia, Jacob E. Moose, Ingrid A. Stock, Sravani Adusumalli, Fatemeh Akhlaghi, James L. Hougland, Agnieszka Sulima, Kenner C. Rice, George F. Koob, Leandro F. Vendruscolo, Birgitte Holst and Lorenzo Leggio
Journal of Pharmacology and Experimental Therapeutics August 1, 2023, 386 (2) 117-128; DOI: https://doi.org/10.1124/jpet.122.001393
Research ArticleSpecial Section on Clinical Pharmacology
PF-5190457 Metabolite Activity at the Ghrelin Receptor
Sara L. Deschaine, Morten A. Hedegaard, Claire L. Pince, Mehdi Farokhnia, Jacob E. Moose, Ingrid A. Stock, Sravani Adusumalli, Fatemeh Akhlaghi, James L. Hougland, Agnieszka Sulima, Kenner C. Rice, George F. Koob, Leandro F. Vendruscolo, Birgitte Holst and Lorenzo Leggio
Journal of Pharmacology and Experimental Therapeutics August 1, 2023, 386 (2) 117-128; DOI: https://doi.org/10.1124/jpet.122.001393
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