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OtherIUPHAR Nomenclature Reports

International Union of Pharmacology. LVI. Ghrelin Receptor Nomenclature, Distribution, and Function

Anthony P. Davenport, Tom I. Bonner, Steven M. Foord, Anthony J. Harmar, Richard R. Neubig, Jean-Philippe Pin, Michael Spedding, Masayasu Kojima and Keniji Kangawa
Pharmacological Reviews December 2005, 57 (4) 541-546; DOI: https://doi.org/10.1124/pr.57.4.1
Anthony P. Davenport
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Tom I. Bonner
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Steven M. Foord
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Anthony J. Harmar
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Richard R. Neubig
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Jean-Philippe Pin
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Michael Spedding
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Masayasu Kojima
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Keniji Kangawa
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)
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Tables

  • TABLE 1
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    TABLE 2

    Classification of ghrelin receptor

    Receptor Ghrelin, GRLN
    Receptor code 2.1:GHS:1:GHS1:HUMAN:00
    Previous names GHS-R, GHS-R1a (approved human gene symbol)
    Structural information 7TM
    Human: 366aa (SwissProt Q92847), chr. 3q26.31 (LocusLink 2693)
    Rat: 364aa (SwissProt O08725), chr. 2Q24 (LocusLink 84022)
    Mouse: 364aa (SwissProt Q99P50), chr. 3A3 (LocusLink 208188)
    Functional assays In vitro pharmacology using human isolated vessels (Wiley and Davenport, 2002)
    In vitro pharmacology using isolated guinea pig papillary muscle (Bedendi et al., 2003)
    Endogenous agonists Ghrelin (IC50 = 8.1 nM/EC50 = 1.5 nM) = des-Gln14-ghrelin (IC50 = 7.4 nM/EC50 = 1.5 nM) (Matsumoto et al., 2001; Bedendi et al., 2003)
    Selective agonists GHRP-2 (IC50 = 0.4 nM) > MK-0677 (IC50 = 0.8 nM) > GHRP-6 (IC50 = 1.5 nM) (cloned rat receptor; McKee et al., 1997)
    Antagonists [d-Lys3]-GHRP-6, EP-80317
    Antagonist potencies
    Radioligand assays Human hypothalamus, human cardiovascular tissue
    Radioligands [125I-His9]-ghrelin, (Kd = 0.22–0.57 nM) (Katugampola et al., 2001)
    [125I-Tyr4]-ghrelin (Kd = 0.44 nM) (Muccioli et al., 2001)
    [125I-Tyr4]-ghrelin (Kd = 0.51 nM) (Bedendi et al., 2003)
    Transduction
    Mechanism Coupled to G-α-11 proteins
    Receptor distribution Humans, specific [125I-His9]-ghrelin binding was localized to the human vasculature including aorta, coronary arteries, pulmonary arteries, arcuate arteries (in the kidney), and saphenous veins; rats: binding sites were also localized to the vasculature in peripheral tissues as well as the granular layer of the cerebellum in the CNS (Katugampola et al., 2001)
    Tissue function Stimulates release of growth hormone from the anterior pituitary, gastric acid secretion, and motility; may alter appetite and energy balance; vasodilation
    • aa, amino acid; chr., chromosome.

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Pharmacological Reviews: 57 (4)
Pharmacological Reviews
Vol. 57, Issue 4
1 Dec 2005
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OtherIUPHAR Nomenclature Reports

International Union of Pharmacology. LVI. Ghrelin Receptor Nomenclature, Distribution, and Function

Anthony P. Davenport, Tom I. Bonner, Steven M. Foord, Anthony J. Harmar, Richard R. Neubig, Jean-Philippe Pin, Michael Spedding, Masayasu Kojima and Keniji Kangawa
Pharmacological Reviews December 1, 2005, 57 (4) 541-546; DOI: https://doi.org/10.1124/pr.57.4.1

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International Union of Pharmacology. LVI. Ghrelin Receptor Nomenclature, Distribution, and Function

Anthony P. Davenport, Tom I. Bonner, Steven M. Foord, Anthony J. Harmar, Richard R. Neubig, Jean-Philippe Pin, Michael Spedding, Masayasu Kojima and Keniji Kangawa
Pharmacological Reviews December 1, 2005, 57 (4) 541-546; DOI: https://doi.org/10.1124/pr.57.4.1
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  • Article
    • Abstract
    • I. Introduction
    • II. Growth Hormone Secretagogue Receptor 1a Designated as the Ghrelin Receptor
    • III. Distribution of Receptor and mRNA Encoding the Receptor
    • IV. Radiolabeled Ligands
    • V. Agonists
    • VI. Antagonists
    • VII. Physiological Role
    • VIII. Pathophysiological Role
    • IX. Genetically Modified Animals
    • Acknowledgments
    • Footnotes
    • References
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