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Research ArticleIUPHAR Nomenclature Reports

International Union of Basic and Clinical Pharmacology. LXXIV. Apelin Receptor Nomenclature, Distribution, Pharmacology, and Function

Sarah L. Pitkin, Janet. J. Maguire, Tom I. Bonner and Anthony P. Davenport
Pharmacological Reviews September 2010, 62 (3) 331-342; DOI: https://doi.org/10.1124/pr.110.002949
Sarah L. Pitkin
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (S.L.P., J.J.M., A.P.D.); and Section on Functional Neuroscience, National Institute of Mental Health, Bethesda, Maryland (T.I.B.)
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Janet. J. Maguire
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (S.L.P., J.J.M., A.P.D.); and Section on Functional Neuroscience, National Institute of Mental Health, Bethesda, Maryland (T.I.B.)
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Tom I. Bonner
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (S.L.P., J.J.M., A.P.D.); and Section on Functional Neuroscience, National Institute of Mental Health, Bethesda, Maryland (T.I.B.)
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Anthony P. Davenport
Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (S.L.P., J.J.M., A.P.D.); and Section on Functional Neuroscience, National Institute of Mental Health, Bethesda, Maryland (T.I.B.)
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  • Fig. 1.
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    Fig. 1.

    Alignment of human, rat, and mouse apelin receptors. *, identical amino acids, :, conserved amino acid substitution; ., semiconserved amino acid substitution.

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    Fig. 2.

    Sequence alignment of mammalian, fish and amphibian apelin-36 amino acid sequences. *, identical amino acids; :, conserved amino acid substitution; ., semiconserved amino acid substitution. Residues that differ from the human sequence are highlighted in red.

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    Fig. 3.

    Amino acid sequence of the endogenous apelin receptor agonists apelin-36 (a), apelin-17 (b), (Pyr1)apelin-13 (c), and apelin-13 (d). Shaded residues are those identical in all peptides. The post-translational modification of the N-terminal glutamate of apelin-13 to pyroglutamate is shown in dark gray. ACE2 cleaves apelin-36 and apelin-13 at the position shown (Vickers et al., 2002). *, residues found to be important for binding and activation of the apelin receptor by apelin-13 (Fan et al., 2003; Medhurst et al., 2003; El Messari et al., 2004).

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    Fig. 4.

    Cyclic apelin analogs drawn from the sequences reported by Hamada et al. (2008) (a) and Macaluso et al. (2009) (b).

Tables

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    TABLE 1

    IUPHAR recommendations on receptor nomenclature

    Family nameApelin receptor
    LigandApelin
    Official IUPHAR receptor nameApelin receptor
    Human gene nameAPLNR
    Rat gene nameaplnr
    Mouse gene nameaplnr
    • View popup
    TABLE 2

    Actions and affinities of endogenous apelin receptor agonists

    LigandActionAffinity (pIC50)References
    Apelin-36Full agonist8.6–8.3Hosoya et al., 2000; Kawamata et al., 2001; Fan et al., 2003; Medhurst et al., 2003
    Apelin-17Full agonist9.0–7.9Medhurst et al., 2003; El Messari et al., 2004
    (Pyr1)apelin-13Full agonist8.9–8.0Hosoya et al., 2000; Medhurst et al., 2003; El Messari et al., 2004
    Apelin-13Full agonist9.2–8.8Fan et al., 2003; Medhurst et al., 2003
    • View popup
    TABLE 3

    Actions and affinities of apelin receptor antagonists

    LigandActionAffinity (pKd)Reference
    ALX40–4CNonspecific antagonist5.5Zhou et al., 2003
    Apelin-13(F13A)Functional antagonistN.D.Lee et al., 2005
    • N.D., not determined.

    • View popup
    TABLE 4

    Radiolabelled ligands of the apelin receptor

    LigandAffinity (pKD)Expression SystemReference
    [125I]apelin-13N.D.HEK-293 cellsFan et al., 2003
    [125I](Pyr1)apelin-139.7–9.2Human/Rat tissueKatugampola et al., 2001; El Messari et al., 2004
    [125I](Pyr1)[Nle75,Tyr77]apelin-138.4–10.7CHO-A10 cells/HEK-293 cellsHosoya et al., 2000; Hashimoto et al., 2005
    [3H](Pyr1)[Met(O)11]apelin-138.6HEK-293 cellsMedhurst et al., 2003
    [125I][Nle75,Tyr77]apelin-3611.2CHO-A10 cellsKawamata et al., 2001
    • N.D., not determined.

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Pharmacological Reviews: 62 (3)
Pharmacological Reviews
Vol. 62, Issue 3
1 Sep 2010
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Research ArticleIUPHAR Nomenclature Reports

International Union of Basic and Clinical Pharmacology. LXXIV. Apelin Receptor Nomenclature, Distribution, Pharmacology, and Function

Sarah L. Pitkin, Janet. J. Maguire, Tom I. Bonner and Anthony P. Davenport
Pharmacological Reviews September 1, 2010, 62 (3) 331-342; DOI: https://doi.org/10.1124/pr.110.002949

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Research ArticleIUPHAR Nomenclature Reports

International Union of Basic and Clinical Pharmacology. LXXIV. Apelin Receptor Nomenclature, Distribution, Pharmacology, and Function

Sarah L. Pitkin, Janet. J. Maguire, Tom I. Bonner and Anthony P. Davenport
Pharmacological Reviews September 1, 2010, 62 (3) 331-342; DOI: https://doi.org/10.1124/pr.110.002949
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  • Article
    • Abstract
    • I. Introduction
    • II. The Apelin Receptor: Recommendations for Nomenclature
    • III. Receptor Structure
    • IV. Endogenous Agonists
    • V. Receptor Distribution
    • VI. Apelin Peptide Distribution
    • VII. Synthetic Agonists
    • VIII. Antagonists
    • IX. Radiolabeled Ligands
    • X. Physiological Roles
    • XI. Pathophysiological Roles
    • XII. Single-Nucleotide Polymorphisms
    • XIII. Knockout Mouse Models
    • XIV. Conclusion
    • Acknowledgments.
    • Footnotes
    • References
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