Structure Activity Relationships of P2 Receptor Agonists and Antagonists View Full Text


Ontology type: schema:Chapter     


Chapter Info

DATE

1998

AUTHORS

Kenneth A. Jacobson , Yong-Chul Kim , Emidio Camaioni , A. Michiel van Rhee

ABSTRACT

With the cloning of numerous new subtypes (Burnstock and King, 1996) of P2 receptors, (belonging to P2X and P2Y super families),* for naturally occurring extracellular purine and pyrimidine nucleotides (structures shown in Fig. 1), ligand development is underway. It is clear that the P2 receptors are structurally distinct from adenosine, or P1, receptors (van Rhee et al., 1995), thus they have markedly different ligand binding requirements. The recently reorganized nomenclature of P2 receptors divides them into ligand-gated ion channels (P2X, of which seven subtypes have been cloned) and metabotropic G protein-coupled subtypes (P2Y, of which at least four subtypes have been cloned). At P2X receptors (see Chapter 2, this volume, for subtype designations) the most potent native nucleotide is adenosine triphos-phate (ATP), 1 (the numbers denote compounds in the figures), whereas at various subtypes of P2Y receptors (see Chapter 3, this volume) uridine triphosphate (UTP), 4, and/or diphosphates such as adenosine diphosphate (ADP), 2, may serve as agonists. Adenine dinucleotides, such as Ap4A, 3, may directly activate P2Y-type dinucleotide receptors, and may allosterically enhance activation of P2X receptors (King et al., 1996). More... »

PAGES

81-107

References to SciGraph publications

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  • 1996-10. P2-purinoceptor antagonists: III. Blockade of P2-purinoceptor subtypes and ecto-nucleotidases by compounds related to suramin in NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY
  • 1995-05. Suramin analogs, divalent cations and ATPγS as inhibitors of ecto-ATPase in NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY
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  • Book

    TITLE

    The P2 Nucleotide Receptors

    ISBN

    978-1-4612-7289-2
    978-1-4612-1800-5

    Identifiers

    URI

    http://scigraph.springernature.com/pub.10.1007/978-1-4612-1800-5_4

    DOI

    http://dx.doi.org/10.1007/978-1-4612-1800-5_4

    DIMENSIONS

    https://app.dimensions.ai/details/publication/pub.1044446495


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