Biexponential Kinetics of (R)‐α‐[3H]Methylhistamine Binding to the Rat Brain H3 Histamine Receptor

  title={Biexponential Kinetics of (R)‐α‐[3H]Methylhistamine Binding to the Rat Brain H3 Histamine Receptor},
  author={R. West and A. Zweig and Russell T. Granzow and M. Siegel and R. Egan},
  journal={Journal of Neurochemistry},
  • R. West, A. Zweig, +2 authors R. Egan
  • Published 1990
  • Chemistry
  • Journal of Neurochemistry
  • Abstract: The H3 histamine receptor is a high‐affinity receptor reported to mediate inhibition of CNS histidine decarboxylase activity and depolarization‐induced histamine release. We have used (R)‐α‐[3H]methylhistamine, a specific, high‐affinity agonist, to characterize ligand binding to this receptor. Saturation binding studies with rat brain membranes disclosed a single class of sites (KD= 0.68 nM; Bmax= 78 fmol/mg of protein). Competition binding assays also yielded an apparently single… CONTINUE READING
    37 Citations
    Detection of multiple H3 receptor affinity states utilizing [3H]A‐349821, a novel, selective, non‐imidazole histamine H3 receptor inverse agonist radioligand
    • 31
    Characterization of the binding of [3H]‐clobenpropit to histamine H3‐receptors in guinea‐pig cerebral cortex membranes
    • 21
    • Highly Influenced
    Evidence that histamine homologues discriminate between H3‐receptors in guinea‐pig cerebral cortex and ileum longitudinal muscle myenteric plexus
    • 23
    • Highly Influenced
    High affinity histamine H3 receptors regulate ACTH release by AtT-20 cells.
    • 24


    Properties and roles of the three subclasses of histamine receptors in brain.
    • 73
    • PDF
    Ligand: a versatile computerized approach for characterization of ligand-binding systems.
    • 7,969
    Inhibition of guinea pig ileum contractions mediated by a class of histamine receptor resembling the H3 subtype.
    • J. Trzeciakowski
    • Biology, Medicine
    • The Journal of pharmacology and experimental therapeutics
    • 1987
    • 118
    A highly potent and selective H3 agonist relaxes rabbit middle cerebral artery, in vitro.
    • 65