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Histamine H2-binding on guinea pig cerebral cortex.

G J Sterk, M W van der Schaar, B Rademaker

    Agents and Actions
    |April 1, 1986
    PubMed
    Summary
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    Histamine H2 receptor affinity (Kd) correlated well with antagonist activity (pA2) in guinea-pig atria. However, agonist affinity (Kd) poorly predicted activity (pD2) in atria and gastric fundus, likely due to spare receptors.

    Area of Science:

    • Pharmacology
    • Neuroscience
    • Biochemistry

    Background:

    • Histamine H2 receptors play crucial roles in various physiological processes.
    • Understanding the relationship between receptor binding affinity and functional activity is essential for drug development.

    Purpose of the Study:

    • To compare the dissociation equilibrium constant (Kd) values from radio-ligand binding studies with functional activity (pA2/pD2) values for histamine H2-active compounds.
    • To investigate the correlation between receptor affinity and H2-activity in different guinea-pig tissues.

    Main Methods:

    • Radio-ligand binding assays using 3H-tiotidine on guinea-pig cerebral cortex homogenates to determine Kd values.
    • Functional assays on guinea-pig right atrium and isolated gastric fundus to determine pA2 (for antagonists) and pD2 (for agonists) values.

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    Main Results:

    • A strong correlation was observed between the Kd values of H2-antagonists and their pA2 values on the guinea-pig right atrium.
    • A significantly weaker correlation was found between the Kd values of H2-agonists and their pD2 values on both guinea-pig right atrium and gastric fundus.
    • The poor correlation for agonists may be attributed to the phenomenon of spare receptors, as partial agonists showed a better correlation between Kd and pD2.

    Conclusions:

    • Receptor affinity (Kd) is a reliable predictor of antagonist activity (pA2) at histamine H2 receptors in the guinea-pig right atrium.
    • The relationship between affinity and activity for histamine H2-agonists is complex and influenced by factors such as spare receptors, particularly in the guinea-pig gastric fundus.
    • These findings highlight the importance of considering receptor reserve when evaluating agonist efficacy based on binding affinities.