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Histamine receptors and cyclic AMP.

J H McNeill

    Canadian Journal of Physiology and Pharmacology
    |September 1, 1980
    PubMed
    Summary

    Selective H1 and H2 receptor antagonists enable histamine receptor study. H2 receptors are found in many tissues, correlating with adenylate cyclase-cyclic AMP. H1 receptors in the brain also involve this system.

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    Area of Science:

    • Pharmacology
    • Cellular Biology
    • Physiology

    Background:

    • Selective agonists and antagonists have advanced the study of histamine receptors (H1 and H2) across various species.
    • H2 receptors are well-established in gastric mucosa, heart, rat uterus, brain, and adipose tissue, with other systems less defined.
    • A correlation between H2 receptors and the adenylate cyclase-cyclic AMP system is observed in examined tissues.

    Purpose of the Study:

    • To review the literature on histamine's involvement with the adenylate cyclase-cyclic AMP system.
    • To focus on specific tissues where this interaction has been extensively studied.

    Main Methods:

    • Review of scientific literature on histamine receptor pharmacology and signal transduction.
    • Analysis of studies investigating the relationship between H1/H2 receptor stimulation and adenylate cyclase activity.
    • Examination of data differentiating H1 and H2 receptor-mediated effects, particularly in the central nervous system.

    Main Results:

    • H2 receptors are widely distributed and linked to adenylate cyclase activation.
    • In most tissues, H1 receptor stimulation is not associated with cyclic AMP.
    • Brain H1 receptor stimulation of adenylate cyclase can be distinguished from H2 receptor effects, being enhanced by adenosine.

    Conclusions:

    • Histamine receptors, particularly H2, play a significant role in regulating the adenylate cyclase-cyclic AMP pathway in various organs.
    • Further research is needed to fully elucidate the complexities of H1 and H2 receptor signaling, especially in the central nervous system.

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