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Somatostatin receptors.

M J Lewin

    Scandinavian Journal of Gastroenterology. Supplement
    |January 1, 1986
    PubMed
    Summary
    This summary is machine-generated.

    Researchers identified the minimal active structure of somatostatin receptors and synthesized active minisomatostatins. Different binding affinities suggest receptor subtypes, impacting stimulus-secretion coupling.

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    Area of Science:

    • Biochemistry
    • Molecular Biology
    • Pharmacology

    Background:

    • Recent research has advanced understanding of somatostatin receptor(s) biochemical structure and function.
    • The minimal active structure of somatostatin receptors has been identified.
    • Active minisomatostatins have been successfully synthesized.

    Purpose of the Study:

    • To elucidate the biochemical structure and operational mechanisms of somatostatin receptors.
    • To investigate the binding characteristics and tissue specificities of somatostatin and its analogs.
    • To explore the interactions of somatostatin with cellular signaling pathways involved in secretion.

    Main Methods:

    • Identification of minimal active receptor structures.
    • Synthesis of active minisomatostatins.

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  • Binding affinity studies using radioligands in various tissues (brain, peripheral organs, pancreas, stomach, intestine).

    • Main Results:

    • High-affinity somatostatin binding sites (Kd 0.1-1 nM) detected in brain and peripheral organs.
    • Evidence for low-affinity somatostatin sites/states in pancreas, stomach, and intestine.
    • Differential binding affinities of somatostatin-14 and somatostatin-28 suggest distinct receptor subtypes.
    • Potential presence of cytosolic somatostatin receptors.

    Conclusions:

    • The study provides significant insights into somatostatin receptor structure and function.
    • Distinct receptor subtypes likely exist, contributing to varied tissue-specific responses.
    • Somatostatin may modulate stimulus-secretion coupling via direct adenylate cyclase inhibition or distal phosphatase activation.