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Peripheral 5-HT4 receptors

S S Hegde1, R M Eglen

  • 1Institute of Pharmacology, Neurobiology Unit, Roche Bioscience, Palo Alto, California 94304, USA.

FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology
|October 1, 1996
PubMed
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The serotonin 5-HT4 receptor, a G-protein-coupled receptor, influences various bodily functions. Selective agonists and antagonists targeting this receptor show potential for treating peripheral disorders.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Gastroenterology

Background:

  • The 5-HT4 receptor is a G-protein-coupled receptor involved in numerous physiological processes.
  • It exists in two isoforms, 5-HT4S and 5-HT4L, differing in their carboxy termini.
  • Pharmacological tools like agonists (SC 53116, RS 67506) and antagonists (GR 113808, SB 204070, RS 39604) define its activity.

Purpose of the Study:

  • To review the physiology and pharmacology of the 5-HT4 receptor.
  • To highlight its distribution and function in both central and peripheral systems.
  • To discuss the therapeutic potential of selective 5-HT4 receptor modulators.

Main Methods:

  • Literature review of studies on 5-HT4 receptor physiology and pharmacology.
  • Analysis of receptor distribution in various tissues.

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  • Examination of the effects of receptor activation/blockade on organ function.

    • Main Results:

    • The 5-HT4 receptor is widely distributed, impacting the alimentary tract, urinary bladder, heart, and adrenal gland.
    • Stimulation affects smooth muscle tone, electrolyte secretion, peristalsis, bladder transmission, cardiac function, and hormone release.
    • Selective agonists and antagonists have been developed.

    Conclusions:

    • The 5-HT4 receptor plays a critical role in peripheral organ systems.
    • Selective modulators of the 5-HT4 receptor offer potential therapeutic applications for conditions like IBS, gastroparesis, and urinary incontinence.