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Related Experiment Videos

Selenium-based antihypertensives. Rationale and potential

S W May1, S H Pollock

  • 1School of Chemistry and Biochemistry, Georgia Institute of Technology and School of Pharmacy, Mercer University, Atlanta, USA.

Drugs
|January 8, 1999
PubMed
Summary
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Selenium compounds show promise as novel antihypertensive agents. Researchers developed an orally active phenylaminoalkyl selenide, the first of its kind, demonstrating dose-dependent blood pressure reduction in rats.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Selenium is an essential dietary antioxidant and a component of vital enzymes like glutathione peroxidase.
  • Selenium deficiency is linked to various diseases, prompting interest in selenium's therapeutic potential.
  • Synthetic selenium compounds are being explored as novel therapeutic agents.

Purpose of the Study:

  • To develop novel selenium-based pharmacological agents.
  • To investigate the antihypertensive activity of phenylaminoalkyl selenides.
  • To identify an orally active selenium-based compound for treating hypertension.

Main Methods:

  • Synthesis of phenylaminoalkyl selenides.
  • Assessment of antihypertensive activity in spontaneously hypertensive rats.

Related Experiment Videos

  • Biochemical analysis of enzyme interactions (dopamine-beta-monooxygenase) and redox properties.
  • Inductively coupled plasma/mass spectrometry and behavioral studies to evaluate CNS permeability and oral activity.

    • Main Results:

    • Phenylaminoalkyl selenides demonstrated dose-dependent antihypertensive effects.
    • These compounds facilitate ascorbate depletion via dopamine-beta-monooxygenase, linked to their redox properties.
    • An orally active phenylaminoalkyl selenide with restricted CNS penetration was successfully developed.
    • This compound, 4-hydroxy-alpha-methyl-phenyl-2-aminoethyl selenide, is the first reported orally active, selenium-based antihypertensive agent.

    Conclusions:

    • Phenylaminoalkyl selenides represent a novel class of selenium-based antihypertensive drugs.
    • The unique mechanism involving redox cycling and enzyme interaction offers new therapeutic avenues.
    • Further development of rationally designed selenium compounds holds potential for treating various human diseases.