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Related Experiment Videos

Angiotensin II receptor antagonists

J C van Meel1, M Entzeroth, N Hauel

  • 1Dr. Karl Thomae GmbH, BiberachlRiss Fed. Rep. of Germany.

Arzneimittel-Forschung
|February 1, 1993
PubMed
Summary

Novel non-peptide compounds targeting angiotensin II (Ang II) receptors have enabled AT1 and AT2 subtype classification. Research explores Ang II receptor antagonist complexity and kidney sensitivity, demonstrating antihypertensive effects in rat models.

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Area of Science:

  • Pharmacology and Medicinal Chemistry
  • Cardiovascular Research
  • Renal Physiology

Background:

  • Development of non-peptide compounds with high affinity for angiotensin II (Ang II) receptors.
  • Facilitation of Ang II receptor subclassification into AT1 and AT2 subtypes.
  • Identification of prototypical antagonists: PD 123177 for AT2 and DuP 753 (losartan) for AT1 receptors.

Purpose of the Study:

  • To explore the complexity of Ang II receptor antagonism at the molecular and functional levels.
  • To investigate the antihypertensive activity of AT1 antagonists in different hypertensive rat models.
  • To assess the role of Ang II and its receptor antagonists in kidney function.

Main Methods:

  • Utilized selective AT2 (PD 123177) and AT1 (DuP 753) receptor antagonists.

Related Experiment Videos

  • Evaluated non-selective antagonists BIBS 39 and BIBS 222 for AT1/AT2 selectivity ratios.
  • Conducted functional studies with AT1 antagonists, including receptor binding kinetics and isolated rat kidney experiments.
  • Demonstrated antihypertensive effects of DuP 753 in high renin (2K 1C) and low renin (TGRmREN2) hypertensive rat models.

    • Main Results:

    • Non-selective non-peptide Ang II receptor antagonists have not yet been identified, though high selectivity ratios were reported for BIBS 39 and BIBS 222.
    • Ang II antagonism at the receptor level is complex, involving receptor binding kinetics, additional binding sites, and potentially AT1 subtypes.
    • The AT1 antagonist DuP 753 demonstrated significant antihypertensive activity in both high and low renin hypertensive rat models.
    • Experimental data indicates the kidney is highly sensitive to Ang II and a potential target for Ang II receptor antagonists.

    Conclusions:

    • Novel non-peptide compounds have advanced the understanding and subclassification of Ang II receptors.
    • Ang II receptor antagonism is a complex process requiring further investigation into binding kinetics and potential receptor subtypes.
    • AT1 receptor antagonists, like DuP 753, show promise for treating hypertension, particularly due to their effects on the kidney.