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Differential effects of Selexipag [corrected] and prostacyclin analogs in rat pulmonary artery.

Author: ClozelMartine, ErnstRoland, HaagFranck, KauserKatalin, MorrisonKeith, StuderRolf

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

The study compared the effects of two prostacyclin receptor agonists, selexipag and treprostinil, on pulmonary artery relaxation. Selexipag and its metabolite ACT-333679 effectively relaxed the pulmonary artery, even under conditions of pulmonary hypertension. Treprostinil, however, showed limited relaxation in these conditions.
Paper Details　
Original Abstract of the Article :
{4-[(5,6-Diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid (ACT-333679) is the main metabolite of the selective prostacyclin (PGI(2)) receptor (IP receptor) agonist selexipag. The goal of this study was to determine the influence of IP receptor selectivity on the vasorelaxant efficacy of ACT-...See full text at original site
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引用元：
https://doi.org/10.1124/jpet.112.197152

データ提供：米国国立医学図書館（NLM）

Selexipag and Treprostinil: Exploring the Role of IP Receptor Selectivity in Pulmonary Artery

Pulmonary arterial hypertension (PAH) is a serious condition affecting the blood vessels in the lungs. This study investigates the vasorelaxant effects of selexipag and treprostinil, two drugs used to treat PAH, focusing on the role of IP receptor selectivity.

Understanding IP Receptor Selectivity in PAH Treatment

The study found that selexipag and its metabolite, ACT-333679, effectively relaxed pulmonary arteries, both in normal and PAH conditions. In contrast, treprostinil showed weaker relaxation in normal arteries and failed to relax PAH arteries. These findings highlight the importance of IP receptor selectivity in the effectiveness of PAH treatments.

Optimizing Treatment Strategies for Pulmonary Arterial Hypertension

This research provides valuable insights into the mechanisms of PAH treatment. It demonstrates the potential of IP receptor-selective drugs like selexipag in addressing the challenges of PAH. Understanding these differences in receptor selectivity can help doctors choose the most appropriate treatment for individual patients with PAH.

Dr.Camel's Conclusion

This study sheds light on the importance of IP receptor selectivity in treating pulmonary arterial hypertension. The findings demonstrate the potential of selexipag and its metabolite as effective treatments for PAH, while highlighting the limitations of non-selective agents like treprostinil. This research underscores the need for individualized treatment approaches based on specific receptor selectivity.

Date :
  1. Date Completed 2013-01-24
  2. Date Revised 2019-01-09
Further Info :

Pubmed ID

22918043

DOI: Digital Object Identifier

10.1124/jpet.112.197152

Related Literature

Article Analysis
・Effects of selexipag
SNS
PICO Info
in preparation
Languages

English

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