ArticleBritish journal of pharmacology2001
Distinction between relaxations induced via prostanoid EP(4) and IP(1) receptors in pig and rabbit blood vessels.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 31 citations in OpenAlex.
- Apolipoprotein E favours the blunting by high-fat diet of prostacyclin receptor activation in the mouse aorta.British journal of pharmacology · 2018Article
- Inhibition of calpain reduces oxidative stress and attenuates endothelial dysfunction in diabetes.Cardiovascular diabetology · 2014Article
- Molecular mechanisms regulating the vascular prostacyclin pathways and their adaptation during pregnancy and in the newborn.Pharmacological reviews · 2012Review
- Prostanoid receptor antagonists: development strategies and therapeutic applications.British journal of pharmacology · 2009Review
- Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations.British journal of pharmacology · 2006Article
- Involvement of Rho-kinase in contraction of guinea-pig aorta induced by prostanoid EP3 receptor agonists.British journal of pharmacology · 2003Article
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Authors and funding
2 authors at 1 institution in 1 country.
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Abstract
1. Our study shows that the prostacyclin analogues AFP-07 and cicaprost are moderately potent agonists for prostanoid EP(4) receptors, in addition to being highly potent IP(1) receptor agonists. Both activities were demonstrated on piglet and rabbit saphenous veins, which are established EP(4) preparations. 2. On piglet saphenous vein, PGE(2) was 6.1, 24, 96, 138, 168 and 285 times respectively more potent than AFP-07, cicaprost, PGI(2), iloprost, carbacyclin and TEI-9063 in causing relaxation. Another prostacyclin analogue taprostene did not induce maximum relaxation (21 - 74%), and did not oppose the action of PGE(2). The EP(4) receptor antagonist AH 23848 (30 microM) blocked relaxant responses to PGE(2) (dose ratio=8.6+/-1.3, s.e.mean) to a greater extent than cicaprost (4.9+/-0.7) and AFP-07 (3.8+/-0.8), had variable effects on TEI-9063-induced relaxation (3.7+/-1.5), and had no effect on taprostene responses (<2.0). 3. On rabbit saphenous vein, AH 23848 blocked the relaxant actions of PGE(2), AFP-07, cicaprost, iloprost and carbacyclin to similar extents. 4. AFP-07, cicaprost and TEI-9063 showed high IP(1) relaxant potency on piglet carotid artery, rabbit mesenteric artery and guinea-pig aorta, with AFP-07 confirmed as the most potent IP(1) agonist reported to date. AH 23848 did not block cicaprost-induced relaxation of piglet carotid artery. EP(3) contractile systems in these preparations can confound IP(1) agonist potency estimations. 5. Caution is urged when using AFP-07 and cicaprost to characterize IP(1) receptors in the presence of EP(4) receptors. Taprostene may be a lead to a highly selective IP(1) receptor agonist.
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