Prostanoid receptors are activated by the endogenous ligands prostaglandin (PG) D2, PGE2, PGF2α, PGH2, prostacyclin (PGI2) and thromboxane A2. Cyclooxygenase (COX) converts arachidonic acid to PGH2, from which the other prostaglandins are synthesized. Prostanoid receptors are a family of nine G-protein-coupled receptors that have distinct tissue distributions and actions.
- DP receptors (DP1-2) are coupled to Gαs. They are expressed in the small intestine, lung, stomach and uterus. Activation of DP1 results in inhibition of platelet activation and vasodilation; they are also involved in sleep regulation. DP2 activation leads to immune cell activation.
- EP receptors (EP1-4) are a diverse group of prostanoid receptors. EP1 receptors are restricted to the kidney, lung and stomach, and induce smooth muscle contraction. EP2 and EP4 couple to Gαs and induce smooth muscle relaxation. EP3 is an inhibitory receptor that prevents smooth muscle relaxation.
- FP receptors are coupled to Gαq. They are abundant in the corpus luteum, where they are involved in luteolysis.
- IP receptors are coupled to Gαs and are involved in pain mediation, relaxation of vascular smooth muscle, inhibition of platelet aggregation and they contribute to cardiovascular health.
- TP receptors can be coupled to both Gαq and Gαi. They are expressed abundantly in highly vascular tissues such as the kidney and heart, and immune-related organs such as the thymus and spleen. They mediate smooth muscle contraction and platelet aggregation.
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Literature for Prostanoid Receptors
A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:
- Thrombosis and Hemostasis
- Myocardial Infarction
- Ischemia/Reperfusion Injury
- Heart Failure
A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:
- Rhodopsin-like Receptors
- Secretin-like Receptors
- Glutamate Receptors
- Frizzled Receptors
- GPCR Signaling
A collection of over 190 products for immunology research, the guide includes research tools for the study of:
- Chemokine and Cytokine Signaling
- Complement System
- Immune Cell Signaling
Written by Peter Barnes, this poster highlights key pathways in the development of asthma. Special focus is given to new therapies used to treat asthma, including those currently in clinical development; treatment pathways include lipid mediator inhibitors, cytokine modulators and mast cell-directed therapies. Compounds available from Tocris are listed.Request copy | View all posters
Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.Request copy | Download PDF | View all posters
Written by Grant D. Nicol and Michael R. Vasko, this poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described. Compounds available from Tocris are listed.Request copy | Download PDF | View all posters