Prostanoid Receptors

Prostanoid receptors are activated by the endogenous ligands prostaglandin (PG) D₂, PGE₂, PGF_2α, 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.

1. DP receptors (DP_1-2) are coupled to G_αs. 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.
2. EP receptors (EP_1-4) 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 G_αs and induce smooth muscle relaxation. EP₃ is an inhibitory receptor that prevents smooth muscle relaxation.
3. FP receptors are coupled to G_αq. They are abundant in the corpus luteum, where they are involved in luteolysis.
4. IP receptors are coupled to G_αs and are involved in pain mediation, relaxation of vascular smooth muscle, inhibition of platelet aggregation and they contribute to cardiovascular health.
5. TP receptors can be coupled to both G_αq and G_αi. 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.

External sources of pharmacological information for Prostanoid Receptors :

• IUPHAR Receptor Code

• BJP Guide

Literature for Prostanoid Receptors

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

• Hypertension
• Thrombosis and Hemostasis
• Atherosclerosis
• Myocardial Infarction
• Ischemia/Reperfusion Injury
• Arrhythmias
• Heart Failure

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GPCR Product Listing

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

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Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

• Chemokine and Cytokine Signaling
• Chemotaxis
• Complement System
• Immune Cell Signaling
• Inflammation

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Asthma Poster

Asthma is one of the most common chronic diseases in the world, affecting over 300 million people. This poster highlights key pathways and new therapies used to treat the condition, including those currently in clinical development.

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Cardiovascular Poster

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.

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Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. 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.

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Prostanoid Receptor Gene Data

Pathway of Prostanoid Production

Prostanoid Receptor Pharmacological Data

References

IUPHAR Compendium of receptor characterization and classification. (2000) 2nd Edition. IUPHAR Media. Breyer et al (2001) Prostanoid receptors: subtypes and signaling. Ann.Rev.Pharmacol.Toxicol. 41 661.