Page last updated: 2024-10-24
prostaglandin D receptor activity
Definition
Target type: molecularfunction
Combining with prostaglandin D (PGD(2)) to initiate a change in cell activity. [ISBN:0198506732]
Prostaglandin D receptor activity is a molecular function that involves the binding and recognition of prostaglandin D2 (PGD2), a lipid mediator with diverse biological roles. PGD2 exerts its effects through two distinct G protein-coupled receptors: DP1 and DP2.
DP1 receptors, also known as CRTH2, are primarily expressed on Th2 cells, eosinophils, and mast cells. Activation of DP1 receptors leads to the downstream signaling cascade involving the G protein Gs, resulting in the production of cAMP. This cAMP signaling pathway triggers a variety of cellular responses, including chemotaxis, degranulation, and cytokine release, contributing to the pathogenesis of allergic inflammation and asthma.
DP2 receptors, also known as the prostaglandin D2 receptor, are expressed on various cells, including neurons, smooth muscle cells, and immune cells. Activation of DP2 receptors primarily involves the G protein Gi, leading to the inhibition of adenylyl cyclase and a decrease in cAMP levels. This signaling pathway is implicated in regulating sleep, inflammation, and pain.
In summary, prostaglandin D receptor activity plays a crucial role in mediating the physiological and pathophysiological effects of PGD2. Its interaction with distinct G protein-coupled receptors, DP1 and DP2, triggers diverse signaling pathways that regulate a wide range of cellular functions, including inflammation, chemotaxis, degranulation, cytokine release, sleep, and pain.'
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Proteins (2)
| Protein | Definition | Taxonomy |
|---|---|---|
| Prostaglandin D2 receptor 2 | A prostaglandin D2 receptor DP2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9Y5Y4] | Homo sapiens (human) |
| Prostaglandin D2 receptor | A prostaglandin D2 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q13258] | Homo sapiens (human) |
Compounds (32)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| indomethacin | indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. | aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole | analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic; xenobiotic metabolite |
| lomerizine | lomerizine: used to treat migraines | diarylmethane | |
| phlorhizin | aryl beta-D-glucoside; dihydrochalcones; monosaccharide derivative | antioxidant; plant metabolite | |
| 2-methyl-4-chlorophenoxyacetic acid | (4-chloro-2-methylphenoxy)acetic acid : A chlorophenoxyacetic acid that is (4-chlorophenoxy)acetic acid substituted by a methyl group at position 2. 2-Methyl-4-chlorophenoxyacetic Acid: A powerful herbicide used as a selective weed killer. | chlorophenoxyacetic acid; monochlorobenzenes | environmental contaminant; phenoxy herbicide; synthetic auxin |
| fentiazac | thiazoles | ||
| duloxetine | duloxetine | ||
| ah 6809 | 6-isopropoxy-9-oxoxanthene-2-carboxylic acid: structure given in UD | xanthones | |
| ramatroban | organic molecular entity | ||
| agatoxin-489 | agatoxin-489: structure given in first source; anhydrous MW 489 Da; isolated from Agelenopsis aperta | ||
| flunarizine | Flunarizine: Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. | diarylmethane | |
| np 118809 | 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one: an N-type calcium channel blocker; structure in first source | ||
| dinoprost | Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor. | monocarboxylic acid; prostaglandins Falpha | human metabolite; mouse metabolite |
| cloprostenol | Cloprostenol: A synthetic prostaglandin F2alpha analog. The compound has luteolytic effects and is used for the synchronization of estrus in cattle. | prostanoid | |
| iloprost | iloprost : A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension. Iloprost: An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation. | carbobicyclic compound; monocarboxylic acid; secondary alcohol | platelet aggregation inhibitor; vasodilator agent |
| sulindac sulfide | sulindac sulfide : An aryl sulfide that is a metabolite of sulindac. A non-steroidal anti-inflammatory drug, which also has anticancer activity. sulindac sulfide: sulfated analog of indomethacin & inhibitor of prostaglandin synthesis in vitro; RN given refers to cpd without isomeric designation; structure given in first source | aryl sulfide; monocarboxylic acid; organofluorine compound | antineoplastic agent; apoptosis inducer; non-steroidal anti-inflammatory drug |
| tg4-155 | TG4-155: an EP2 receptor antagonist; structure in first source | ||
| u 62840 | U 62840: stereoisomeric benzindene prostaglandin analog; structure given in first source | carbotricyclic compound; carboxylic acid | antihypertensive agent; cardiovascular drug; human blood serum metabolite; platelet aggregation inhibitor; vasodilator agent; vitamin K antagonist |
| mk-0524 | MK-0524: a potent orally active human prostaglandin D(2) receptor 1 antagonist; structure in first source | indolyl carboxylic acid | |
| selexipag | selexipag : A member of the class of pyrazines that is N-(methanesulfonyl)-2-{4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetamide carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. An orphan drug used for the treatment of pulmonary arterial hypertension. It is a prodrug for ACT-333679 (the free carboxylic acid). selexipag: prostacyclin receptor agonist | aromatic amine; ether; monocarboxylic acid amide; N-sulfonylcarboxamide; pyrazines; tertiary amino compound | orphan drug; platelet aggregation inhibitor; prodrug; prostacyclin receptor agonist; vasodilator agent |
| mre 269 | (4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid: active form of NS-304 ACT-333679 : A member of the class of pyrazines that is {4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetic acid carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. The active metabolite of selexipag, an orphan drug used for the treatment of pulmonary arterial hypertension. | aromatic amine; ether; monocarboxylic acid; pyrazines; sulfonamide; tertiary amino compound | drug metabolite; orphan drug; platelet aggregation inhibitor; prostacyclin receptor agonist; vasodilator agent |
| amg 009 | AMG 009: an anti-inflammatory agent; structure in first source | ||
| azd1981 | |||
| cay 10471 | CAY 10471: a prostaglandin D2 receptor antagonist; structure in first source | ||
| oc000459 | |||
| l-798106 | L-798106 : An N-sulfonylcarboxamide resulting from the formal condensation of the carboxy group of o-naphthalen-2-ylcinnamic acid with the sulfonamide group of 5-bromo-2-methoxybenzenesulfonamide. It is a selective antagonist for the prostanoid receptor EP3, a prostaglandin receptor for prostaglandin E2 (PGE2). | aromatic ether; bromobenzenes; N-sulfonylcarboxamide | prostaglandin receptor antagonist |
| fevipiprant | fevipiprant: a CRTh2 antagonist; structure in first source | ||
| fr181157 | |||
| pf-04418948 | 1-(4-fluorobenzoyl)-3-(((6-methoxy-2-naphthyl)oxy)methyl)azetidine-3-carboxylic acid: structure in first source | ||
| amg 853 | vidupiprant: structure in first source | ||
| cay 10580 | 2-(3-hydroxyoctyl)-5-oxo-1-pyrrolidineheptanoic acid : A pyrrolidin-2-one substituted by 6-carboxyhexyl and 3-hydroxyoctyl groups at positions 1 and 2, respectively. It is a potent prostaglandin EP4 receptor agonist (Ki=35 nM). CAY 10580: a E-prostanoid EP4 receptor agonist | hydroxy monocarboxylic acid; pyrrolidin-2-ones; secondary alcohol | prostaglandin receptor agonist |
| mk-7246 | |||
| tg6-10-1 | TG6-10-1: brain-permeant prostaglandin E receptor 2 antagonist; structure in first source |