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Prostanoid and leukotriene receptor (None standardized for the combined class; prostanoid receptors are abbreviated as DP, EP, FP, IP, TP; leukotriene receptors as BLT, CysLT, GPR17, etc.[1][3][5][6])

Target
None standardized for the combined class; prostanoid receptors are abbreviated as DP, EP, FP, IP, TP; leukotriene receptors as BLT, CysLT, GPR17, etc.[1][3][5][6]
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

Prostanoid and leukotriene receptors are two distinct families of G protein-coupled receptors that mediate the biological actions of eicosanoids: prostanoids (including prostaglandins and thromboxanes) and leukotrienes. These receptors regulate a broad spectrum of physiological and pathological processes such as inflammation, pain, immune response, vascular tone, and smooth muscle function. Prostanoid receptors include DP, EP, FP, IP, and TP, with further subtypes (e.g., EP1–4), whereas leukotriene receptors are divided into BLT and CysLT classes (e.g., BLT1, CysLT1, CysLT2). Drugs targeting these receptors are widely used in the management of asthma, allergies, pain, and cardiovascular diseases[1][3][4][5][6][7].

Other names
Prostanoid receptor family (includes DP, EP, FP, IP, TP)Leukotriene receptor family (includes BLTR, CysLTR)Eicosanoid receptors (sometimes collectively used for both)
02

Mechanism of action

Antagonism of leukotriene receptors (reduces bronchoconstriction and inflammation) Agonism or antagonism of prostanoid receptors (modulates vascular tone, platelet aggregation, inflammation, and pain) Modulation of GPCR signaling pathways with downstream effects on cAMP, Ca²⁺, and phospholipase activity

03

Biological functions

Signal transductionRegulation of vascular toneImmune responseInflammation (initiation and resolution)Smooth muscle contraction/relaxationRegulation of pain perceptionModulation of blood pressure and blood flowCell proliferation, apoptosis, and differentiation
04

Disease associations

InflammationAsthmaCardiovascular diseaseCancerAllergyPain disordersThrombosis
05

Safety considerations

Hypersensitivity and allergic reactions (notably with leukotriene receptor antagonists)Cardiovascular risk (e.g., prostacyclin analogues can cause hypotension)Bleeding risk (prostanoid receptor modulation affects platelet function)Neuropsychiatric events (reported with some leukotriene antagonists)
06

Interacting drugs

Leukotriene receptor antagonists (e.g., montelukast, zafirlukast, pranlukast)

3 more in the full profile.

07

Biomarkers

Genetic polymorphisms in prostanoid (PTGER, PTGDR, TBXA2R, etc.) and leukotriene receptor genes (CYSLTR1, CYSLTR2) can influence drug response and disease predispositionLeukotriene and prostaglandin urine or blood levels can be used as biomarkers in some settings

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