Platelet-activating factor receptor

Overview

Platelet-activating factor (PAF, 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine) is an ether phospholipid mediator associated with platelet coagulation, but also subserves inflammatory roles. The PAF receptor is activated by PAF and other suggested endogenous ligands are oxidized phosphatidylcholine [1] and lysophosphatidylcholine [2]. It may also be activated by bacterial lipopolysaccharide [3].

References

  1. Marathe GK, Davies SS, Harrison KA, et al. Inflammatory platelet-activating factor-like phospholipids in oxidized low density lipoproteins are fragmented alkyl phosphatidylcholines. J Biol Chem 1999;274:28395-404.
  2. Ogita T, Tanaka Y, Nakaoka T, et al. Lysophosphatidylcholine transduces Ca2+ signaling via the platelet-activating factor receptor in macrophages. Am J Physiol 1997;272:H17-24.
  3. Nakamura M, Honda Z, Waga I, et al. Endotoxin transduces Ca2+ signaling via platelet-activating factor receptor. FEBS Lett 1992;314:125-9.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Family
Assays
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Hematology
Ophthalmology
Cardiology
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Gastrointestinal
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Reference agonist:
CH3‐carbamyl PAF C‐16
EC50:
840 pM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CH3‐carbamyl PAF C‐16
EC50:
480 pM