Human PTAFR

Figure. Concentration-dependent activation of PTAFR by CH3‐carbamyl PAF C‐16

Reporter cells were transfected with either the expression plasmid for human platelet activating factor receptor (PTAFR) or the mock plasmid and treated with various concentrations of CH3‐carbamyl PAF C‐16. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 840 pM.

Nomenclature
platelet activating factor receptor
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
Panels
à la carte, Immunology/Infection, Hematology, Ophthalmology, Cardiology, Respiratory, Gastrointestinal, Urology/Reproduction, Human non-orphan GPCRs

Platelet-activating factor receptor

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

Related Receptors

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Human
PTAFR
platelet activating factor receptor
Mouse
Ptafr
platelet-activating factor receptor