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 (provisional nomenclature recommended by NC-IUPHAR [2]) is activated by PAF and other suggested endogenous ligands are oxidized phosphatidylcholine [7] and lysophosphatidylcholine [10]. It may also be activated by bacterial lipopolysaccharide [9].

Note that a previously recommended radioligand ([³H]apafant; K_d 44.6 nM) is currently unavailable.

* Key recommended reading is highlighted with an asterisk

* Foord SM, Bonner TI, Neubig RR, Rosser EM, Pin JP, Davenport AP, Spedding M, Harmar AJ. (2005) International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev, 57 (2): 279-88. [PMID:15914470]

* Ishii S, Shimizu T. (2000) Platelet-activating factor (PAF) receptor and genetically engineered PAF receptor mutant mice. Prog Lipid Res, 39 (1): 41-82. [PMID:10729607]

Montrucchio G, Alloatti G, Camussi G. (2000) Role of platelet-activating factor in cardiovascular pathophysiology. Physiol Rev, 80 (4): 1669-99. [PMID:11015622]

* Prescott SM, Zimmerman GA, Stafforini DM, McIntyre TM. (2000) Platelet-activating factor and related lipid mediators. Annu Rev Biochem, 69: 419-45. [PMID:10966465]

Shimizu T. (2009) Lipid mediators in health and disease: enzymes and receptors as therapeutic targets for the regulation of immunity and inflammation. Annu Rev Pharmacol Toxicol, 49: 123-50. [PMID:18834304]

Summers JB, Albert DH. (1995) Platelet activating factor antagonists. Adv Pharmacol, 32: 67-168. [PMID:7748804]

1. Albert DH, Magoc TJ, Tapang P, Luo G, Morgan DW, Curtin M, Sheppard GS, Xu L, Heyman HR, Davidsen SK et al.. (1997) Pharmacology of ABT-491, a highly potent platelet-activating factor receptor antagonist. Eur J Pharmacol, 325 (1): 69-80. [PMID:9151941]

2. Foord SM, Bonner TI, Neubig RR, Rosser EM, Pin JP, Davenport AP, Spedding M, Harmar AJ. (2005) International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev, 57 (2): 279-88. [PMID:15914470]

3. Fukunaga K, Ishii S, Asano K, Yokomizo T, Shiomi T, Shimizu T, Yamaguchi K. (2001) Single nucleotide polymorphism of human platelet-activating factor receptor impairs G-protein activation. J Biol Chem, 276 (46): 43025-30. [PMID:11560941]

4. Goldring WP, Alexander SP, Kendall DA, Pattenden G. (2005) Novel phomactin analogues as PAF receptor ligands. Bioorg Med Chem Lett, 15 (13): 3263-6. [PMID:15922596]

5. Herbert JM, Laplace MC, Cailleau C, Maffrand JP. (1993) Effect of SR 27417 on the binding of [3H]PAF to rabbit and human platelets and human polymorphonuclear leukocytes. J Lipid Mediat, 7 (1): 57-78. [PMID:8395255]

6. Hwang SB, Lam MH, Alberts AW, Bugianesi RL, Chabala JC, Ponpipom MM. (1988) Biochemical and pharmacological characterization of L-659,989: an extremely potent, selective and competitive receptor antagonist of platelet-activating factor. J Pharmacol Exp Ther, 246 (2): 534-41. [PMID:2841449]

7. Marathe GK, Davies SS, Harrison KA, Silva AR, Murphy RC, Castro-Faria-Neto H, Prescott SM, Zimmerman GA, McIntyre TM. (1999) Inflammatory platelet-activating factor-like phospholipids in oxidized low density lipoproteins are fragmented alkyl phosphatidylcholines. J Biol Chem, 274 (40): 28395-404. [PMID:10497200]

8. Nakamura M, Honda Z, Izumi T, Sakanaka C, Mutoh H, Minami M, Bito H, Seyama Y, Matsumoto T, Noma M et al.. (1991) Molecular cloning and expression of platelet-activating factor receptor from human leukocytes. J Biol Chem, 266 (30): 20400-5. [PMID:1657923]

9. Nakamura M, Honda Z, Waga I, Matsumoto T, Noma M, Shimizu T. (1992) Endotoxin transduces Ca2+ signaling via platelet-activating factor receptor. FEBS Lett, 314 (2): 125-9. [PMID:1333988]

10. Ogita T, Tanaka Y, Nakaoka T, Matsuoka R, Kira Y, Nakamura M, Shimizu T, Fujita T. (1997) Lysophosphatidylcholine transduces Ca2+ signaling via the platelet-activating factor receptor in macrophages. Am J Physiol, 272 (1 Pt 2): H17-24. [PMID:9038918]

11. Parent JL, Gouill CL, Escher E, Rola-Pleszczynski M, Staková J. (1996) Identification of transmembrane domain residues determinant in the structure-function relationship of the human platelet-activating factor receptor by site-directed mutagenesis. J Biol Chem, 271 (38): 23298-303. [PMID:8798529]

12. Svetlov S, Nigam S. (1993) Evidence for the presence of specific high affinity cytosolic binding sites for platelet-activating factor in human neutrophils. Biochem Biophys Res Commun, 190 (1): 162-6. [PMID:8380690]

Rebecca Hills (Past curator) Satoshi Ishii Department of Immunology Graduate School of Medicine Akita University 1-1-1 Hondo Akita City Akita 010-8543, Japan Sonia Jancar (Past chairperson) University of San Paulo, Brazil Thomas McIntyre Department of Molecular Cardiology Lerner Research Institute The Cleveland Clinic Foundation 9500 Euclid Ave. Cleveland, OH 44195 USA Ewa Ninio (Past chairperson) Directeur de Recherche au CNRS INSERM UMRS937 (anciennement UMRS525)/6ème étage Faculté de Médecine Pierre et Marie Curie 91, bd de l'Hôpital 75634 Paris Cx13 France Francisco Jose Oliveira Rios University of San Paulo, Brazil Chris O'Neill E25 - Royal North Shore Hospital The University of Sydney NSW 2006 Australia Jeffery B. Travers Indiana University School of Medicine 550 N. University Blvd. Suite 3240 Indianapolis, IN USA Mark Whittaker Evotec (UK) Ltd 111 Milton Park Abingdon Oxfordshire OX 14 4RZ UK