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PAF receptor

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Target id: 334

Nomenclature: PAF receptor

Family: Platelet-activating factor receptor

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 342 1p35.3 PTAFR platelet activating factor receptor 10,36,50,61,65
Mouse 7 341 4 65.56 cM Ptafr platelet-activating factor receptor 30
Rat 7 341 5q36 Ptafr platelet-activating factor receptor 7
Previous and Unofficial Names Click here for help
PAFr | AGEPC receptor
Database Links Click here for help
Specialist databases
GPCRdb ptafr_human (Hs), ptafr_mouse (Mm), ptafr_rat (Rn)
Other databases
Alphafold P25105 (Hs), Q62035 (Mm), P46002 (Rn)
ChEMBL Target CHEMBL250 (Hs), CHEMBL3993 (Mm), CHEMBL4127 (Rn)
Ensembl Gene ENSG00000169403 (Hs), ENSMUSG00000056529 (Mm), ENSRNOG00000013231 (Rn)
Entrez Gene 5724 (Hs), 19204 (Mm), 58949 (Rn)
Human Protein Atlas ENSG00000169403 (Hs)
KEGG Gene hsa:5724 (Hs), mmu:19204 (Mm), rno:58949 (Rn)
OMIM 173393 (Hs)
Pharos P25105 (Hs)
RefSeq Nucleotide NM_000952 (Hs), NM_001164721 (Hs), NM_001164722 (Hs), NM_001164723 (Hs), NM_001081211 (Mm), NM_053321 (Rn)
RefSeq Protein NP_000943 (Hs), NP_001074680 (Mm), NP_445773 (Rn)
UniProtKB P25105 (Hs), Q62035 (Mm), P46002 (Rn)
Wikipedia PTAFR (Hs)
Natural/Endogenous Ligands Click here for help
methylcarbamyl PAF
PAF

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]PAF Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Full agonist 8.8 – 8.9 pKd 22,50
⤷ pKd 8.8 – 8.9 (Kd 1.6x10-9 – 1.3x10-9 M) [22,50]
PAF Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 7.5 – 7.9 pKi 50,53
⤷ pKi 7.5 – 7.9 [50,53]
PAF Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 8.2 pIC50 3
⤷ pIC50 8.2 [3]
2-O-ethyl-PAF C-16 Small molecule or natural product Hs Full agonist 7.7 pIC50 3
⤷ pIC50 7.7 [3]
2-O-methyl-PAF C-18 Small molecule or natural product Hs Full agonist 5.8 pIC50 3
⤷ pIC50 5.8 [3]
enantio PAF C-16 Small molecule or natural product Hs Full agonist 5.0 pIC50 3
⤷ pIC50 5.0 [3]
Agonist Comments
Some oxidised phospholipids (oxLDL) also behave as agonists at the PAF receptor [6,40,57,63], reviewed in [41] and [43]. In a murine model of melanoma, oxidised glycerophosphocholines (ox-GPCs) with PAF receptor agonist activity may enhance tumour growth by targeting host immune cells [59]. Enhanced clearance of damaged or altered cells (eg apoptotic cells) by phagocytosis has been reported to involve direct interaction of the PAF receptor on phagocytes and PAF-like molecules on the cell surface of the apoptotic cells [14].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PCA 4248 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 7.4 pA2 19
⤷ pA2 7.4 Displacement of [3H]PAF binding to polymorphonuclear cells. [19]
[3H]52770 RP Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.4 pKd 42
⤷ pKd 8.4 [42]
[3H]apafant Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 7.4 – 8.0 pKd 3,22,50
⤷ pKd 7.4 – 8.0 [3,22,50]
foropafant Small molecule or natural product Ligand has a PDB structure Hs Antagonist 10.3 pKi 25
⤷ pKi 10.3 [25]
ABT-299 Small molecule or natural product Hs Antagonist 9.5 pKi 1
⤷ pKi 9.5 [1]
ABT-491 Small molecule or natural product Ligand has a PDB structure Hs Antagonist 9.2 pKi 2
⤷ pKi 9.2 [2]
RP-52770 Small molecule or natural product Hs Antagonist 8.2 pKi 42
⤷ pKi 8.2 [42]
L659989 Small molecule or natural product Hs Antagonist 7.8 pKi 28
⤷ pKi 7.8 (Ki 1.43x10-8 M) [28]
10-OBn-7α-F-gingkolide B Small molecule or natural product Mm Antagonist 7.0 pKi 72
⤷ pKi 7.0 [72]
7α-Cl-ginkgolide B Small molecule or natural product Mm Antagonist 7.0 pKi 72
⤷ pKi 7.0 [72]
10-OBn-ginkgolide B Small molecule or natural product Mm Antagonist 6.9 pKi 72
⤷ pKi 6.9 [72]
BN 50739 Small molecule or natural product Hs Antagonist 6.9 pKi 67
⤷ pKi 6.9 [67]
apafant Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 5.2 – 7.5 pKi 53,67
⤷ pKi 5.2 – 7.5 [53,67]
7α-N3-ginkgolide B Small molecule or natural product Mm Antagonist 6.3 pKi 72
⤷ pKi 6.3 [72]
10-OBn-epi-ginkgolide C Small molecule or natural product Mm Antagonist 6.2 pKi 72
⤷ pKi 6.2 [72]
7α-NHMe-ginkgolide B Small molecule or natural product Mm Antagonist 6.2 pKi 72
⤷ pKi 6.2 [72]
ginkgolide B Small molecule or natural product Mm Antagonist 6.1 – 6.2 pKi 64,72
⤷ pKi 6.1 – 6.2 [64,72]
7α-F-ginkgolide B Small molecule or natural product Mm Antagonist 6.0 pKi 72
⤷ pKi 6.0 [72]
10-OBn-ginkgolide C Small molecule or natural product Mm Antagonist 5.8 pKi 72
⤷ pKi 5.8 [72]
7α-NHEt-ginkgolide B Small molecule or natural product Mm Antagonist 5.8 pKi 72
⤷ pKi 5.8 [72]
ginkgolide A Small molecule or natural product Mm Antagonist 5.8 pKi 64
⤷ pKi 5.8 [64]
7α-OCOCH2Ph-ginkgolide B Small molecule or natural product Mm Antagonist 5.6 pKi 72
⤷ pKi 5.6 [72]
rupatadine Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 5.4 pKi 46
⤷ pKi 5.4 (Ki 3.7x10-6 M) [46]
7-epi-ginkgolide C Small molecule or natural product Mm Antagonist 5.4 pKi 72
⤷ pKi 5.4 [72]
7α-NH2-ginkgolide B Small molecule or natural product Mm Antagonist 5.1 pKi 72
⤷ pKi 5.1 [72]
7α-OAc-ginkgolide B Small molecule or natural product Mm Antagonist 5.1 pKi 72
⤷ pKi 5.1 [72]
ginkgolide J Small molecule or natural product Mm Antagonist 5.0 pKi 64
⤷ pKi 5.0 [64]
ginkgolide C Small molecule or natural product Mm Antagonist 4.9 pKi 64
⤷ pKi 4.9 [64]
israpafant Small molecule or natural product Hs Antagonist 9.0 pIC50 50
⤷ pIC50 9.0 [50]
CV-6209 Small molecule or natural product Hs Antagonist 8.1 – 8.3 pIC50 23,50
⤷ pIC50 8.1 – 8.3 [23,50]
SDZ 64-412 Small molecule or natural product Hs Antagonist 7.2 pIC50 24
⤷ pIC50 7.2 [24]
CV-3988 Small molecule or natural product Hs Antagonist 6.8 pIC50 69
⤷ pIC50 6.8 (IC50 1.6x10-7 M) [69]
SCH 37370 Small molecule or natural product Hs Antagonist 6.2 pIC50 35
⤷ pIC50 6.2 [35]
SCH 40338 Small molecule or natural product Hs Antagonist 6.2 pIC50 35
⤷ pIC50 6.2 [35]
PCA 4248 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 5.4 pIC50 19
⤷ pIC50 5.4 (IC50 3.6x10-6 M) Inhibition of PAF-induced platelet aggregation. [19]
bepafant Small molecule or natural product Hs Antagonist 3.6 – 6.5 pIC50 19,26
⤷ pIC50 6.1 – 6.5 (IC50 8.3x10-7 – 3.2x10-7 M) Inhibition of PAF-induced platelet or neutrophil aggregation. [26]
pIC50 3.6 – 6.5 (IC50 2.5x10-4 – 3x10-7 M) Induction of apoptosis in human NB4 (acute promyelocytic leukemia) cells. [19]
View species-specific antagonist tables
Antagonist Comments
The above binding assays were performed using transfected cells, except references [1-2,24] which measured binding to preparations of platelet membranes, reference [42] which measured binding to human polymorphonuclear leukocytes and reference [35] which measured the inhibition of platelet aggregation.

The above table lists a small selection of the known PAF receptor antagonists. For reviews on PAF receptor antagonists see [13,66].
Immunopharmacology Comments
PAF deficiency results in defective inflammatory response to infection in mice.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Cellular signalling
Immuno Process:  Immune regulation
Immuno Process:  Chemotaxis & migration
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family
Gq/G11 family
G protein independent mechanism 		Adenylyl cyclase stimulation
Other - See Comments
Comments:  Other=Janus kinase/STAT
References:  8,16,37-38,57
Tissue Distribution Click here for help
Bone marrow stromal cells.
Species:  Human
Technique:  RT-PCR.
References:  17
Spermatozoa (proximal head, midpiece >> distal head, tail).
Species:  Human
Technique:  Immunofluorescent microscopy.
References:  55
Fallopian tubes.
Species:  Human
Technique:  RT-PCR and Western blotting.
References:  71
Dorsal root ganglion and spinal cord.
Species:  Mouse
Technique:  RT-PCR.
References:  45
Spleen > skeletal muscle, thioglycollate elicited macrophages > small intestine > resident peritoneal macrophages > lung > heart > liver > kidney > brain.
Species:  Mouse
Technique:  Northern blotting.
References:  30
Spleen > small intestine > kidney > lung > liver >> pancreas >> brain.
Species:  Rat
Technique:  Northern blotting.
References:  7
Microglia.
Species:  Rat
Technique:  in situ hybridisation, Northen blotting and RT-PCR.
References:  44
Pancreatic microvascular endothelial cells.
Species:  Rat
Technique:  Immunohistochemistry.
References:  21
Kidney: glomerulus > proximal convoluted tubule > proximal straight tubule > cortical collecting duct, outer medullary collecting duct, distal convoluted tubule > cortical thick ascending limb, medullary thick ascending limb.
Species:  Rat
Technique:  RT-PCR.
References:  4
Cerebral cortex (intense signals scattered randomly in all of the layers, moderate signals found in layers II-VI), olfactory bulb, hippocampus (intense signals scattered randomly, moderate signals found in the pyramidal cell layer and dentate gyrus), medial thalamus, hypothalamus, and cerebellum (intense signals were scattered randomly, slight to moderate signals were found in the granular cell and Purkinje cell layers).
Species:  Rat
Technique:  in situ hybridisation.
References:  44
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of PLCβ3 activity in HUVECs.
Species:  Human
Tissue:  HUVECs.
Response measured:  PLCβ3 activation via Gαq upon application of agonist.
References:  16
Measurement of membrane potential in Xenopus oocytes transfected with the human PAF recptor.
Species:  Human
Tissue:  Xenopus oocytes.
Response measured:  Production of an inward current upon application of an agonist.
References:  50
Measurement of IP3 levels in COS-7 cells transfected with the human PAF receptor.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  Accumulation of IP3 upon application of an agonist.
References:  50
Measurement of membrane potential in Xenopus oocytes transfected with the human PAF receptor.
Species:  Human
Tissue:  Xenopus oocytes.
Response measured:  Production of a Ca2+-activated Cl- current upon application of an agonist.
References:  65
Measurement of membrane potential in Xenopus oocytes transfected with the rat PAF receptor.
Species:  Rat
Tissue:  Xenopus oocytes.
Response measured:  Cl- channel opening.
References:  7
Measurement of cAMP levels in Human Umbilical Vein Endothelial cells (HEVECs) endogenously expressing the PAF receptor.
Measurement of PKA activity and subsequent signalling to Src.
Species:  Human
Tissue:  HUVECs.
Response measured:  Increase in cAMP levels via Gαq, subsequent increase in PKA activity and signalling to Src, upon application of an agonist.
References:  16
Measurement of FAK (Focal Adhesion Kinase) activity in HUVECs.
Species:  Human
Tissue:  HUVECs.
Response measured:  FAK activation via Gαq upon application of an agonist.
References:  16
Measurement of Ca2+ mobilisation in CHO cells transfected with the wild-type receptor or the Ala224 -> Asp substituted mutant PAF receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Equivalent Ca2+ mobilisation in both the wild-type and mutant receptors.
References:  22
Measurement of IP3 and cAMP levels in CHO cells transfected with the wild-type receptor or the Ala224 -> Asp substituted mutant PAF receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  IP3 production and inhibition of cAMP accumulation upon activation of the wild-type receptor. Both reduced with the mutant receptor.
References:  22
Measurement of chemotactic activity in CHO cells transfected with either the wild-type or the Ala224 -> Asp substituted mutant PAF receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Reduced chemotactic index with the mutant receptor.
References:  22
Measurement of Ca2+ levels in isolated rat microglial cells using fluorometric Ca2+ imaging.
Species:  Rat
Tissue:  Isolated microglia.
Response measured:  Elevated [Ca2+]i in response to PAF.
References:  44
Measurement of Ca2+ levels in cultured rat hippocampal cells using fluorometric Ca2+ imaging.
Species:  Rat
Tissue:  Cultured hippocampal cells.
Response measured:  Elevated [Ca2+]i in response to PAF.
References:  44
Measurement of arachidonic acid levels in isolated rat microglial cells endogenously expressing the PAF receptor.
Species:  Rat
Tissue:  Isolated microglia.
Response measured:  Arachidonic acid release is response to PAF.
References:  44
Physiological Functions Click here for help
Vasodilation.
Species:  Rat
Tissue:  Mesenteric arterial bed.
References:  34
Superoxide production.
Species:  Human
Tissue:  Eosinophils.
References:  5
Cell proliferation, motility and angiogenic response.
Species:  Human
Tissue:  Breast cancer cells.
References:  9
Enhancement of excitatory synaptic transmission.
Species:  Rat
Tissue:  Cultured hippocampal neurons.
References:  12
PAF receptor activation may be an initiator of neuronal dysfunction and cell death involved with HIV-1 associated dementia.
Species:  Human
Tissue:  Primary neurons.
References:  54
Cell aggregation.
Species:  Human
Tissue:  Leukocytes and platelets.
References:  15
Regulation of angiogenesis and inflammatory response.
Species:  Mouse
Tissue:  In vivo
References:  20
Mediation of lipopolysaccharide (LPS)-induced systemic inflammation.
Species:  Rat
Tissue:  In vivo.
References:  33
Parasite phagocytosis.
Species:  Mouse
Tissue:  Cardiac tissue.
References:  68
Upregulation of bradykinin B1 receptors as measured by bradykinin-induced oedema.
Species:  Rat
Tissue:  In vivo.
References:  18
Intrathecal administration of PAF induces tactile allodynia (pain induced from normally non-painful stimuli) and thermal hyperalgesia at the level of the spinal cord.
Species:  Mouse
Tissue:  In vivo.
References:  45
Neovascularisation (thought to be linked to the PAF-induced upregulation of angiogenic factors VEGF and FGF-2 as found in HUVECs).
Species:  Mouse
Tissue:  Cornea.
References:  39
Bronchoconstiction via the production of thromboxane A2, LTC4, LTD4 and LTE4.
Species:  Mouse
Tissue:  Airway smooth muscle.
References:  47
Platelet aggregation.
There appears to be a synergistic interaction between 5-HT and PAF on platelet aggregation, TXA2 formation and ERK1/2 phosphorylation. It is thought to involve PLC/Ca2+, COX and MAPK pathways.
Species:  Human
Tissue:  Platelets.
References:  62
Physiological Consequences of Altering Gene Expression Click here for help
PAF receptor knockout mice exhibit reduced anaphylactic symptoms, although normal neuronal development, reproduction and responses to bacterial endotoxin.
A possible use for PAF receptor antagonists could be to prevent anaphylactic responses without serious side-effects.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  29
PAF receptor knockout mice exhibit a decreased airway hyperresponsiveness to muscarinic cholinergic stimulation in an asthma model, although no difference to the eosinophilic inflammatory response when compared to the wild-type.
This suggests that PAF acts downstream of the airway inflammation in brionchial asthma.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  31
PAF receptor knockout mice and wild-type mice were innoculated intranasally with S. pneumoniae. The knockout mice had an increased resistance to pneumococcal pneumonia compared to the wild-type mice.
This study suggests that S. pneumoniae uses the PAF receptor to induce pneumonia.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  56
PAF receptor knockout mice exhibit increased angiogenesis and decreased inflammation in comparison to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  20
The embryos of PAF receptor knockout mice show an increase in the thickness of the external granular layer of the cerebellum.
In vitro studies using cerebellar granule neurons from PAF receptor knockout mice show reduced migration when compared to wild-type neurons.
However, PAF still had some effect on the migration of the wild-type neurons, suggesting an additional receptor-independent pathway for PAF.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  70
PAF receptor knockout mice are found to be protected from the spacial learning deficits, increased oxidative stress, inflammatory signalling and apoptosis that are associated with intermittent hypoxia (IH) during sleep.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  58
PAF receptor knockout mice exhibit reduced high frequency stimulation-induced LTP in hippocampal dentate gyrus cells compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  11
PAF receptor knockout mice and wild-type mice were infected with Strongyloides venezuelensis. The PAF receptor knockout mice exhibited a decrease in inflammatory response and subsequent delay in worm elimination. They also showed a reduction in the number of eggs produced by the worms, suggesting that PAF receptor-mediated responses may effect egg output.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  51
Transgenic mice overexpressing the PAF receptor exhibit enhanced acid aspiration-induced lung injury and respitatory failure.
PAF receptor knockout mice exhibit reduced acid aspiration-induced lung injury and respitatory failure.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  48
Transgenic mice overexpressing the PAF receptor exhibit epidermal hyperproliferation and an increase in dermal melanocytes. The PAF receptor gene was found in keratinocytes, not melanocytes, suggesting that the receptor has a role in the growth of epidermal keratinocytes.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  60
Comparison of PAF receptor knockout mice and wild-type mice following ovariectomies suggested that the PAF receptor links eostrogen depletion with osteoporosis.
It is suggested that a reduction in eostrogen enhances PAF production. In wild-type mice this alters osteoclast cell functions and leads to bone resorption. In PAF receptor knockout mice this bone loss is reduced.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  27
PAF receptor knockout mice infected with the hemoflagellate parasite Trypanosoma cruzi exhibited increased parasite replication and increased inflammatory response.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  68
Transgenic mice overexpressing the PAF receptor exhibited bronchoconstiction mediated via the PAF-induced production of thromboxane A2 and and cysteneinly leukotrienes LTC4, LTD4 and LTE4.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  47
Transgenic mice overexpressing the PAF receptor exhibit hyperresponsiveness to metacholine and PAF, blocked by atropine. This suggests that this hyperresponsiveness may involve the muscarinic pathway.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  49
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Ptafrtm1Eit Ptafrtm1Eit/Ptafrtm1Eit
involves: C57BL/6		 MGI:106066  MP:0005167 abnormal blood-brain barrier function PMID: 16299272 
Ptafrtm1Eit Ptafrtm1Eit/Ptafrtm1Eit
involves: C57BL/6		 MGI:106066  MP:0004003 abnormal vascular endothelial cell physiology PMID: 16299272 
Ptafrtm1Tksh Ptafrtm1Tksh/Ptafrtm1Tksh
involves: 129P2/OlaHsd * C57BL/6		 MGI:106066  MP:0001876 decreased inflammatory response PMID: 14742561 
Ptafrtm1Tksh Ptafrtm1Tksh/Ptafrtm1Tksh
C57BL/6-Ptafr		 MGI:106066  MP:0002411 decreased susceptibility to bacterial infection PMID: 14767826 
Ptafrtm1Tksh Ptafrtm1Tksh/Ptafrtm1Tksh
involves: 129P2/OlaHsd * C57BL/6		 MGI:106066  MP:0005027 increased susceptibility to parasitic infection PMID: 14742561 
Ptafrtm1Tksh Ptafrtm1Tksh/Ptafrtm1Tksh
involves: 129P2/OlaHsd * C57BL/6		 MGI:106066  MP:0005596 increased susceptibility to type I hypersensitivity reaction PMID: 9607919 
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  An Ala224 -> Asp substitution in the 3rd cytoplasmic loop of the PAF receptor has been found in Japanese subjects, with an estimated allele frequency of 7.8% among the Japanese population.
This polymorphism has been linked to an increased susceptibility to multiple sclerosis.
Amino acid change:  A224D
References:  22,52
General Comments
Transgenic mice overexpressing the guinea-pig PAF receptor have shown bronchial hyperreactivity to methacholine and increased mortality when exposed to bacterial endotoxin [32].

References

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1. Albert DH, Conway RG, Magoc TJ, Tapang P, Rhein DA, Luo G, Holms JH, Davidsen SK, Summers JB, Carter GW. (1996) Properties of ABT-299, a prodrug of A-85783, a highly potent platelet activating factor receptor antagonist. J Pharmacol Exp Ther, 277 (3): 1595-606. [PMID:8667228]

2. 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]

3. Aoki Y, Nakamura M, Kodama H, Matsumoto T, Shimizu T, Noma M. (1995) A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor. J Immunol Methods, 186 (2): 225-31. [PMID:7594622]

4. Asano K, Taniguchi S, Nakao A, Watanabe T, Kurokawa K. (1996) Distribution of platelet activating factor receptor mRNA along the rat nephron segments. Biochem Biophys Res Commun, 225 (2): 352-7. [PMID:8753768]

5. Bartemes KR, McKinney S, Gleich GJ, Kita H. (1999) Endogenous platelet-activating factor is critically involved in effector functions of eosinophils stimulated with IL-5 or IgG. J Immunol, 162: 2982-2989. [PMID:10072549]

6. Beaudeux JL, Said T, Ninio E, Ganné F, Soria J, Delattre J, Soria C, Legrand A, Peynet J. (2004) Activation of PAF receptor by oxidised LDL in human monocytes stimulates chemokine releases but not urokinase-type plasminogen activator expression. Clin Chim Acta, 344 (1-2): 163-71. [PMID:15149885]

7. Bito H, Honda Z, Nakamura M, Shimizu T. (1994) Cloning, expression and tissue distribution of rat platelet-activating-factor-receptor cDNA. Eur J Biochem, 221 (1): 211-8. [PMID:8168510]

8. Brown SL, Jala VR, Raghuwanshi SK, Nasser MW, Haribabu B, Richardson RM. (2006) Activation and regulation of platelet-activating factor receptor: role of G(i) and G(q) in receptor-mediated chemotactic, cytotoxic, and cross-regulatory signals. J Immunol, 177 (5): 3242-9. [PMID:16920964]

9. Bussolati B, Biancone L, Cassoni P, Russo S, Rola-Pleszczynski M, Montrucchio G, Camussi G. (2000) PAF produced by human breast cancer cells promotes migration and proliferation of tumor cells and neo-angiogenesis. Am J Pathol, 157 (5): 1713-25. [PMID:11073830]

10. Chase PB, Halonen M, Regan JW. (1993) Cloning of a human platelet-activating factor receptor gene: evidence for an intron in the 5'-untranslated region. Am J Respir Cell Mol Biol, 8 (3): 240-4. [PMID:8383507]

11. Chen C, Magee JC, Marcheselli V, Hardy M, Bazan NG. (2001) Attenuated LTP in hippocampal dentate gyrus neurons of mice deficient in the PAF receptor. J Neurophysiol, 85 (1): 384-90. [PMID:11152738]

12. Clark GD, Happel LT, Zorumski CF, Bazan NG. (1992) Enhancement of hippocampal excitatory synaptic transmission by platelet-activating factor. Neuron, 9 (6): 1211-6. [PMID:1334422]

13. Curtin ML. (1998) Current status of platelet-activating factor antagonists. Expert Opinion on Therapeutic Patents, 8: 703-711.

14. de Oliveira SI, Fernandes PD, Amarante Mendes JG, Jancar S. (2006) Phagocytosis of apoptotic and necrotic thymocytes is inhibited by PAF-receptor antagonists and affects LPS-induced COX-2 expression in murine macrophages. Prostaglandins Other Lipid Mediat, 80 (1-2): 62-73. [PMID:16846787]

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