Page last updated: 2024-11-07

1-hexadecyl-2-acetyl-glycero-3-phosphocholine

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Description

Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine : A 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID108156
CHEMBL ID1235246
CHEBI ID44811
SCHEMBL ID433361
MeSH IDM0112596

Synonyms (92)

Synonym
chebi:44811 ,
CHEMBL1235246
gtpl1831
[3h]paf
[3h]platelet activating factor
paf c-16 ,
gtpl1833
[(2r)-2-acetyloxy-3-hexadecoxypropyl] 2-trimethylazaniumylethyl phosphate
1-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine
c16-paf acether
3,5,9-trioxa-4-phosphapentacosan-1-aminium, 7-(acetyloxy)-4-hydroxy-n,n,n-trimethyl-, inner salt, 4-oxide, (7r)- (9ci)
hag-pc
3,5,9-trioxa-4-phosphapentacosan-1-aminium, 7-(acetyloxy)-4-hydroxy-n,n,n-trimethyl-, inner salt, 4-oxide, (r)-
3,5,9-trioxa-4-phosphapentacosan-1-aminium, 7-(acetyloxy)-4-hydroxy-n,n,n-trimethyl-, hydroxide, inner salt, 4-oxide, (7r)-
platelet-activating factor c16
1-o-hexadecyl-2-o-acetyl-sn-glyceryl-3-phosphorylcholine
beta-acetyl-gamma-o-hexadecyl-l-alpha-phosphatidylcholine
1-o-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine
1-o-palmityl-2-acetyl-sn-glycero-3-phosphocholine monohydrate
1-o-hexadecyl-2-acetyl-sn-glyceryl-3-phosphorylcholine
blood platelet-activating factor acether
blood platelet-activating factor
c16-paf
ethanaminium, 2-[[[[(2r)-2-(acetyloxy)-3-(hexadecyloxy)propyl]oxy]hydroxyphosphinyl]oxy]-n,n,n-trimethyl-, inner salt
paf acether
3,5,9-trioxa-4-phosphapentacosan-1-aminium, 7-(acetyloxy)-4-hydroxy-n,n,n-trimethyl-, hydroxide, inner salt, 4-oxide, (r)-
3-sn-phosphatidylcholine, 1-hexadecyl-2-acetyl
1-o-hexadecyl-2-acetyl-sn-glycerophosphocholine
1-o-hexadecyl-platelet-activating factor
platelet-activating factor acether
1-o-hexadecyl-2-o-acetyl-sn-glycero-3-phosphocholine
74389-68-7
2-acetyl-1-hexadecyl-sn-glycero-3-phosphocholine
hexadecyl-paf-acether
platelet-activating factor
PAF ,
aprl
platelet activating factor
LMGP01020046
pc(o-16:0/2:0)
paf 16
1-hexadecyl-2-acetyl-glycero-3-phosphocholine
DB02261
NCGC00161373-02
NCGC00161373-01
paf (c16)
1-o-hexadecyl-2-o-acetyl-sn-glycero-3-phosophocholine
NCGC00161373-03
HMS1989I10
paf c16
BML3-E03
HMS1361I10
HMS1791I10
(2r)-2-acetoxy-3-(hexadecyloxy)propyl 2-(trimethylammonio)ethyl phosphate
[(2r)-2-acetyloxy-3-hexadecoxypropyl] 2-(trimethylazaniumyl)ethyl phosphate
bdbm85035
cas_65154-06-5
bloodplatelet-activatingfactor
(2r)-2-(acetyloxy)-3-(hexadecyloxy)propyl 2-(trimethylammonio)ethyl phosphate
unii-42ewd89i80
42ewd89i80 ,
c16 paf
1-o-hexadecyl paf
c16:0 paf
2-o-acetyl-1-o-hexadecyl-sn-glycero-3-phosphocholine
(r)-7-(acetyloxy)-4-hydroxy-n,n,n-trimethyl-3,5,9-trioxa-4-phosphapentacosan-1-aminium hydroxide inner salt 4-oxide
SCHEMBL433361
DTXSID00225377
(7r)-7-(acetyloxy)-4-hydroxy-n,n,n-trimethyl-3,5,9-trioxa-4-phosphapentacosan-1-aminium-4-oxide
HVAUUPRFYPCOCA-AREMUKBSSA-N
platelet-activating factor c-16
AKOS024457347
HMS3402I10
HMS3648N18
mfcd00043214
paf(c16)
((2r)-2-acetyloxy-3-hexadecoxypropyl) 2-trimethylazaniumylethyl phosphate
platelet-activating factor (1-o-hexadecyl)
3,5,9-trioxa-4-phosphapentacosan-1-aminium, 7-(acetyloxy)-4-hydroxy-n,n,n-trimethyl-, inner salt, 4-oxide, (7r)-
pc(o18:0)
paf (platelet activating factor)
(r)-2-acetoxy-3-(hexadecyloxy)propyl (2-(trimethylammonio)ethyl) phosphate
c16-02:0 pc, 1-o-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine, powder
c16-02:0 pc, 1-o-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine, chloroform
Q420577
beta-acetyl-gamma-o-hexadecyl-l-alpha-phosphatidylcholine hydrate
platelet activating factor c 16;1-o-hexadecyl-2-o-acetyl-sn-glyceryl-3-phosphorylcholine
3,5,9-trioxa-4-phosphapentacosan-1-aminium,7-(acetyloxy)-4-hydroxy-n,n,n-trimethyl-, inner salt, 4-oxide, (7r)-
CS-0029366
HY-108635
ZCA38968
A917451

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" No clinically relevant drug related adverse events or changes in laboratory or vital parameters such as blood pressure, heart rate, respiratory rate and ECG were observed."( Pharmacodynamics, pharmacokinetics and safety profile of the new platelet-activating factor antagonist apafant in man.
Adamus, WS; Birke, FW; Brecht, HM; Heuer, HO; Kempe, ER, 1991
)
0.28
" Nevertheless, no clinically significant drug-related effects on vital and laboratory parameters or obvious drug-dependent adverse reactions were observed."( Safety, tolerability, and pharmacologic activity of multiple doses of the new platelet activating factor antagonist WEB 2086 in human subjects.
Adamus, WS; Brecht, HM; Heuer, H; Meade, CJ, 1989
)
0.28
" CP-46,665 was the most toxic compound, but did not reveal significant differences between nonneoplastic bone marrow and leukemic cells when added in concentrations greater than 1 microgram/ml."( Cytotoxic effects of ether lipids and derivatives in human nonneoplastic bone marrow cells and leukemic cells in vitro.
Berdel, WE; Eibl, H; Fink, U; Fromm, M; Jehn, U; Rastetter, J; Reichert, A; Schick, HD; Ulm, K; Unger, C, 1987
)
0.27
"Cyclosporin (CsA) is a potent immunosuppressive drug whose main side-effect is nephrotoxicity."( Prevention of cyclosporin nephrotoxicity with a platelet-activating factor (PAF) antagonist.
Aupetit, B; Baghos, W; Bagnis, C; Braquet, P; Deray, G; Dubois, M; Jacobs, C; Jacquiaud, C; Pirotzky, E, 1996
)
0.29
" It has been shown that a vasoactive role may be partially responsible for the toxic effects of CN."( The effects of EDRF/NO releasers or calcium ionophore A23187 on cyanide toxicity in mice.
Baskin, SI; Lempka, JC; Nealley, EW, 1996
)
0.29
" The results show that HDL-like phospholipid particles effectively inhibit the toxic effect of phospholipids and other lipid-soluble factors."( Lipoprotein-like phospholipid particles inhibit the smooth muscle cell cytotoxicity of lysophosphatidylcholine and platelet-activating factor.
Ares, M; Cercek, B; Dahlgren, B; Hultgårdh Nilsson, A; Nilsson, J; Shah, PK; Westman, J, 1998
)
0.3
" If so, rPAF-AH can be used for the treatment of those adverse reactions."( Vasoactive side effects of intravenous immunoglobulin preparations in a rat model and their treatment with recombinant platelet-activating factor acetylhydrolase.
Agterberg, J; Bleeker, WK; Hack, CE; Koenderman, AH; Kuijpers, TW; Rigter, GM; Teeling, JL; Tool, AT; Verhoeven, AJ, 2000
)
0.31
" No clinically important adverse events were observed."( Effect of a platelet-activating factor receptor antagonist, E5880, on cerebral vasospasm after aneurysmal subarachnoid hemorrhage--open clinical trial to investigate efficacy and safety.
Endo, S; Hirashima, Y; Kobayashi, N; Nukui, H; Takaku, A, 2001
)
0.31
" In the present study, neurones treated with three different phospholipase A2 inhibitors were resistant to the toxic effects of PrP peptides or a synthetic miniprion (sPrP106)."( The role of platelet activating factor in prion and amyloid-beta neurotoxicity.
Bate, C; Salmona, M; Williams, A, 2004
)
0.32
" All treatments were well tolerated and no serious adverse events were recorded."( A randomized, double-blind, parallel-group study, comparing the efficacy and safety of rupatadine (20 and 10 mg), a new PAF and H1 receptor-specific histamine antagonist, to loratadine 10 mg in the treatment of seasonal allergic rhinitis.
Dumur, JP; Izquierdo, I; Pérez, I; Saint-Martin, F, 2004
)
0.32
"The present results suggest that rupatadine 10 mg a day may be a valuable and safe alternative for the symptomatic treatment of seasonal allergic rhinitis."( A randomized, double-blind, parallel-group study, comparing the efficacy and safety of rupatadine (20 and 10 mg), a new PAF and H1 receptor-specific histamine antagonist, to loratadine 10 mg in the treatment of seasonal allergic rhinitis.
Dumur, JP; Izquierdo, I; Pérez, I; Saint-Martin, F, 2004
)
0.32
" The administration of a toxic dose of acetaminophen (3."( Platelet-activating factor (PAF) involvement in acetaminophen-induced liver toxicity and regeneration.
Basayiannis, AC; Demopoulos, CA; Grypioti, AD; Mykoniatis, MG; Papadimas, GK; Papadopoulou-Daifoti, Z; Theocharis, SE, 2005
)
0.33
" As C16:0 PAF is a naturally occurring lipid involved in cellular signaling, it is likely that mechanisms exist to protect cells against its toxic effects."( Srf1 is a novel regulator of phospholipase D activity and is essential to buffer the toxic effects of C16:0 platelet activating factor.
Ahmed, F; Baetz, K; Bennett, SA; Bryan, J; Figeys, D; Kabbani, N; Kennedy, MA; Lambert, JP; Swayne, LA, 2011
)
0.37
"The review of these data indicates that rupatadine is highly selective for histamine H1-receptors, exhibits additional PAF antagonism in in vitro and in vivo studies, does not cross the blood-brain barrier, and has similar adverse events comparable with other second-generation antihistamines."( Rupatadine: global safety evaluation in allergic rhinitis and urticaria.
Bachert, C; González-Núñez, V; Mullol, J, 2016
)
0.43
" The safety assessments showed that all treatment related side effects were of mild intensity and there were no serious adverse events (SAEs) or withdrawals due to treatment-emergent adverse events (TEAEs) in this study."( Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial.
Ferber, G; Fernandes, S; Izquierdo, I; Lorch, U; Santamaría, E; Täubel, J, 2016
)
0.43
"This study demonstrated that rupatadine is safe and well tolerated by Japanese healthy subjects."( Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial.
Ferber, G; Fernandes, S; Izquierdo, I; Lorch, U; Santamaría, E; Täubel, J, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
" Apafant (WEB 2086, CAS 105219-56-5), a novel synthetic PAF receptor antagonist, was administered to a total of 101 healthy volunteers within 5 studies to investigate its pharmacologic activity, pharmacokinetic behaviour and safety profile."( Pharmacodynamics, pharmacokinetics and safety profile of the new platelet-activating factor antagonist apafant in man.
Adamus, WS; Birke, FW; Brecht, HM; Heuer, HO; Kempe, ER, 1991
)
0.28
" As a whole the pharmacodynamic profile of isbufylline is promising and, in the clinical setting, this compound might exert enhanced antiasthma effects coupled to a low incidence of central and cardiovascular adverse effects."( Pharmacodynamic profile of isbufylline, a new antibronchospastic xanthine devoid of central excitatory actions.
Antonelli, T; Bacciarelli, C; Ballati, L; Beani, L; Borea, PA; Giachetti, A; Manzini, S; Meini, S, 1990
)
0.28
" The pharmacokinetic behaviour of both PAF-acether and lyso-PAF-acether can be described by a three-compartment model."( Pharmacokinetic study of 3H-labelled PAF-acether II. Comparison with 3H-labelled lyso-PAF-acether after intravenous administration in the rabbit and protein binding.
Berger, JA; Chabard, JL; Godeneche, D; Lartigue-Mattei, C; Petit, J, 1984
)
0.27
" A pharmacokinetic study and a preliminary metabolic evaluation were carried out in three rabbits, after the intravenous administration of 3H-labelled PAF-acether (40 Ci/mM, CEA, Saclay, France)."( Pharmacokinetic study of PAF-acether. Preliminary results after the intravenous administration of a 3H-labelled product to the rabbit.
Berger, JA; Chabard, JL; Godeneche, D; Lartigue-Mattei, C, 1982
)
0.26
"The pharmacodynamic profile of a new xanthine derivative, 7-[(2,2-dimethyl)propyl]-1-methyl xanthine (CAS 155006-67-0, MX2/120), was investigated in comparison with theophylline."( Pharmacodynamic profile of the new potent antibronchospastic agent 7-[(2,2-dimethyl)propyl]-1-methyl xanthine.
Ballati, L; Boni, P; Castellucci, A; Evangelista, S; Perretti, F; Toja, E; Tramontana, M, 1995
)
0.29
" In addition, time to maximal activity and half-life differed in PMNs and in plasma (4."( Pharmacokinetics and pharmacodynamics of neutrophil-associated ciprofloxacin in humans.
Blardi, P; Capecchi, PL; Ceccatelli, L; De Lalla, A; Di Perri, T; Pasini, L; Volpi, L, 1995
)
0.29
"00 h and the half-life for each animal was almost the same as that after intravenous administration."( Development of radioimmunoassay for the novel platelet activating factor receptor antagonist, E6123, and its application to pharmacokinetics in laboratory animals.
Abe, Y; Ida, S; Kagei, Y; Kusano, K; Miyazawa, S; Tadano, K; Tanaka, S; Ueda, M; Yuzuriha, T, 1994
)
0.29
"A nonlinear mixed-effects modelling approach was used to analyse pharmacokinetic and pharmacodynamic data from two Phase I studies of a platelet activating factor (PAF) antagonist under development for the treatment of seasonal allergic rhinitis."( A pharmacokinetic/pharmacodynamic model for a platelet activating factor antagonist based on data arising from Phase I studies.
Aarons, L; Brearley, C; Evans, L, 2005
)
0.33
" The method has been successfully applied to a pharmacokinetic study of rupatadine and its major metabolite after oral administration of 10, 20 and 40mg rupatadine tablets to healthy Chinese volunteers."( Simultaneous determination of rupatadine and its metabolite desloratadine in human plasma by a sensitive LC-MS/MS method: application to the pharmacokinetic study in healthy Chinese volunteers.
Fan, G; Hong, Z; Wei, H; Wen, J; Wu, Y, 2009
)
0.35
"0 mg/kg ginkgolide B, parameters of pharmacokinetics of ginkgolide B were: Tmax were all (0."( [Study on the pharmacokinetics of ginkgolide B for injection in rats].
Jiao, HY; Suo, QL; Zhang, XT, 2012
)
0.38
"Exposure to rupatadine as measured by Cmax and AUC was found to increase in a dose dependent manner over the dose range of 10-40 mg for both single and multiple dose administration."( Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial.
Ferber, G; Fernandes, S; Izquierdo, I; Lorch, U; Santamaría, E; Täubel, J, 2016
)
0.43
" Half-life of bilobalide after dosing the tablet was around 5 h."( Human pharmacokinetics of ginkgo terpene lactones and impact of carboxylation in blood on their platelet-activating factor antagonistic activity.
Du, FF; Duan, XN; Gao, Q; Huang, YH; Jia, WW; Li, C; Li, L; Li, YF; Liu, XW; Niu, W; Olaleye, OE; Wang, FQ; Wen, Q; Xu, F; Yang, JL; Zhong, CC, 2018
)
0.48

Compound-Compound Interactions

ExcerptReferenceRelevance
"Differential effects on human platelet function of thromboxane A2 (TXA2) synthetase inhibition singly and of TXA2 synthetase inhibition combined with TXA2/prostaglandin endoperoxide receptor antagonism were revealed, using ridogrel as a probe."( Effect of thromboxane A2 synthetase inhibition, singly and combined with thromboxane A2/prostaglandin endoperoxide receptor antagonism, on inositol phospholipid turnover and on 5-HT release by washed human platelets.
de Chaffoy de Courcelles, D; De Clerck, F, 1990
)
0.28
" When one of the NSAID was given combined with mepyramine and with methysergide, bronchoconstriction was suppressed, but thrombocytopenia and hypotension persisted."( Non-steroidal anti-inflammatory drugs if combined with anti-histamine and anti-serotonin agents interfere with the bronchial and platelet effects of "platelet-activating factor" (PAF-acether).
Chignard, M; Lefort, J; Medeiros, MC; Vargaftig, BB; Wal, F, 1982
)
0.26
" Treatment of rats with WEB, alone or in combination with Zileuton, did not attenuate ANIT-induced liver injury as assessed by increases in plasma alanine aminotransferase or gamma-glutamyl transferase activities."( Platelet activating factor receptor blockade alone or in combination with leukotriene synthesis inhibition does not ameliorate alpha-naphthylisothiocyanate-induced hepatotoxicity.
Bailie, MB; Fink, GD; Pearson, JM; Roth, RA, 1996
)
0.29
"To investigate the role and significance of PAF in the early pulmonary injury following burns combined with endotoxemia in rats."( [The role and significance of PAF in the early pulmonary injury following burns combined with endotoxemia in rats].
Chen, Y; Huang, H; Liu, Y, 1999
)
0.3
"An animal model, in which rats were subjected to 20% TBSA III degree burns combined with intraperitoneal injection of lipopolysaccharide (LPS), was used for this experiment."( [The role and significance of PAF in the early pulmonary injury following burns combined with endotoxemia in rats].
Chen, Y; Huang, H; Liu, Y, 1999
)
0.3
"PAF was one of the inflammatory mediators to precede TNF changes during burns combined with endotoxemia in the early stage of pulmonary injury."( [The role and significance of PAF in the early pulmonary injury following burns combined with endotoxemia in rats].
Chen, Y; Huang, H; Liu, Y, 1999
)
0.3
"The results suggest that PAF plays an very important pathogenic role in the early lung injury resulted from burns combined with endotoxemia."( [The role and significance of PAF in the early pulmonary injury following burns combined with endotoxemia in rats].
Chen, Y; Huang, H; Liu, Y, 1999
)
0.3

Bioavailability

ExcerptReferenceRelevance
" The bioavailability of the drug was low (less than or equal to 10%) for all monkeys, probably due to rapid first pass metabolism."( Metabolism of the platelet-activating factor antagonist (+/-)-trans-2-(3'-methoxy-5'-methylsulphonyl-4'-propoxyphenyl)-5-(3",4" ,5"- trimethoxyphenyl)tetrahydrofuran (L-659,989) in rhesus monkeys.
Arison, BH; Bugianesi, RL; Chabala, JC; Chang, MN; Hucker, HB; Ponpipom, MM; Sweeney, BM; Thomson, KL; White, SD, 1991
)
0.28
" More than 90% of alprazolam is absorbed after an oral dose; the absorption rate is dose independent."( The pharmacology of alprazolam: a review.
Huybrechts, I,
)
0.13
" These results suggest that by depressing the bioavailability of PAF, CRP may be an important modulator of platelet activation during acute inflammatory reactions."( C-reactive protein inhibits binding of platelet-activating factor to human platelets.
Filep, JG; Földes-Filep, E; Hermán, F; Kelemen, E, 1991
)
0.28
" The pharmacokinetic study of CsA showed that this lack of efficacy of combined treatment may be interpreted as the decreased CsA bioavailability observed when the animals also received RP 48740."( Prolonged survival of renal transplants in nonimmunized and hyperimmunized rats receiving a platelet-activating factor antagonist.
Freiche, JC; Lang, J; Sedivy, P; Touraine, JL, 1990
)
0.28
" By introduction of selective enzyme inhibitors, it was determined that the bioavailability of each mediator class occurred without regulatory effects on the others."( Pharmacologic regulation of mediator generation and release from the murine bone marrow derived mast cell.
Austen, KF; Lewis, RA; Robin, JL, 1985
)
0.27
" Previous work with related pyrido[2,1-b]-quinazoline-8-carboxamides suggests that the presence of such an alkyl group improves bioavailability by rendering the resulting compounds resistant to degradation by liver amidases."( Biphenylcarboxamide derivatives as antagonists of platelet-activating factor.
Clader, JW; Crowley, H; LeMahieu, RA; O'Donnell, M; Tilley, JW; Welton, AF; Wirkus, M; Zawoiski, S, 1989
)
0.28
" The bioavailability of the parent drug, calculated by dose-normalized AUC and deconvolution methods, was only 10-15% from the low dose, but increased to approximately 40% following the high dose."( Pharmacokinetics of SDZ 64-412, a novel antiasthmatic agent, following intravenous, oral, and inhalation dosing in the rat.
Athill, LV; Charnick, SB; Karara, AH; Lau, DT; Tse, FL; Yu, Z, 1994
)
0.29
" The superiority of the GI physiology regulated-dogs over the intact dogs was confirmed by comparative bioavailability studies using two classes of preparations of poorly water-soluble 4-(2-chlorophenyl)-2-[2-(4-isobutylphenyl)ethyl]-6,9-dimethyl-6H- thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine (Y-24180)."( Gastrointestinal physiology-regulated dogs: utilization of a bioavailability study of a new thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]-diazepine, an antagonist of platelet-activating factor, and its preparations.
Kawazoe, Y; Mizuta, H; Sagara, K; Shibata, M; Yamada, I, 1994
)
0.29
" The bioavailability of ginkgolides in these extracts was assessed in rabbits in comparison with a commercially available standardized 24/6 extract."( The bioavailability of ginkgolides in Ginkgo biloba extracts.
Li, CL; Wong, YY, 1997
)
0.3
" The failure of a receptor blocker of leukotrienes to moderate disease expression suggests either a less important role for these chemicals in AOM or an insufficient bioavailability of the specific MK 571 inhibitor."( Expression of acute otitis media after receptor blockade of platelet activating factor, thromboxane, and leukotrienes in the chinchilla.
Alper, CM; Burckart, GJ; Diven, WF; Doyle, WJ; Evans, RW; Jaffe, R, 1998
)
0.3
" The transport parameter measured (K(in)) proves that 1a is able to cross this biological barrier, but a pharmacokinetic study reveals its weak bioavailability in rats."( Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
Bensaid, O; Cisternino, S; Clayette, P; Dereuddre-Bosquet, N; Dong, CZ; Dormont, D; Heymans, F; Huet, J; Lamouri, A; Martin, M; Redeuilh, C; Rousselle, C; Scherrmann, JM; Serradji, N, 2004
)
0.32
" Apparent oral bioavailability of ginkgolides A and B was mostly >100%, while that of ginkgolides C and J was 6-15%."( Human pharmacokinetics of ginkgo terpene lactones and impact of carboxylation in blood on their platelet-activating factor antagonistic activity.
Du, FF; Duan, XN; Gao, Q; Huang, YH; Jia, WW; Li, C; Li, L; Li, YF; Liu, XW; Niu, W; Olaleye, OE; Wang, FQ; Wen, Q; Xu, F; Yang, JL; Zhong, CC, 2018
)
0.48

Dosage Studied

ExcerptRelevanceReference
" Given orally, RP 58802B (5 mg/kg, 60 min before challenge) produced a greater than three-fold shift to the right of the dose-response curve and depressed the maximum response to histamine by 39 +/- 11%."( RP 58802B, a long-acting beta 2-adrenoceptor agonist: assessment of antiasthma activity in the guinea-pig in vivo.
Lewis, SA; Raeburn, D; Underwood, SL, 1992
)
0.28
"Dissolution testing of solid oral dosage forms plays a very important part both in the development of new products and in quality control."( The automation of dissolution testing of solid oral dosage forms.
Lamparter, E; Lunkenheimer, CH,
)
0.13
" Based on dose-response experiments, the relative rank order of potency for the three chemoattractants was: LTB4 = FMLP greater than PAF for filter alone barrier; LTB4 greater than FMLP greater than PAF for HUVE cell barrier; and FMLP greater than LTB4 greater than PAF for MDCK and A549 epithelial cell barriers."( Degree of neutrophil chemotaxis is dependent upon the chemoattractant and barrier.
Abbas, MK; Carolan, EJ; Casale, TB, 1992
)
0.28
" For assay of drug concentrations in plasma of rats dosed intravenously or orally with tritium-labeled I, we have developed a high-performance liquid chromatographic (HPLC) method which directly resolved the two enantiomers."( Determination of enantiomeric concentrations of a 2,5-diaryltetrahydrofuran (L-668,750), a platelet-activating factor receptor antagonist, in rat plasma using a chiral alpha 1-acid glycoprotein high-performance liquid chromatographic column.
Alvaro, RF; Chiu, SH; Rosegay, A, 1992
)
0.28
", dose-response curves for U46619 and U44069 were shifted to the right in a parallel manner."( Blockade of thromboxane/endoperoxide receptor-mediated responses in the pulmonary vascular bed of the cat by sulotroban.
Babycos, CR; Hood, JS; Ibrahim, IN; Kadowitz, PJ; McMahon, TJ; Nossaman, BD; Ragheb, MS, 1992
)
0.28
" Dose-response curves for U-46619 and U-44069 were shifted to the right in a parallel manner, and daltroban had no significant effect on responses to norepinephrine, serotonin, angiotensin II, BAY K 8644, endothelin-(ET) 1, ET-2, or platelet-activating factor (PAF)."( Daltroban blocks thromboxane responses in the pulmonary vascular bed of the cat.
Babycos, CR; Hood, JS; Ibrahim, IN; Kadowitz, PJ; McMahon, TJ; Nossaman, BD, 1992
)
0.28
" Dose-response curves to methacholine were determined in all animals at the start of the experiment."( The effect of platelet activating factor antagonist on ozone-induced airway inflammation and bronchial hyperresponsiveness in guinea pigs.
Bethel, RA; Tan, WC, 1992
)
0.28
" These results demonstrate the specificity and dose-response characteristics of PAF antagonists in cultured human endothelial cells and suggest that a PAF antagonist could be a valuable therapeutic agent in certain human diseases where PAF activation of endothelial cells may have a critical role."( Antagonism of platelet-activating factor-induced increase in cytosolic free calcium concentration in human endothelial cells.
Hirafuji, M; Shinoda, H, 1992
)
0.28
" We found that a PAF dosage of 6 micrograms/kg increased the tracheal dye content 7-fold compared to controls."( Effects of platelet-activating factor on vascular permeability and granulocyte recruitment in the rat trachea.
Brokaw, JJ; Kirsch, CM; Prow, DM; White, GW, 1991
)
0.28
" Dose-response studies revealed that a maximal two- to three-fold increase in release of TNF alpha occurs at 10-100 pM PAF."( Tumor necrosis factor release by human monocytes stimulated with platelet-activating factor.
Rose, JK; Ruis, NM; Valone, FH, 1991
)
0.28
" The dose-response curve characterizing the dependence of ROI production on the concentration of platelet-activating factor (PAF) showed that stimulation occurred within a concentration range of 2 x 10(-9)M to 5 x 10(-6)M."( Platelet-activating factor stimulates receptor-mediated formation of reactive oxygen intermediates in human monocytes.
Kozyukov, AV; Makarova, OV; Porodenko, NV; Pustynnikov, MG; Severin, ES; Sokolovsky, AA, 1991
)
0.28
" When compounds were administered intravenously, at a dosage (1 mg/kg) which fully abolished responses to intravenous histamine, the observed rank order for inhibition of PAF-induced hyperreactivity was: ketotifen greater than cetirizine greater than acrivastine greater than KB-2413 greater than oxatomide greater than azelastine greater than terfenadine = astemizole = clemastine = mepyramine = loratadine = saline."( Histamine(H1) antagonists and airway hyperreactivity in the guinea-pig.
Chapman, ID; Hoshiko, K; Morley, J, 1991
)
0.28
" Tachyphylaxis was not noted in 5 control pigs given sequential repeats of the PAF dosing series."( In vivo enhancement of platelet activating factor-induced prostacyclin production by OKY-046, a selective inhibitor of thromboxane A2 synthase.
Davenport, NJ; Feuerstein, GZ; Goldstein, RE, 1991
)
0.28
" In seven conscious sheep, specific lung resistance (SRL) was measured before and after x-xo challenge; approximately 30 min later when SRL had returned to baseline, airway responsiveness to carbachol was determined from dose-response curves by calculating the cumulative provocating dose of carbachol in breath units (BU, defined as one breath of a 1% wt/vol carbachol solution) that increased SRL 400% over baseline (PD400)."( Lipid mediators contribute to oxygen-radical-induced airway responses in sheep.
Abraham, WM; Ahmed, A; Cortes, A; Garcia, L; Lansing, MW; Lauredo, IT; Mansour, E; Wanner, A, 1991
)
0.28
" BN 50739 caused a right shift in PAF dose-response curves of platelet aggregation both in vitro and ex vivo."( Inhibitory effect of new PAF antagonists on PAF-induced rabbit platelet aggregation in vitro and ex vivo.
Farhat, M; Feuerstein, G; Rabinovici, R; Yue, TL,
)
0.13
" Dose-response curves illustrate that acrylyl-PAF was about half an order of magnitude less potent than PAF as an agonist."( Acrylyl-PAF, a synthetic platelet-activating factor analogue.
Duffy-Krywicki, RH; Olson, MS; Steinhelper, ME,
)
0.13
" An intradermal dose-response study showed that rIL-8 is an extremely potent inducer of selective neutrophil infiltration in canine skin."( Recombinant human interleukin-8 is a potent activator of canine neutrophil aggregation, migration, and leukotriene B4 biosynthesis.
Ahnfelt-Rønne, I; Kirstein, D; Larsen, CG; Skak-Nielsen, T; Thestrup-Pedersen, K; Thomsen, HK; Thomsen, MK, 1991
)
0.28
" Alteration of airways function was assessed by measuring specific pulmonary conductance (SGL) and dose-response relationships to inhaled histamine, where airways responsiveness was expressed as the effective concentration causing 50% of maximal change in specific airways conductance (EC50SGL)."( Body temperature modulates the effect of platelet-activating factor (PAF) on airways responsiveness in the rabbit.
Hill, M; Irvin, CG; Nieminen, MM, 1991
)
0.28
" The dose-response curves for renal blood flow and systemic blood pressure generated by intrarenal C18-PAF administration were approximately 7 fold to the right of the dose-response curves generated by C16-DPAF."( Vasorelaxant effect of C16-PAF and C18-PAF on renal blood flow and systemic blood pressure in the anesthetized rat.
Buckalew, VM; Handa, RK; Strandhoy, JW, 1991
)
0.28
" Dose-response and time-course experiments indicated no significant differences in PAF-induced hypodense versus normodense EOS chemotactic responses."( Comparison of platelet-activating factor-induced chemotaxis of normodense and hypodense eosinophils.
Casale, TB; Little, MM, 1991
)
0.28
"The temporal and dose-response relationships of platelet-activating-factor (PAF)-induced changes in the concentrations of cytosolic Ca2+ ([Ca2+]i), Ins(1,4,5)P3 and 1,2-diacylglycerol (DAG) were examined."( The relationship between cytosolic Ca2+, sn-1,2-diacylglycerol and inositol 1,4,5-trisphosphate elevation in platelet-activating-factor-stimulated rabbit platelets. Influence of protein kinase C on production of signal molecules.
Elmore, M; Kellie, S; Murphy, CT; Westwick, J, 1991
)
0.28
" Dose-response curves were generated cumulatively by infusing 10(-10) to 10(-7) mol PAF dissolved in Krebs-Henseleit solution buffer containing 4% bovine serum albumin into the BC or PC."( Effects of PAF on isolated rat airways perfused with blood-free solution.
Blumenthal, RN; Kirchhoff, CF; Leff, AR; Munoz, NM; Strek, ME, 1991
)
0.28
" Propranolol (1 mg/kg) produced a small shift to the left and atropine (1 mg/kg) and the serotonin antagonist, methysergide (1 mg/kg), produced a small shift to the right in the bombesin dose-response curve."( Bombesin-induced bronchoconstriction in the guinea pig: mode of action.
Barnes, PJ; Belvisi, MG; Stretton, CD, 1991
)
0.28
"1 mg/kg) of Y-24180 also prevented hemoconcentration due to PAF in a dose dependent manner and produced a parallel shift of the PAF dose-response curve."( Pharmacological actions of Y-24180: I. A potent and specific antagonist of platelet-activating factor.
Aratani, H; Setoguchi, M; Tahara, T; Terasawa, M, 1990
)
0.28
" The effect was most pronounced 5 min after dosing the inhibitor and detectable over a period of 30 min."( Platelet-activating factor (PAF) inhibitory profile of KO-286011 on blood platelets in vitro and in vivo.
Hofmann, B; Kertscher, HP; Ostermann, G; Till, U, 1990
)
0.28
", shifted the dose-response curves of platelet-activating factor-induced platelet aggregation to the right in a parallel manner."( Pharmacological properties of YM264, a potent and orally active antagonist of platelet-activating factor.
Hara, H; Horie, M; Mase, T; Nagaoka, H; Saito, M; Tomioka, K; Yamada, T,
)
0.13
"Using the hamster cheek pouch preparation and intravital microscopy and fluorometry methods, we quantitated the dose-response effects of topically applied platelet-activating factor (PAF) on microvascular permeability, vessel diameter and leukocyte adhesion and investigated the biochemical pathways of this compound."( Acute microcirculatory effects of platelet-activating factor.
Dillon, PK; Durán, WN, 1990
)
0.28
" Specific lung resistance (SRL) was measured to assess bronchial responses to PAF, and airway responsiveness was determined by deriving a provocative dose of carbachol in breath units causing an increase in SRL to 4 L times centimeters of H2O per liters per second (PD4) from carbachol dose-response curves."( PAF-induced airway responses in sheep: effects of a PAF antagonist and nedocromil sodium.
Abraham, WM; Ahmed, T; D'Brot, J; Fernandez, A; Mansour, E; Soler, M, 1990
)
0.28
" PCA 4248 behaved as a competitive and selective antagonist in [3H]serotonin secretion studies on rabbit platelets, since it displaced rightwards log dose-response curves and lacked any effect on thrombin- and ionophore A23187-induced platelet secretion."( 1,4-Dihydropyridines, a new class of platelet-activating factor receptor antagonists: in vitro pharmacologic studies.
de Casa-Juana, MF; García, MC; Gijón, MA; Ortega, MP; Priego, JG; Sanchez Crespo, M; Sunkel, C, 1990
)
0.28
" The PAF receptor antagonism with BN 50730 was overcome when 10-fold larger doses of PAF were administered and the dose-response curves for changes in lung resistance and dynamic compliance were shifted to the right in a parallel manner."( Influence of SK&F 95587 and BN 50730 on bronchoconstrictor responses in the cat.
Beckerman, RC; Bellan, JA; Braquet, P; Dyson, MC; Kadowitz, PJ; McNamara, DB; Minkes, RK; Wegmann, MJ, 1990
)
0.28
" Although LTC4 was as potent as LTD4 in stimulating TxB2 generation, LTC4's dose-response curve was shifted significantly to the right by AT-125, an irreversible gamma-glutamyl transpeptidase inhibitor, suggesting that at least a part of LTC4 sensitized lungs with antigen (0."( Evidence that peptidoleukotriene is a prerequisite for antigen-dependent thromboxane synthesis in IgG1-passively sensitized guinea pig lungs.
Breslow, R; Cheng, JB; Conklyn, MJ; Pillar, JS; Shirley, JT; Showell, HJ, 1990
)
0.28
" PAF stimulates the release of IL-1 beta activity into THP-1 cell supernatants with a multiphasic dose-response curve very similar to that for monocytes."( Synergistic increases in IL-1 synthesis by the human monocytic cell line THP-1 treated with PAF and endotoxin.
Barthelson, RA; Potter, T; Valone, FH, 1990
)
0.28
" The amount of dye extracted from the paw showed a clear dose-response relationship to the dose of each agonist injected into the paw."( Assessment of vascular permeability increase in the mouse by dye leakage during paw edema.
Hayashi, M; Oh-ishi, S; Qu, XF; Yamaki, K, 1990
)
0.28
" The slopes of the dose-response curves for all three compounds were linear and parallel, with statistically different potencies."( The effect of platelet-activating factor (PAF), histamine, and ethanol on vascular permeability of the guinea pig conjunctiva.
Kim, ED; Roth, SI; Stock, EL; Thamman, R; Walsh, MK, 1990
)
0.28
" In this study, we quantitated the dose-response effects of topically applied PAF on microvascular permselectivity and investigated the biochemical pathways of this compound."( Effect of platelet-activating factor on microvascular permselectivity: dose-response relations and pathways of action in the hamster cheek pouch microcirculation.
Dillon, PK; Durán, WN, 1988
)
0.27
" When platelets were pretreated with either BDZR ligand, and then exposed to various concentrations of WEB 2086, there was no alteration of the dose-response relationship of the hetrazepine on PAF-induced aggregation, as reflected by threshold concentration, ED50, or maximum inhibition seen with WEB 2086."( The benzodiazepine receptor ligands RO 5-4864 and RO 15-1788 do not block the inhibition of PAF-induced platelet aggregation seen with the hetrazepine WEB2086.
Griffin, K; Hong, T; Levy, JV, 1989
)
0.28
" Incubation of eosinophils with the PAF-antagonist WEB 2086 led to a parallel shift of the dose-response curve to the right, indicating a competitive antagonism."( Stimulation of degranulation from human eosinophils by platelet-activating factor.
Barnes, PJ; Chung, KF; Dent, G; Kroegel, C; Venge, P; Yukawa, T, 1989
)
0.28
" In explanted rat hypothalami maintained viable in vitro, PAF stimulated immunoreactive CRH secretion in a bell-shaped dose-response fashion."( The alkyl-ether phospholipid platelet-activating factor is a stimulator of the hypothalamic-pituitary-adrenal axis in the rat.
Bernardini, R; Brucke, T; Calogero, AE; Chrousos, GP; Ehrlich, YH; Gold, PW, 1989
)
0.28
" WEB 2086 shifted the Paf dose-response curve rightwards in a parallel manner."( Interaction of the Paf antagonist WEB 2086 and its hetrazepine analogues with human platelets and endothelial cells.
Benveniste, J; Bidault, J; Delautier, D; Hirafuji, M; Keraly, CL; Korth, R, 1989
)
0.28
" Airway responsiveness was determined from the slopes of dose-response curves of SRL vs."( YM461, a PAF antagonist, blocks antigen-induced late airway responses and airway hyperresponsiveness in allergic sheep.
Abraham, WM; Ahmed, A; Garrido, R; Stevenson, JS; Tomioka, K, 1989
)
0.28
" The dose-response curves for the SCP were found to be virtually identical for both sheep and human platelets."( Measuring platelet function with platelet shape change, an early event in aggregation.
Beaumont, DO; Mock, RG; Slattery, CW; Whitten, KW, 1989
)
0.28
" In five dogs, dose-response curves were generated by rapid intra-arterial injection of 10(-10) to 10(-6) mol PAF into the isolated tracheal circulation; tracheal contractile response was measured isometrically in situ."( PAF-induced contraction of canine trachea mediated by 5-hydroxytryptamine in vivo.
Blake, JS; Leff, AR; Mack, MM; Moss, J; Munoz, NM; Murphy, TM, 1989
)
0.28
" The dose-response to PAF was shifted to the right by the concomitant intra-arterial infusion of the PAF antagonist SRI 63-441."( Inhibition of vasoconstriction by platelet activating factor in the in situ blood perfused rat mesentery.
Gerkens, JF, 1989
)
0.28
" Administration of Ascaris antigen caused a leftward shift in the dose-response curve to serotonin and only mild tachyphylaxis to the maximal response to histamine."( Evidence for platelet-activating factor secretion during immune activation in dogs.
Blake, JS; Kelly, E; Leff, AR; Mack, MM; Munoz, NM; Murphy, TM; Stimler-Gerard, NP; Tutins, C, 1989
)
0.28
" Previous treatment with 1 microM indomethacin (IND) or 10 microM quinacrine (QUIN) markedly displaced the dose-response curves for Ach on OAS preparations to the left, whereas the EC50 of His was only increased by QUIN."( Tracheal responsiveness to histamine, PAF-acether and acetylcholine in normal and actively ovalbumin-sensitized guinea pigs.
Calixto, JB; Medeiros, YS; Torres, RC, 1989
)
0.28
" The dose-response curve for fall in BP was shifted to the right by one order of magnitude."( Platelet-activating factor (Paf) antagonist, WEB 2086, protects against Paf-induced hypotension in Macaca fascicularis.
Antoniw, JW; Izumi, T; Piper, PJ; Stanton, AW, 1989
)
0.28
" For these studies, airway responsiveness was determined from slopes of carbachol dose-response curves (DRC) performed at base line (prechallenge) and 2 h after Ascaris suum antigen challenges in the following three protocols: 1) antigen challenge alone (control trial), 2) WEB-2086 (1 mg/kg iv) given 30 min before antigen challenge (WEB pretreatment), and 3) WEB-2086 given 2 h after antigen challenge, immediately before the postchallenge DRC (WEB posttreatment)."( A PAF antagonist blocks antigen-induced airway hyperresponsiveness and inflammation in sheep.
Abraham, WM; Sielczak, MW; Solèr, M, 1989
)
0.28
" Aggregometry was performed on platelet-rich plasma samples from blood taken 1 h before dosing with Tanakan and 2, 4 and 8 h after intake of Tanakan."( Tanakan inhibits platelet-activating-factor-induced platelet aggregation in healthy male volunteers.
Caffrey, E; Darragh, A; Guinot, P; Lambe, R, 1989
)
0.28
" All antagonists produced a shift to the right in the dose-response curve to Paf (0."( Antagonism of platelet activating factor-induced chemiluminescence in guinea-pig peritoneal macrophages in differing states of activation.
Bittner, C; Lambrecht, G; Parnham, MJ, 1989
)
0.28
" A method that avoided tachyphylaxis encountered in prior investigations was developed for isometric measurement of multiple dose-response effects."( Parasympathetic involvement in PAF-induced contraction in canine trachealis in vivo.
Leff, AR; Munoz, NM; Popovich, KJ; Shioya, T; Stimler-Gerard, NP; White, SR, 1987
)
0.27
" The inhibition was shown to be specific and competitive with PAF on its receptor by the following observations: parallel shift of the dose-response curve; crossing of double reciprocal plots on the intersection of the ordinate; and no inhibition on other autacoids such as bradykinin, histamine, 5-hydroxytryptamine and LTC4."( Characterization of the activity of a platelet activating factor antagonist, CV-3988.
Hayashi, M; Kimura, J; Nomura, H; Oh-Ishi, S; Tsushima, S, 1987
)
0.27
" We determined the nebulizer concentration of PAF which reduced specific airway conductance (SGaw) 35% (PC35 SGaw) and the slope of the PAF dose-response curve."( Mechanism of platelet activating factor-induced bronchoconstriction in humans.
Patterson, R; Rubin, AH; Smith, LJ, 1988
)
0.27
" To study the vascular receptor responsible for L-PAF-induced vasodilation, dose-response curves to NE and ang II were established with and without L-PAF (10(-7) M)."( L-platelet activating factor induces changes on renal vascular resistance, vascular reactivity, and renin release in the isolated perfused rat kidney.
Gerber, JG; Mathias, M; Nies, AS; Scherf, H; Schwertschlag, U, 1987
)
0.27
" Inhibition of PAF by SRI 63-441 alone, at the dosage and schedule used in these experiments, did not significantly prolong xenograft survival or function."( Prolongation of pig-to-dog renal xenograft survival by modification of the inflammatory mediator response.
Banner, B; Chapchap, P; Esquivel, CO; Makowka, L; Mazzaferro, V; Miller, C; Pan, C; Podesta, L; Pressley, D; Todo, S, 1987
)
0.27
" CVF and PAF were also injected separately at the same dosage to other groups of rats."( Cobra venom factor, an activator of the complement system, enhances the bowel necrosis induced by platelet-activating factor.
Arroyave, CM; Arroyave, JL; Gonzalez-Crussi, F; Hsueh, W; Llausas-Magana, E; Torre-Amione, G,
)
0.13
"Platelet-activating factor (PAF), 1-o-alkyl-2-acetyl-sn-glyceryl-3-phosphoryl choline, induced acute bronchoconstriction in the guinea pig when intravenously administered in a very small dosage (30 ng/kg)."( Bronchoconstriction induced by platelet-activating factor in the guinea pig and its inhibition by CV-3988, a PAF antagonist: serial changes in findings of lung histology and bronchoalveolar lavage cell population.
Ishii, A; Miyamoto, T; Shiga, J; Suzuki, S; Takizawa, H, 1988
)
0.27
"The release of inflammatory mediators (histamine, PGD2, TxB2, and LTC4) from purified human lung mast cells was characterized by kinetic and anti-IgE dose-response parameters."( Characterization of inflammatory mediator release from purified human lung mast cells.
Adkinson, NF; Lichtenstein, LM; MacGlashan, DW; Peters, SP; Pinckard, RN; Schleimer, RP, 1986
)
0.27
" Immature megakaryocytes revealed the same responsiveness to titrated amounts of the various factors tested, with similar slopes to the dose-response curves."( Immature megakaryocytes in the mouse: synergistic response to megakaryocyte potentiator, thrombopoietic stimulatory factor with interleukin 3.
Oon, SH; Williams, N, 1987
)
0.27
" Histamine dose-response curves were performed before and 4 h after PAF administration."( Effect of platelet-activating factor on aerosol histamine responsiveness in awake sheep.
Christman, BW; Lefferts, PL; Snapper, JR, 1987
)
0.27
"025-16 micrograms/paw) were followed by a bell-shaped dose-response curve for oedema."( Interactions between local inflammatory and systemic haematological effects of PAF-acether in the rat.
Castro, HC; Cordeiro, RS; Lima, MC; Martins, MA; Neto, F; Silva, PM; Vargaftig, BB, 1987
)
0.27
" In dose-response studies, the amount of AGEPC required to induce a lethal response in 50% of the animals tested (LD50) was found to inversely correlate with age."( Ontogeny of the responsiveness to intravenous platelet-activating factor.
Angle, MJ; McManus, LM; Pinckard, RN; Showell, HJ, 1987
)
0.27
" administered L-652,731 gave a dose-response inhibition of PAF-induced lysosomal hydrolase secretion and extravasation with ED50 values of 1 and 3 mg/kg, respectively."( Inhibition of the platelet activating factor (PAF)-induced in vivo responses in rats by trans-2,5-(3,4,5-trimethoxyphenyl) tetrahydrofuran (L-652,731), a PAF receptor antagonist.
Biftu, T; Doebber, TW; Wu, MS, 1986
)
0.27
" The time course and dose-response relationship of the early response was determined and a synergistic interaction between PAF-acether and prostaglandin E2 established."( Inflammatory characteristics of PAF-acether in the skin of experimental animals and man.
Archer, CB; MacDonald, DM; Morley, J; Page, CP; Paul, W, 1985
)
0.27
" This was associated with increasing inhibition of ex vivo platelet aggregation induced by platelet-activating factor during the dosing period, but inhibition of arachidonic acid-induced aggregation did not increase cumulatively during dosing and collagen-induced aggregation was not inhibited."( Cyclooxygenase inhibition, platelet function, and metabolite formation during chronic sulfinpyrazone dosing.
FitzGerald, GA; Pedersen, AK, 1985
)
0.27
" The induction of thrombocytopenia by embryo culture media displayed a dose-response curve that was parallel to that of the platelet-activating factor, 1-0-alkyl-2-acetyl-sn-glycero(3)phosphocholine."( Examination of the causes of early pregnancy-associated thrombocytopenia in mice.
O'Neill, C, 1985
)
0.27
"The platelet-activating factor (PAF) produced by mouse embryos showed similar kinetics of action and dose-response curve, in a bioassay, as did 1-0-alkyl-2-acetyl-sn-glyceryl-3-phosphocholine (PAF-acether)."( Partial characterization of the embryo-derived platelet-activating factor in mice.
O'Neill, C, 1985
)
0.27
" Leukotrienes, the chemotactic fragment of the fifth component of complement (C5a des arg), N-formyl-L-methionylyl-L-leucyl-L-phenylalanine (FMLP), platelet-activating factor (PAF), and phorbol myristate acetate (PMA) increased the nonadherence of human leukocytes to glass with bell-shaped dose-response curves."( Various authentic chemoattractants mediating leukocyte adherence inhibition.
Thomson, DM, 1984
)
0.27
" Since C18- AGPC suppressed not only the pressor response to noradrenaline but also to angiotensin II and vasopressin, and furthermore, did not disturb the dose-response curve of noradrenaline in the isolated aorta, the possibility of the agent being an alpha-adrenergic antagonist is ruled out."( Mechanism(s) of the hypotensive effect of synthetic 1-O-octadecyl-2-O-acetyl-glycero-3-phosphorylcholine.
Kamitani, T; Katamoto, M; Katsuta, K; Kikuchi, H; Kumada, S; Ono, T; Tatsumi, M, 1984
)
0.27
" Finally, in a dosage which blocked degranulation, verapamil inhibited calcium uptake."( Role of extracellular calcium and neutrophil degranulation responses to 1-O-alkyl-2-O-acetyl-sn-glycero-3-phosphocholine.
Lees, CJ; McCall, CE; O'Flaherty, JT; Swendsen, CL, 1981
)
0.26
" The parallel antigen-induced dose-response relationship, along with the superimposable time-course of the extracellular appearance, of beta-hexosaminidase, PAF-acether, and both leukotrienes indicated that the origin of these diverse mediators was from a common cell type with IgE-Fc receptors."( Antigen-initiated release of platelet-activating factor (PAF-acether) from mouse bone marrow-derived mast cells sensitized with monoclonal IgE.
Austen, KF; Lewis, RA; Mencia-Huerta, JM; Razin, E, 1983
)
0.27
" PAF release precedes permeability changes and both show a parallel dose-response pattern plateauing for doses higher than 1 mg."( Platelet-activating factor: an effector substance of the vasopermeability changes induced by the infusion of immune aggregates in the mouse.
Alonso, F; Iñarrea, P; Sanchez-Crespo, M, 1983
)
0.27
" Under phase-contrast microscopy, PAF caused contraction of mesangial cells with a dose-response and time-course parallel to that for PGE2 synthesis."( Effect of platelet-activating factor and serum-treated zymosan on prostaglandin E2 synthesis, arachidonic acid release, and contraction of cultured rat mesangial cells.
Baud, L; Hagege, J; Perez, J; Satriano, JA; Schlondorff, D, 1984
)
0.27
" The time-course and dose-response relationship of the early response has been determined and a synergistic interaction between PAF-acether and prostaglandin E2 established."( Inflammatory characteristics of platelet activating factor (PAF-acether) in human skin.
Archer, CB; MacDonald, DM; Morley, J; Page, CP; Paul, W, 1984
)
0.27
" The desensitizing activities of 14 analogues of PAF-acether were explored with particular attention to the dose-response dependency of the desensitization process."( Effect of structural analogues of PAF-acether on platelet desensitization.
Benveniste, J; Borrel, MC; Coëffier, E; Keraly, CL; Tencé, M, 1983
)
0.27
" Further studies indicated that monocyte binding to endothelial cells follows similar dose-response kinetics as the up-regulation of integrins and can be partially blocked by Abs to CD11b and CD11c."( Regulation of monocyte integrin expression by beta-family chemokines.
Newton, RC; Vaddi, K, 1994
)
0.29
" No differences in ELGV dose-response curves to LTD4 were seen in A23187- and vehicle-exposed animals."( Inhaled A23187 produces a preferential sensitization to substance P.
Bendele, AM; Cockerham, SL; Silbaugh, SA; Stengel, PW, 1993
)
0.29
" When indomethacin (30 microM) was added to the perfusing blood, the dose-response curve for the pulmonary hypertensive responses produced by PAF was strongly reduced (90%) in comparison to control preparations, whereas the bronchoconstrictor effects of PAF were only partially diminished (23%)."( Mechanisms of pulmonary vasoconstriction and bronchoconstriction produced by PAF in the guinea-pig: role of platelets and cyclo-oxygenase metabolites.
Argiolas, L; del Basso, P; Fabi, F, 1995
)
0.29
" Comparisons of relative potency 30 min post dosing between emedastine and other anti-histamines demonstrated that emedastine is equipotent to ketotifen, and 7, 7, 10, 10, 100, 357, 3333, and 5813 times more potent than brompheniramine, chlorpheniramine, clemastine, pyrilamine, levocabastine, pheniramine, diphenhydramine, and antazoline, respectively."( Preclinical efficacy of emedastine, a potent, selective histamine H1 antagonist for topical ocular use.
Parnell, DW; Spellman, JM; Stephens, DJ; Yanni, JM, 1994
)
0.29
" Dose-response analysis revealed that maximal reduction of IL-1 binding was reached at FMLP concentrations that were also optimal for chemotaxis (50% effective dose = 5 x 10(-9) M)."( Chemoattractants induce rapid release of the interleukin 1 type II decoy receptor in human polymorphonuclear cells.
Colotta, F; Fadlon, EJ; Mantovani, A; Matteucci, C; Orlando, S; Sozzani, S, 1995
)
0.29
" Since PAF has unusual dose-response characteristics in vitro, this study investigated the effects of different doses or concentrations of PAF given by intravenous and aerosol administration in anesthetized rabbits."( Bimodal effect of platelet-activating factor (PAF) on airways responsiveness in the rabbit.
Henson, PM; Irvin, CG; Nieminen, MM,
)
0.13
" On the other hand, such concentrations of PAF inhibited the ciliary activity in a dose-response fashion within 5 min in the presence of alveolar macrophages."( Presence of bronchoalveolar lavage fluid necessary for platelet activating factor-induced ciliary depression.
Hayashi, M; Kakinoki, Y; Nakai, Y; Ohashi, Y; Ohno, Y; Okamoto, H; Sakamoto, H; Sugiura, Y; Tanaka, A, 1994
)
0.29
" Terfenadine, at concentrations achievable at standard dosing regimens, has anti-inflammatory properties in vitro."( Effect of terfenadine on human eosinophil and neutrophil chemotactic response and generation of superoxide.
Eda, R; Hopp, RJ; Townley, RG, 1994
)
0.29
"The pharmacokinetics of SDZ 64-412, an antiasthmatic agent, were investigated following intravenous, oral, and inhalation dosing in rats."( Pharmacokinetics of SDZ 64-412, a novel antiasthmatic agent, following intravenous, oral, and inhalation dosing in the rat.
Athill, LV; Charnick, SB; Karara, AH; Lau, DT; Tse, FL; Yu, Z, 1994
)
0.29
" A further 416 (57) micrograms reduction in inhaled corticosteroid dosage was possible during the treatment phase but this was almost identical in the WEB 2086 and placebo-treated groups, amounting to 353 (92) and 481 (65) micrograms/day respectively (not significant [NS])."( The effect of the orally active platelet-activating factor antagonist WEB 2086 in the treatment of asthma.
Calverley, PM; Dhillon, P; Higgins, C; Holgate, ST; Johnston, SL; Ramhamadany, E; Spence, DP; Turner, S; Winning, A; Winter, J, 1994
)
0.29
" Peak plasma and tissue concentrations were seen at 5 minutes after dosing except for the small intestine (4 hrs) and abdominal fat, stomach and large intestine (4 hrs)."( Disposition and metabolism of Ro 24-4736 in the rat.
Anastasi, EM; Chang, D; Liberato, DJ; Loh, AC; Sasso, GJ; Williams, TH, 1994
)
0.29
" dosing (1 mg/kg), the plasma concentration-time curves fitted a two-compartment model."( Pharmacokinetics of a new thienodiazepine platelet activating factor receptor antagonist (E6123) in laboratory animals. Is there a metabolic polymorphism in the rhesus monkey?
Abe, Y; Ida, S; Kusano, K; Tanaka, S; Yuzuriha, T, 1993
)
0.29
" Drugs were dosed as dry powders directly into the tracheobronchial tree and MVL was assessed by using the fluorescent macromolecule fluorescein isothiocyanate-dextran (FITC-dextran, 150 kD)."( Effects of isoenzyme-selective inhibitors of cyclic nucleotide phosphodiesterase on microvascular leak in guinea pig airways in vivo.
Karlsson, JA; Raeburn, D, 1993
)
0.29
" PAF injected into the peritoneal cavity induced a bell-shaped dose-response curve of EB extravasation in both strains of mouse."( Differential sensitivity of mouse strains to platelet activating factor-induced vasopermeability and mortality: effect of antagonists.
Jancar, S; Russo, M; Vásquez-Bravo, YL, 1993
)
0.29
" Eighty Wistar rats were divided into a sham-operated group, two control groups, and four study groups, according to the dosage and route of BN 52021 administration."( Protective effect of the PAF antagonist BN 52021 in an experimental renal warm ischemia model.
Alsina, J; Bordalba, JR; Carrera, M; Griño, JM; Martinez-Castelao, A; Moliner, R; Seron, D; Torras, J; Valles, J, 1993
)
0.29
" Experiments examining the influence of Promega dosage indicated that the AA/EPA ratio in neutrophil lipids decreased in a dose-dependent manner."( Dietary n-3 fatty acid effects on neutrophil lipid composition and mediator production. Influence of duration and dosage.
Chilton, FH; Fonteh, AN; Hubbard, WC; Patel, M; Triggiani, M, 1993
)
0.29
" Histamine was found to induce a dose-response related increase, whereas blood flow volume tended to decrease in each concentration range in the series of PAF administration."( Regional blood flow volume in the eustachian tube.
Kubo, N; Kumazawa, T; Minami, T; Tomoda, K; Yamashita, T, 1993
)
0.29
" Addition of antihistamines (mepyramine and metiamide) to the organ bath abolished the response to exogenous histamine, but failed to alter the dose-response relationship of the reaction to cumulative challenge with rising titres of anti-IgE."( Leukotrienes and histamine mediate IgE-dependent contractions of human bronchi: pharmacological evidence obtained with tissues from asthmatic and non-asthmatic subjects.
Björck, T; Dahlén, SE, 1993
)
0.29
" CsA alone induced a dose-response increase in proteoglycan synthesis and a slight decrease in cell proliferation."( Cyclosporin A (CsA) modulates the glomerular production of inflammatory mediators and proteoglycans in experimental nephrosis.
Bustos, C; Egido, J; Gómez-Guerrero, C; González, E; González-Cuadrado, S; Plaza, JJ; Ruiz-Ortega, M, 1995
)
0.29
" Selective PAF, TXA2 and 5HT antagonists (WEB 2086, sulotroban and MCI-9042) clearly inhibited both the shape change and the aggregation induced by the appropriate agonist; in each case the effect of the antagonist was to move the dose-response curve to the right."( Studies on the effects of agonists and antagonists on platelet shape change and platelet aggregation in whole blood.
Heptinstall, S; Lösche, W; Sanderson, HM; Vickers, J, 1996
)
0.29
" Dose-response relationships were analyzed by probit dose-response methods and protective ratios for each compound were computed."( The effects of EDRF/NO releasers or calcium ionophore A23187 on cyanide toxicity in mice.
Baskin, SI; Lempka, JC; Nealley, EW, 1996
)
0.29
" In order to take into account a possible tachyphylaxis, we compared PAF dose-response curves performed on one day with the curves obtained by giving the same doses separately on different days."( Acute bronchial obstruction following inhalation of PAF in asthmatic and normal subjects: comparison with methacholine.
Louis, RE; Radermecker, MF, 1996
)
0.29
" Addition of WEB 2086 to bovine platelets in vitro induced a rightward shift in the dose-response curve to PAF."( Inhibition of PAF-induced platelet aggregation by WEB 2086 'in-vitro', an antagonist to the receptor for platelet-activating factor, in bovine.
da Silva, MB; David, JL; Dessy, C; Gustin, P; Herion, F; Lekeux, P; Raskinet, R, 1996
)
0.29
" We determined both the dose-response curve and the time course of PAF-induced bronchoconstriction."( Bronchoconstriction and eosinophil recruitment in guinea pig lungs after platelet activating factor administration.
Lin, CC; Lin, CY, 1997
)
0.3
" Although lower WEB 2170 doses prevented NEC, neither fourfold higher dosing with WEB 2170 nor similar dosing with WEB 2086 affected the incidence of disease in this study."( The platelet-activating factor receptor antagonist WEB 2170 prevents neonatal necrotizing enterocolitis in rats.
Adler, L; Caplan, MS; Hedlund, E; Hsueh, W; Lickerman, M, 1997
)
0.3
"Peripheral blood taken over 12 h after dosing was used for ex vivo beta-TG release and, in the case of the 70 mg dose, measurement of plasma drug concentration."( Ex vivo inhibition of beta-thromboglobulin release following administration to man of ABT-299, a novel prodrug of a potent platelet activating factor antagonist.
Albert, DH; Carter, GW; Kleinert, HD; Magoc, TJ; Menacherry, SD; Morgan, DW; Reyes, AE; Summers, JB; Sun, E, 1997
)
0.3
"In this study we have investigated dose-response and time curves of IL-5-, IL-3-, and GM-CSF-induced tyrosine phosphorylation in eosinophils."( Cytokine-induced protein tyrosine phosphorylation is essential for cytokine priming of human eosinophils.
Kanters, D; Koenderman, L; Lammers, JW; Raaijmakers, JA; Tool, AT; van der Bruggen, T; Verhoeven, AJ, 1998
)
0.3
" In group A, the PAF antagonist CV-6209 was administered in a single dosage of 1 mg/kg by slow intravenous injection at 1 hour before crossclamping of the aorta in both donors and recipients."( A new platelet-activating factor antagonist (CV-6209) in preservation of heart and lung for transplantation.
English, JC; Feeley, EJ; Nikbakht-Sangari, M; Poostizadeh, A; Qayumi, KA, 1997
)
0.3
" Third, lower levels of HDL cholesterol are associated in a dose-response fashion with the severity and number of angiographically documented atherosclerotic coronary arteries."( The antiatherogenic role of high-density lipoprotein cholesterol.
Kwiterovich, PO, 1998
)
0.3
" Dose-response inhibition curves of [3H]PAF-specific binding were generated using increasing concentrations of several PAF-R antagonists."( PAF binding to a single receptor in corneal epithelium plasma membrane.
Bazan, HE; Hurst, J; Ma, X, 1999
)
0.3
" Glutamate treatment caused a dose-response increase of cyclic GMP levels in hippocampal slices."( Glutamate release is involved in PAF-increased cyclic GMP levels in hippocampus.
Calcerrada, MC; Catalán, RE; Martínez, AM, 1999
)
0.3
" Optimum PAF concentration had been determined in previous dose-response experiments."( Platelet-activating factor inhibits ciliary beat frequency of human bronchial epithelial cells.
Klettke, U; Luck, W; Niggemann, B; Wahn, U,
)
0.13
" However, comparison of normal subjects, atopics without dermatitis and patients with atopic dermatitis, showed the differences in dose-response effects of PAF and histamine on weal volume and flare area to be nonsignificant."( Comparison of weal and flare responses to platelet activating factor (PAF) and histamine, and the ultrastructural effects of PAF in the skin of atopic and normal subjects.
Archer, CB; Bradfield, JW; Brooks, J; Jenks, PJ; Kavanagh, GM, 1999
)
0.3
" The primary outcome measure for tolerability was the ability to complete the study on the originally assigned dosage of medication."( Randomized trial of the platelet-activating factor antagonist lexipafant in HIV-associated cognitive impairment. Neurological AIDS Research Consortium.
Epstein, LG; Kieburtz, K; Marder, K; McArthur, JC; McDermott, MP; Sacktor, N; Schifitto, G; Small, S, 1999
)
0.3
" Dose-response curves to noradrenaline-induced vasoconstriction were performed before and after continuous infusions of two different PAF-receptor antagonists (WEB 2086 and yangambin) and of the phospholipase A2 inhibitor mepacrine."( Involvement of platelet-activating factor in the modulation of vascular tone in the isolated perfused rabbit kidney.
Aimbire, F; Cailleaux, S; Cordeiro, RS; Lopes-Martins, RA; Tibiriçá, E, 1999
)
0.3
" After recovery, dose-response curves to PAF were generated by systemic infusion at 10, 30, and 100 ng."( Hemodynamic effects of platelet-activating factor in nonpregnant and pregnant sheep.
Clark, KE; Greenberg, SG, 1999
)
0.3
"1-400 nM) by using the dose-response curves of PAF on calf platelet aggregation."( In vitro inhibitory effect of SR 27417, a potent platelet-activating factor (PAF) receptor antagonist, on the PAF-induced bovine platelet aggregation.
Bastos da Silva, M; Delaunois, A; Godeau, JM; Gustin, P; Lekeux, P,
)
0.13
" In HLPs perfused with homologous blood, dose-response curves for the haemodynamic and bronchial effects of PAF (1 - 32 ng) were carried out in the absence or presence of L-NNA (200 microM)."( Nitric oxide (NO) modulation of PAF-induced cardiopulmonary action: interaction between NO synthase and cyclo-oxygenase-2 pathways.
Calabrese, R; del Basso, P; Fabi, F; Stati, T, 2001
)
0.31
" In contrast, the dose-response curve for substance P recorded 1 h after antigen challenge was not modified by pretreatment with silymarin."( Protective effect of silymarin in antigen challenge- and histamine-induced bronchoconstriction in in vivo guinea-pigs.
Apostoliti, F; Breschi, MC; Martinotti, E; Nieri, P, 2002
)
0.31
" There was a dose-response inhibition of TNF, PCA, Il-8, and PGE2 production following pretreatment with PAF-AH."( The macrophage response to endotoxin requires platelet activating factor.
Arbabi, S; Bulger, EM; Garcia, I; Maier, RV, 2002
)
0.31
" In addition, the dose-response curve for histamine-induced elevations in intracellular calcium was shifted following IL-4 stimulation."( IL-4 primes human endothelial cells for secondary responses to histamine.
Awong, G; Cuvelier, SL; Iqbal, SM; Patel, KD; Tibbles, LA; Wierzbicki, T, 2003
)
0.32
" Corresponding dose-response relationships are close to single-site binding isotherms."( Structure-activity studies with Ginkgo biloba extract constituents as receptor-gated chloride channel blockers and modulators.
Chatterjee, SS; Kondratskaya, EL; Krishtal, OA, 2003
)
0.32
"The 1, 2 or 4 nmol x L(-1) [3H]PAF specific binding to rabbit platelet receptor was inhibited by Kae dosage dependently and the IC50 were 30."( [Inhibitory effect of kaempferol against binding of platelet activating factor to its receptor].
Chen, WM; Jin, M; Li, JR; Piao, YZ; Wu, W; Zang, BX, 2004
)
0.32
" The results were used to simulate a 320-mg twice-daily dosing regimen."( A pharmacokinetic/pharmacodynamic model for a platelet activating factor antagonist based on data arising from Phase I studies.
Aarons, L; Brearley, C; Evans, L, 2005
)
0.33
" Importantly, immunogenicity may be substantially reduced by modifying the alkyl chain of the PEG-lipid conjugate, thereby allowing successful repeat dosing of the modified plasmid formulations without adverse side effects."( Hypersensitivity and loss of disease site targeting caused by antibody responses to PEGylated liposomes.
Judge, A; Maclachlan, I; McClintock, K; Phelps, JR, 2006
)
0.33
") could reverse scopolamine-induced memory retrieval deficits in mice, and displayed a typical bell-shaped dose-response relationship."( Pharmacological profile of PMS777, a new AChE inhibitor with PAF antagonistic activity.
Chen, HZ; Dong, CZ; Gao, XL; Heymans, F; Huang, H; Li, J; Massicot, F; Miezan Ezoulin, JM, 2007
)
0.34
" The 1,3,5-triazines tested inhibited the adhesion evoked by pro-inflammatory stimuli, such as platelet activating factor (PAF), FMLP, phorbol myristate acetate (PMA), tumour necrosis factor-alpha (TNF-alpha) and interleukin-1beta(IL-1beta) in a dose-response manner over the concentration range 10(-9) to 10(-4)M, compounds 5 and 6 being the most active."( Evaluation of in-vitro anti-inflammatory activity of some 2-alkyl-4,6-dimethoxy-1,3,5-triazines.
Collino, M; Dianzani, C; Fantozzi, R; Gallicchio, M; Menicagli, R; Samaritani, S; Signore, G, 2006
)
0.33
" In the dose-response study in mice, C57BL/6 mice were anesthetized and received 1 h MCAo by intraluminal suture."( LAU-0901, a novel platelet-activating factor antagonist, is highly neuroprotective in cerebral ischemia.
Alvarez-Builla, J; Atkins, K; Bazan, NG; Belayev, L; Gordon, WC; Khoutorova, L, 2008
)
0.35
" Flares were induced before dosing and up to 96 h afterwards by intradermal PAF and histamine."( Efficacy and tolerability of rupatadine at four times the recommended dose against histamine- and platelet-activating factor-induced flare responses and ex vivo platelet aggregation in healthy males.
Church, MK, 2010
)
0.36
" However, when GMA161 or its murine parent 3G8 were dosed repeatedly in transgenic mice having both human CD16 isoforms, severe reactions were observed that were not associated with significant cytokine release, nor were they alleviated by antihistamine administration."( Nonclinical evaluation of GMA161--an antihuman CD16 (FcγRIII) monoclonal antibody for treatment of autoimmune disorders in CD16 transgenic mice.
Andrews, L; Bonvini, E; Flaherty, MM; Garman, R; Johnson, S; MacLachlan, TK; Magee, T; Stein, KE; Troutt, M; Tuaillon, N, 2012
)
0.38
" Rupatadine has a rapid onset of action and a long-lasting effect, so a once-daily dosing is permitted, moreover is well tolerated by young adults and the elders."( Rupatadine for the treatment of urticaria.
Calogiuri, GF; Delle Donne, P; Di Leo, E; Ferrannini, A; Nettis, E; Vacca, A, 2013
)
0.39
" A modification of light transmission aggregometry created dose-response curves of platelet reactivity in response to multiple agonists at differing concentrations."( Altered Platelet Function in Intrauterine Growth Restriction: A Cause or a Consequence of Uteroplacental Disease?
Burke, N; Cotter, B; Cowman, J; Dempsey, M; Dicker, P; Flood, K; Geary, MP; Kearney, M; Kenny, D; Malone, FD; Müllers, SM; O'connor, H; Tully, E, 2016
)
0.43
" Other two groups were the intravenous (IV) resuscitation (group VR) with lactated Ringer's solution with the same dosage and no fluid rehydration (group NR)."( Pyruvate in oral rehydration salt improves hemodynamics, vasopermeability and survival after burns in dogs.
Bai, XD; Guo, SJ; Hu, S; Hu, XH; Li, ZY; Liu, R; Wang, SM; Zhou, FQ, 2016
)
0.43
" After dosing YinXing-TongZhi tablet, ginkgolides A and B and bilobalide exhibited significantly higher systemic exposure levels than ginkgolides C and J; after dosing ShuXueNing, ginkgolides A, B, C, and J exhibited high exposure levels."( Human pharmacokinetics of ginkgo terpene lactones and impact of carboxylation in blood on their platelet-activating factor antagonistic activity.
Du, FF; Duan, XN; Gao, Q; Huang, YH; Jia, WW; Li, C; Li, L; Li, YF; Liu, XW; Niu, W; Olaleye, OE; Wang, FQ; Wen, Q; Xu, F; Yang, JL; Zhong, CC, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
beta-adrenergic antagonistAn agent that binds to but does not activate beta-adrenergic receptors thereby blocking the actions of endogenous or exogenous beta-adrenergic agonists. beta-Adrenergic antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches and anxiety.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
bronchoconstrictor agentA drug which causes a narrowing of the lumen of a bronchus or bronchiole.
hematologic agentDrug that acts on blood and blood-forming organs and those that affect the hemostatic system.
vasodilator agentA drug used to cause dilation of the blood vessels.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
2-acetyl-1-alkyl-sn-glycero-3-phosphocholineA 2-acyl-1-alkyl-sn-glycero-3-phosphocholine where the 2-O-acyl group is specified as acetyl; a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (3)

PathwayProteinsCompounds
Ether Lipid Metabolism412
Disturbed pathways in Duchenne Muscular Dystrophy211
PAFAH1B1 copy number variation01

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency25.11890.003245.467312,589.2998AID2517
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
regulator of G-protein signaling 4Homo sapiens (human)Potency0.09470.531815.435837.6858AID504845
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency2.23871.000010.475628.1838AID1457
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Platelet-activating factor receptorHomo sapiens (human)IC50 (µMol)0.00030.00030.63183.7000AID751655
Platelet-activating factor receptorHomo sapiens (human)Ki0.00020.00020.53762.2700AID751655
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
positive regulation of cellular extravasationPlatelet-activating factor receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIPlatelet-activating factor receptorHomo sapiens (human)
chemotaxisPlatelet-activating factor receptorHomo sapiens (human)
inflammatory responsePlatelet-activating factor receptorHomo sapiens (human)
immune responsePlatelet-activating factor receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
parturitionPlatelet-activating factor receptorHomo sapiens (human)
response to symbiotic bacteriumPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of interleukin-6 productionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of tumor necrosis factor productionPlatelet-activating factor receptorHomo sapiens (human)
inositol trisphosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of neutrophil degranulationPlatelet-activating factor receptorHomo sapiens (human)
transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of translationPlatelet-activating factor receptorHomo sapiens (human)
negative regulation of blood pressurePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
cellular response to gravityPlatelet-activating factor receptorHomo sapiens (human)
cellular response to cAMPPlatelet-activating factor receptorHomo sapiens (human)
cellular response to fatty acidPlatelet-activating factor receptorHomo sapiens (human)
response to dexamethasonePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of leukocyte tethering or rollingPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of maternal process involved in parturitionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of gastro-intestinal system smooth muscle contractionPlatelet-activating factor receptorHomo sapiens (human)
cellular response to 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholinePlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide immune receptor activityPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor activityPlatelet-activating factor receptorHomo sapiens (human)
platelet activating factor receptor activityPlatelet-activating factor receptorHomo sapiens (human)
protein bindingPlatelet-activating factor receptorHomo sapiens (human)
phospholipid bindingPlatelet-activating factor receptorHomo sapiens (human)
mitogen-activated protein kinase bindingPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityPlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membranePlatelet-activating factor receptorHomo sapiens (human)
membranePlatelet-activating factor receptorHomo sapiens (human)
secretory granule membranePlatelet-activating factor receptorHomo sapiens (human)
tertiary granule membranePlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID751720Displacement of [3H]PAF from platelet activating factor receptor in human platelets at 10 uM after 3 hrs relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID751655Displacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346403Human PAF receptor (Platelet-activating factor receptor)1991The Journal of biological chemistry, Oct-25, Volume: 266, Issue:30
Molecular cloning and expression of platelet-activating factor receptor from human leukocytes.
AID1346403Human PAF receptor (Platelet-activating factor receptor)1996The Journal of biological chemistry, Sep-20, Volume: 271, Issue:38
Identification of transmembrane domain residues determinant in the structure-function relationship of the human platelet-activating factor receptor by site-directed mutagenesis.
AID1346403Human PAF receptor (Platelet-activating factor receptor)1995Journal of immunological methods, Oct-26, Volume: 186, Issue:2
A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1346403Human PAF receptor (Platelet-activating factor receptor)2001The Journal of biological chemistry, Nov-16, Volume: 276, Issue:46
Single nucleotide polymorphism of human platelet-activating factor receptor impairs G-protein activation.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,786)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902311 (26.30)18.7374
1990's4478 (50.97)18.2507
2000's1361 (15.49)29.6817
2010's522 (5.94)24.3611
2020's114 (1.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 5.32

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index5.32 (24.57)
Research Supply Index9.14 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (5.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials187 (2.04%)5.53%
Reviews965 (10.54%)6.00%
Case Studies51 (0.56%)4.05%
Observational2 (0.02%)0.25%
Other7,951 (86.84%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]