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thromboxane b2

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Description

Thromboxane B2: A stable, physiologically active compound formed in vivo from the prostaglandin endoperoxides. It is important in the platelet-release reaction (release of ADP and serotonin). [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

thromboxane B2 : A member of the class of thromboxanes B that is (5Z,13E)-thromboxa-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. [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 CID5283137
CHEMBL ID1552426
CHEBI ID28728
SCHEMBL ID38223
MeSH IDM0021439

Synonyms (33)

Synonym
(5z,13e,15s)-9alpha,11,15-trihydroxythromboxa-5,13-dien-1-oic acid
CHEBI:28728 ,
SMP1_000294
LMFA03030002
9s,11,15s-trihydroxy-thromboxa-5z,13e-dien-1-oic acid
54397-85-2
txb2
thromboxane b2
NCGC00161306-01
BML2-B07
thromboxa-5,13-dien-1-oic acid, 9,11,15-trihydroxy-, (5z,9alpha,13e,15s)-
(z)-7-[(2r,3s,4s)-4,6-dihydroxy-2-[(e,3s)-3-hydroxyoct-1-enyl]oxan-3-yl]hept-5-enoic acid
bdbm82210
pg thromboxane b2
cas_54397-85-2
CHEMBL1552426
5-heptenoic acid, 7-(tetrahydro-4,6-dihydroxy-2-(3-hydroxy-1-octenyl)-2h-pyran-3-yl)-, (2r-(2alpha(1e,3s*),3beta(z),4beta,6alpha))-
unii-v94m3r26zv
txb2 (thromboxane b2)
SCHEMBL38223
HMS3648N08
XNRNNGPBEPRNAR-JQBLCGNGSA-N
DTXSID60903947
63783-09-5
5-heptenoic acid, 7-[(2r,3s,4s)-tetrahydro-4,6-dihydroxy-2-[(1e,3s)-3-hydroxy-1-octen-1-yl]-2h-pyran-3-yl]-, (5z)-rel-
Q3009646
sr-01000946531
SR-01000946531-1
CS-0059625
HY-113331
AS-78188
5-heptenoicacid,7-[(2r,3s,4s)-tetrahydro-4,6-dihydroxy-2-[(1e,3s)-3-hydroxy-1-octen-1-yl]-2h-pyran-3-yl]-,(5z)-rel-
AKOS040758541

Research Excerpts

Overview

Thromboxane B2 (TXB2) is a stable hydrolysis product of a highly reactive, short-lived intermediate. It is formed from the prostaglandin endoperoxide (PGH2) as indicated in Fig. 2. Thromboxene B2 seems to be an important mediator in hyperacute rejection.

ExcerptReferenceRelevance
"Thromboxane B2 seems to be an important mediator in hyperacute rejection."( Allogeneic heart transplantation following xenogeneic bridging.
Babic, R; Brandl, U; Breuer, M; Engelhardt, M; Hammer, C; Kemkes, BM; Pratschke, J; Reichart, B; Schütz, A, 1992
)
1
"Thromboxane B2 (TXB2) is a stable hydrolysis product of a highly reactive, short-lived intermediate, thromboxane A2 (TXA2), which is formed from the prostaglandin endoperoxide (PGH2) as indicated in Fig."( Thromboxane molecules do not adopt the prostaglandin hairpin conformation.
DeTitta, GT; Erman, MG; Fortier, S; Langs, DA, 1979
)
0.98
"Thromboxane B2 seems to be an important mediator in hyperacute rejection.(ABSTRACT TRUNCATED AT 250 WORDS)"( Bridging to transplant: allogeneic heart transplantation after xenografting.
Babic, R; Brandl, U; Breuer, M; Engelhardt, M; Hammer, C; Kemkes, BM; Pratschke, J; Reichart, B; Saumweber, D; Schütz, A,
)
0.85

Treatment

ExcerptReferenceRelevance
"Pretreatment thromboxane B2 was elevated compared with age-matched controls, fell moderately with high-dose aspirin (60 to 100 mg/kg/day) and marginally increased with low-dose aspirin (3 to 5 mg/kg/day) 6 to 8 weeks after treatment."( Effects of current therapy of Kawasaki disease on eicosanoid metabolism.
Fulton, DR; Meissner, C; Peterson, MB, 1988
)
0.63

Toxicity

ExcerptReferenceRelevance
"Previous work has shown that cyclosporin A is toxic to the endocrine and exocrine pancreas."( Importance of endogenous prostaglandins for the toxicity of cyclosporin A to rat endocrine and exocrine pancreas?
Müller, MK; Peskar, BM; Rünzi, M; von Schönfeld, J, 1992
)
0.28
" When we administered the combination of captopril (100 mg X kg-1 X day-1) and gentamicin in potassium-depleted rats, we observed a surprising and significant adverse effect of this combination on the clearances of inulin (CIn) and PAH (CPAH) and renal blood flow (RBF)."( Captopril enhances aminoglycoside nephrotoxicity in potassium-depleted rats.
Baker, JD; Boatman, JE; Klotman, PE; Volpp, BD; Yarger, WE, 1985
)
0.27
" In this article, the toxic effect of CsA on pancreatic islet cells and the preventive effect of K-MAP on CsA-associated islet cell toxicity were investigated."( Modulation of prostaglandin metabolism by K-MAP and prevention of toxic effect of cyclosporin on pancreatic islet cells.
Babazono, T; Fuchinoue, S; Fujikawa, H; Fujita, S; Hayashi, T; Honda, H; Kawai, T; Nakagawa, Y; Nakajima, I; Teraoka, S, 1989
)
0.28
" We suggest that the vasodilating PGs attenuate the renal toxic effects induced by CSA."( The role of eicosanoids in cyclosporine nephrotoxicity in the rat.
Chen-Gal, B; Erman, A; Rosenfeld, J, 1989
)
0.28
" In contrast, urinary PGE2 excretion was not increased in CsA toxic rats."( Evidence that renal prostaglandin and thromboxane production is stimulated in chronic cyclosporine nephrotoxicity.
Carr, DR; Coffman, TM; Klotman, PE; Yarger, WE, 1987
)
0.27
"The toxic effect of cyclosporine A (CsA) on pancreatic islet beta-cells and the preventive effect of ligustrazine (LIG) on CsA-associated beta-cell toxicity in SD rats were investigated."( [Prevention of toxicity of cyclosporine A on rat pancreatic islet beta-cells by Ligustrazine].
Gu, MJ; Liu, ZM, 1993
)
0.29
"The main adverse effect of cyclosporine A (CyA) is nephrotoxicity."( Cyclosporine A nephrotoxicity: role of thromboxane and reactive oxygen species.
Arribas, I; de Arriba, G; Parra, T; Perez de Lema, G; Rodriguez-Puyol, D; Rodriguez-Puyol, M, 1998
)
0.3
"SC-58635 achieves analgesic and antiinflammatory efficacy in arthritis through selective COX-2 inhibition, without showing any evidence of 2 of the toxic effects of COX-1 inhibition associated with nonsteroidal antiinflammatory drugs."( Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor: efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects.
Geis, GS; Hubbard, RC; Isakson, PC; Lanza, FL; Lipsky, PE; Schwartz, BD; Simon, LS; Talwalker, S, 1998
)
0.3
" The better GI tolerability of meloxicam was also suggested by fewer adverse GI events and no withdrawals due to adverse events compared with piroxicam."( Endoscopic comparison of the gastroduodenal safety and the effects on arachidonic acid products between meloxicam and piroxicam in the treatment of osteoarthritis.
Chang, DM; Hsieh, TC; Hsu, CT; Kuo, SY; Young, TH, 2001
)
0.31
"We measured serum levels of soluble (s) P-selectin and thromboxane B2 (TxB2) in patients with lung cancer treated with gefitinib, and investigated the effect of low-dose aspirin on some adverse effects of gefitinib."( Aspirin reduces adverse effects of gefitinib.
Kanazawa, S; Kinoshita, Y; Komiyama, Y; Muramatsu, M; Nomura, S; Yamaguchi, K, 2006
)
0.58
"The assessment of safety in traditional toxicology protocols relies on evidence arising from observed adverse events (AEs) in animals and on establishing their correlation with different measures of drug exposure (e."( Model-based analysis of thromboxane B₂ and prostaglandin E₂ as biomarkers in the safety evaluation of naproxen.
Danhof, M; Della Pasqua, O; Sahota, T; Sanderson, I, 2014
)
0.4
"Despite the increasing importance of biomarkers as predictors of drug effects, toxicology protocols continue to rely on the experimental evidence of adverse events (AEs) as a basis for establishing the link between indicators of safety and drug exposure."( Model-based prediction of the acute and long-term safety profile of naproxen in rats.
Danhof, M; Della Pasqua, O; Sahota, T; Sanderson, I, 2015
)
0.42

Pharmacokinetics

We examined the sex-related differences in vessel wall PGI2 release and its inhibition by and recovery from aspirin in rabbits and man. We also examined the effects of aspirin on platelet aggregation, thromboxane B2 and beta-thromboglobulin (BTG) release in man, and (3) the pharmacokinetic characteristics of aspirin.

ExcerptReferenceRelevance
" Only minor differences in the pharmacokinetic parameters were observed between the younger and elderly patients."( The pharmacokinetics of flurbiprofen in younger and elderly patients with rheumatoid arthritis.
Antal, EJ; Buchanan, WW; Cauvier, H; Grace, EM; Kean, WF; Rischke, J, 1992
)
0.28
" It had an elimination half-life of 40."( Pharmacokinetics and pharmacodynamics of piroxicam in dogs.
Galbraith, EA; McKellar, QA, 1991
)
0.28
" Repeated administration showed no significant changes in half-lives, tmax values, cmax values and AUC values."( The pharmacokinetics and pharmacodynamics of a new thromboxane synthetase inhibitor, 6-(1-imidazolylmethyl)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid (DP-1904) in man after repeated oral doses.
Hakusui, H; Nii, S; Ono, K; Shibata, H; Shiozawa, T; Suzuki, T; Takegoshi, T; Tanaka, M, 1990
)
0.28
" The pharmacokinetic profile of indomethacin nanocapsule formulations was compared to a solution of free drug following oral administration of 5 mg/kg in rats; no difference in the mean concentration-time profiles of the drug was observed."( Jejunal absorption, pharmacological activity, and pharmacokinetic evaluation of indomethacin-loaded poly(d,l-lactide) and poly(isobutyl-cyanoacrylate) nanocapsules in rats.
Ammoury, N; Benita, S; Devissaguet, JP; Dubrasquet, M; Fessi, H, 1991
)
0.28
" DP-1904 concentrations declined monophasically after Cmax with half lives of 30-40 min."( The pharmacokinetics and pharmacodynamics of a new thromboxane synthetase inhibitor, 6-(1-imidazolylmethyl)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid (DP-1904), in man after single oral administration.
Nii, S; Ono, K; Shibata, H; Shiozawa, T; Suzuki, T; Takegoshi, T; Tanaka, M, 1989
)
0.28
" In normotensive subjects with normal renal function, cicletanine was rapidly and regularly absorbed, its apparent elimination half-life established around 7 h, and both its renal clearance (0."( Influence of renal insufficiency on the pharmacokinetics of cicletanine and its effects on the urinary excretion of electrolytes and prostanoids.
Benzoni, D; Cuisinaud, G; Ferry, N; Geoffroy, J; Pozet, N; Sassard, J; Zech, PY, 1988
)
0.27
" To test these possibilities we examined the sex-related differences in (1) vessel wall PGI2 release and its inhibition by and recovery from aspirin in rabbits; (2) the effects of aspirin on platelet aggregation, thromboxane B2 and beta-thromboglobulin (BTG) release in man, and (3) the pharmacokinetic characteristics of aspirin, in both rabbits and man."( The sex-related differences in aspirin pharmacokinetics in rabbits and man and its relationship to antiplatelet effects.
Buchanan, MR; Butt, R; Hirsh, J; Rischke, JA; Rosenfeld, J; Turpie, AG, 1983
)
0.45
" Both enantiomers distributed into peripheral subcutaneous tissue cage fluids, but Cmax and AUC values were lower for both transudate (non-stimulated tissue cage fluid) and exudate (induced by the intracaveal administration of the irritant carrageenan) than for plasma."( Stereospecific pharmacodynamics and pharmacokinetics of carprofen in the dog.
Delatour, P; Lees, P; McKellar, QA, 1994
)
0.29
" Pharmacokinetic parameters were determined."( Pharmacodynamics and antithrombotic effects after intravenous administration of the new thromboxane A2 receptor antagonist sodium 4-[[1-[[[(4-chlorophenyl)sulfonyl]amino]methyl]cyclopentyl] methyl]benzeneacetate.
Chavernac, G; Depin, JC; Guerrier, D; Lardy, C; Rousselot, C; Vigié, A, 1994
)
0.29
" Plasma pharmacokinetic data were fitted to either two or three compartment open models."( Correlation between the pharmacokinetics of oxindanac and inhibition of serum thromboxane B2 in calves.
King, JN, 1994
)
0.52
"There are relatively few non-steroidal anti-inflammatory drugs (NSAIDs) for which basic pharmacokinetic and toxicological data are available in the cat."( Flunixin in the cat: a pharmacodynamic, pharmacokinetic and toxicological study.
Jefferies, R; Lees, P; Taylor, PM; Winnard, JG,
)
0.13
" We tested the hypotheses that alterations in the metabolic clearance rate and the half-life of angiotensin II account for reduced pressor dose-responses during gestation and that angiotensin II increases circulating levels of vasodilatory prostaglandins I2 and E2 relative to thromboxane A2."( Angiotensin II metabolic clearance rate and pressor responses in nonpregnant and pregnant women.
Cox, K; Gant, NF; Magness, RR; Rosenfeld, CR, 1994
)
0.29
" The angiotensin II metabolic clearance rate and half-life were similar in nonpregnant and pregnant women: metabolic clearance rate = 85 +/- 10 versus 68 +/- 3 ml/min."( Angiotensin II metabolic clearance rate and pressor responses in nonpregnant and pregnant women.
Cox, K; Gant, NF; Magness, RR; Rosenfeld, CR, 1994
)
0.29
"Age and species reportedly affect the pharmacokinetic variables of nonsteroidal anti-inflammatory drugs."( Pharmacokinetics of and serum thromboxane suppression by flunixin meglumine in healthy foals during the first month of life.
Ashcraft, SM; Sams, RA; Semrad, SD, 1993
)
0.29
"A selective thromboxane (TX) synthase inhibitor, CS-518, was orally administered to healthy male Japanese volunteers and the pharmacokinetic and pharmacodynamic properties were investigated."( Pharmacokinetic and pharmacodynamic profiles of CS-518, a selective, long-lasting thromboxane synthase inhibitor, after single and multiple oral administration to healthy volunteers.
Inaba, H; Kosuge, K; Mizuno, A; Nagashima, S; Nakashima, M; Uematsu, T, 1994
)
0.29
" Population pharmacokinetic analysis with NONMEM showed plasma concentration-time profiles of AA-2414 to be best characterized by a two-compartment open model with zero-order input and first-order elimination."( Characterization of the pharmacokinetics and pharmacodynamics of a new oral thromboxane A2-receptor antagonist AA-2414 in normal subjects: population analysis.
Granneman, GR; Hussein, Z; Locke, CS; Orchard, MA; Ringham, GL; Samara, E, 1994
)
0.29
" Pharmacokinetic variables calculated for each drug when given alone and in combination were similar to those reported."( Effects of concurrent administration of phenylbutazone and flunixin meglumine on pharmacokinetic variables and in vitro generation of thromboxane B2 in mares.
Ashcraft, SM; Harris, ON; Sams, RA; Semrad, SD, 1993
)
0.49
"7 mg racemic carprofen/kg bwt, mean values for pharmacokinetic parameters were 18."( Pharmacodynamics and pharmacokinetics of carprofen in the horse.
Lees, P; Ludwig, B; May, SA; McKellar, Q, 1994
)
0.29
" Age had no significant effect on the pharmacodynamic parameter Emax, the maximum percent inhibition of TxB2 formation."( Effects of age on the pharmacodynamics of naproxen in the rat.
Boudinot, FD; Satterwhite, JH,
)
0.13
" Pharmacodynamic properties were evaluated using a model of acute inflammation, comprising subcutaneously implanted tissue cages stimulated by intracaveal injection of carrageenan."( Pharmacokinetics and pharmacodynamics of ketoprofen enantiomers in calves.
Landoni, MF; Lees, P, 1995
)
0.29
"The potential pharmacokinetic and pharmacodynamic interactions between zileuton, a 5-lipoxygenase inhibitor, and naproxen, a nonsteroidal anti-inflammatory drug that acts as a cyclo-oxygenase inhibitor, have been investigated in 24 healthy volunteers."( The pharmacokinetic and pharmacodynamic interactions between the 5-lipoxygenase inhibitor zileuton and the cyclo-oxygenase inhibitor naproxen in human volunteers.
Awni, WM; Braeckman, RA; Cavanaugh, JH; Dubé, LM; Granneman, GR; Linnen, PJ; Locke, CS, 1995
)
0.29
"The pharmacokinetic and pharmacodynamic (PK/PD) characteristics of ozagrel, a new potent and selective thromboxane synthetase inhibitor, were investigated in rabbits after its intravenous, oral, and rectal administration."( Pharmacokinetic and pharmacodynamic studies of a thromboxane synthetase inhibitor, ozagrel, in rabbits.
Adachi, I; Horikoshi, I; Kanamoto, I; Sato, H; Zheng, NX, 1995
)
0.29
" In the single-dose study (200, 300, 400 mg), the area under the plasma concentration-time curve (AUC) and the maximum plasma concentration (Cmax) increased non-linearly with dose, while the mean elimination half-life (V0) was essentially unchanged (3."( Pharmacokinetic and pharmacodynamic properties of FK070 (KDI-792), a novel thromboxane receptor antagonist/thromboxane synthetase inhibitor, after single and multiple oral administrations to healthy volunteers.
Kosuge, K; Nakano, M; Nakashima, M; Terakawa, M; Uematsu, T; Umemura, K, 1996
)
0.29
" In addition, the half-life of each enantiomer was negatively correlated with CLCR."( The influence of renal function on the enantioselective pharmacokinetics and pharmacodynamics of ketoprofen in patients with rheumatoid arthritis.
Ahern, MJ; Bochner, F; Hayball, PJ; Nation, RL; Sansom, LN; Smith, MD, 1993
)
0.29
" Tolfenamic acid pharmacokinetics were characterized by a relatively short tmax (0."( Pharmacodynamics and pharmacokinetics of tolfenamic acid in ruminating calves: evaluation in models of acute inflammation.
Foot, R; Gettinby, G; Lees, P; McKellar, QA, 1998
)
0.3
" Volume of distribution was greater for S(+) vedaprofen, whilst elimination half-life (t(1/2beta)) and mean residence time were greater for R(-) vedaprofen."( A pharmacodynamic and pharmacokinetic study with vedaprofen in an equine model of acute nonimmune inflammation.
Coert, A; Hoeijmakers, M; Lees, P; May, SA; Rens, PV, 1999
)
0.3
"Pharmacokinetic and pharmacodynamic parameters were established for the enantiomers of the 2-arylpropionic acid (APA) nonsteroidal anti-inflammatory drug (NSAID), ketoprofen (KTP)."( Enantiospecific pharmacokinetics and pharmacodynamics of ketoprofen in sheep.
Anglarilli, G; Bidal, D; Comas, W; Landoni, MF; Lees, P; Mucci, N, 1999
)
0.3
"To establish pharmacokinetic and pharmacodynamic properties of a racemic mixture and individual R(-) and S(+) enantiomeric forms of ketoprofen (KTP) in sheep and determine pharmacodynamic variables of KTP by pharmacokinetic-pharmacodynamic modeling."( Pharmacodynamics and pharmacokinetics of ketoprofen enantiomers in sheep.
Arifah, AK; Frean, SP; Landoni, MF; Lees, P, 2001
)
0.31
"Both KTP enantiomers had elimination half-life and mean residence time measurements that were short and volume of the central compartment and steady state volume of distribution that were low."( Pharmacodynamics and pharmacokinetics of ketoprofen enantiomers in sheep.
Arifah, AK; Frean, SP; Landoni, MF; Lees, P, 2001
)
0.31
" In addition, pharmacokinetic parameters of Harpagophytum extracts were investigated in vivo."( Investigations on the pharmacokinetic properties of Harpagophytum extracts and their effects on eicosanoid biosynthesis in vitro and ex vivo.
Kaszkin, M; Loew, D; Möllerfeld, J; Puttkammer, S; Schrödter, A, 2001
)
0.31
" Furthermore, in 3 independent studies with different numbers of human male volunteers, a Harpagophytum extract was administered orally and tested in whole blood samples for Cys-LT and thromboxane B2 (TXB2) biosynthesis and for the determination of pharmacokinetic parameters of harpagoside."( Investigations on the pharmacokinetic properties of Harpagophytum extracts and their effects on eicosanoid biosynthesis in vitro and ex vivo.
Kaszkin, M; Loew, D; Möllerfeld, J; Puttkammer, S; Schrödter, A, 2001
)
0.5
" Data were evaluated with a population pharmacokinetic model that integrated pharmacogenetic information."( Enantiospecific effects of cytochrome P450 2C9 amino acid variants on ibuprofen pharmacokinetics and on the inhibition of cyclooxygenases 1 and 2.
Brockmöller, J; Freytag, G; Kirchheiner, J; Meineke, I; Meisel, C; Roots, I, 2002
)
0.31
"The reduced S-ibuprofen total clearance accompanied by increased pharmacodynamic activity may have medical impact in patients receiving ibuprofen."( Enantiospecific effects of cytochrome P450 2C9 amino acid variants on ibuprofen pharmacokinetics and on the inhibition of cyclooxygenases 1 and 2.
Brockmöller, J; Freytag, G; Kirchheiner, J; Meineke, I; Meisel, C; Roots, I, 2002
)
0.31
" The usual pharmacokinetic parameters were then derived."( Pharmacokinetic and pharmacodynamic differences between two low dosages of aspirin may affect therapeutic outcomes.
Cerletti, C; de Gaetano, G; Dell'Elba, G; Di Castelnuovo, A; Feliziani, V; Manarini, S; Pecce, R; Scorpiglione, N, 2003
)
0.32
"We investigated the occurrence of pharmacodynamic interaction between low-dose aspirin and naproxen."( Pharmacodynamic interaction of naproxen with low-dose aspirin in healthy subjects.
Capone, ML; Di Gregorio, P; Grana, M; Merciaro, G; Patrignani, P; Renda, G; Ricciotti, E; Sciulli, MG; Tacconelli, S, 2005
)
0.33
" The pharmacodynamic interaction between the two drugs was then investigated in four healthy volunteers who received aspirin (100 mg daily) for 6 days and then the combination of aspirin and naproxen for further 6 days: aspirin 2 h before naproxen (500 mg, twice-daily dosing)."( Pharmacodynamic interaction of naproxen with low-dose aspirin in healthy subjects.
Capone, ML; Di Gregorio, P; Grana, M; Merciaro, G; Patrignani, P; Renda, G; Ricciotti, E; Sciulli, MG; Tacconelli, S, 2005
)
0.33
" Moreover, the rapid recovery of platelet COX-1 activity and function supports the occurrence of a pharmacodynamic interaction between naproxen and aspirin."( Pharmacodynamic interaction of naproxen with low-dose aspirin in healthy subjects.
Capone, ML; Di Gregorio, P; Grana, M; Merciaro, G; Patrignani, P; Renda, G; Ricciotti, E; Sciulli, MG; Tacconelli, S, 2005
)
0.33
" This pharmacodynamic interaction might undermine the sustained inhibition of platelet COX-1 that is necessary for aspirin's cardioprotective effects."( Pharmacodynamic interaction of naproxen with low-dose aspirin in healthy subjects.
Capone, ML; Di Gregorio, P; Grana, M; Merciaro, G; Patrignani, P; Renda, G; Ricciotti, E; Sciulli, MG; Tacconelli, S, 2005
)
0.33
" There were no significant differences between CYP2C9*1/*2 and CYP2C 9*1/*3 individuals in these pharmacokinetic parameters (P=."( Influence of CYP2C9 genotypes on the pharmacokinetics and pharmacodynamics of piroxicam.
Brogliato, AR; Perini, JA; Suarez-Kurtz, G; Vianna-Jorge, R, 2005
)
0.33
"The objectives of these analyses were to (1) develop a population pharmacokinetic/pharmacodynamic model for a novel COX-2 inhibitor (CS-706) using data from primarily Caucasian subjects, (2) predict responses in subpopulations of interest (including Japanese subjects), and (3) correlate pharmacodynamic parameters to safety outcomes."( Predictive population pharmacokinetic/pharmacodynamic model for a novel COX-2 inhibitor.
Gao, Y; Kastrissios, H; Moberly, J; Rohatagi, S; Salazar, D; Takahashi, M; Truitt, K; Wada, R; Xu, J; Yoshihara, K; Zhang, N, 2007
)
0.34
" There is, however, limited information on its pharmacokinetic and pharmacodynamic effects in vivo."( Pharmacokinetic and pharmacodynamic study of NO-donating aspirin in F344 rats.
Choi, CI; Gao, L; Joseph, S; Kopelovich, L; Patlolla, JM; Rao, CV; Rigas, B; Steele, VE, 2008
)
0.35
" Therefore, more easily accessible plasma salicylate and thromboxane B(2) concentrations were representative of the salicylate exposure and prostaglandin E(2) pharmacodynamic biomarker in the target colon, respectively."( Comparison of pharmacokinetic and pharmacodynamic profiles of aspirin following oral gavage and diet dosing in rats.
Bauer, KS; Kapetanovic, IM; Lindeblad, MO; Lubet, R; Lyubimov, A; Tessier, DM; Zakharov, AD, 2009
)
0.35
"Patients with type 2 diabetes mellitus (T2DM) have reduced aspirin-induced pharmacodynamic effects."( Pharmacodynamic effects of different aspirin dosing regimens in type 2 diabetes mellitus patients with coronary artery disease.
Angiolillo, DJ; Bass, TA; Capodanno, D; Capranzano, P; Darlington, A; Desai, B; Dharmashankar, K; Ferreiro, JL; Kodali, M; Patel, A; Seecheran, N; Tello-Montoliu, A; Tomasello, SD; Ueno, M, 2011
)
0.37
" Pharmacodynamic assessments included light-transmittance aggregometry after arachidonic acid, collagen and adenosine diphosphate stimuli; VerifyNow-Aspirin assay; and serum thromboxane B(2) (TXB(2)) levels."( Pharmacodynamic effects of different aspirin dosing regimens in type 2 diabetes mellitus patients with coronary artery disease.
Angiolillo, DJ; Bass, TA; Capodanno, D; Capranzano, P; Darlington, A; Desai, B; Dharmashankar, K; Ferreiro, JL; Kodali, M; Patel, A; Seecheran, N; Tello-Montoliu, A; Tomasello, SD; Ueno, M, 2011
)
0.37
"Aspirin dosing regimens are associated with different pharmacodynamic effects in platelets from T2DM patients and stable coronary artery disease, with a twice-daily, low-dose aspirin administration resulting in greater platelet inhibition than once-daily administration as assessed by aspirin-sensitive assays and a dose-dependent effect on serum TXB(2) levels."( Pharmacodynamic effects of different aspirin dosing regimens in type 2 diabetes mellitus patients with coronary artery disease.
Angiolillo, DJ; Bass, TA; Capodanno, D; Capranzano, P; Darlington, A; Desai, B; Dharmashankar, K; Ferreiro, JL; Kodali, M; Patel, A; Seecheran, N; Tello-Montoliu, A; Tomasello, SD; Ueno, M, 2011
)
0.37
" Results from previous feline studies showed that, despite a short half-life in blood, the effect of robenacoxib persisted for 24 h in clinical studies."( Pharmacokinetic/pharmacodynamic modelling of robenacoxib in a feline tissue cage model of inflammation.
Elliott, J; King, JN; Lees, P; Pelligand, L; Toutain, PL, 2012
)
0.38
"The absence of a pharmacokinetic interaction between the proton pump inhibitor esomeprazole (40 mg) and acetylsalicylic acid (aspirin, ASA; 325 mg) has previously been established."( Evaluation of the pharmacodynamics of acetylsalicylic acid 81 mg with or without esomeprazole 20 mg in healthy volunteers.
Andersson, T; Morrison, D; Nagy, P; Pisupati, J; Schettler, J; Warner, TD, 2012
)
0.38
"This study set out to investigate the potential for pharmacodynamic interaction between low-dose ASA and esomeprazole in healthy volunteers, by measuring ASA antiplatelet activity."( Evaluation of the pharmacodynamics of acetylsalicylic acid 81 mg with or without esomeprazole 20 mg in healthy volunteers.
Andersson, T; Morrison, D; Nagy, P; Pisupati, J; Schettler, J; Warner, TD, 2012
)
0.38
"A total of 29 volunteers (19 aged ≥50 years; 8 women; 21 men) were evaluable for pharmacodynamic analysis (per protocol)."( Evaluation of the pharmacodynamics of acetylsalicylic acid 81 mg with or without esomeprazole 20 mg in healthy volunteers.
Andersson, T; Morrison, D; Nagy, P; Pisupati, J; Schettler, J; Warner, TD, 2012
)
0.38
"No pharmacodynamic interaction between low-dose ASA and esomeprazole was found with regard to platelet function."( Evaluation of the pharmacodynamics of acetylsalicylic acid 81 mg with or without esomeprazole 20 mg in healthy volunteers.
Andersson, T; Morrison, D; Nagy, P; Pisupati, J; Schettler, J; Warner, TD, 2012
)
0.38
"A tissue cage model of inflammation in calves was used to determine the pharmacokinetic and pharmacodynamic properties of individual carprofen enantiomers, following the administration of the racemate."( Influence of oxytetracycline on carprofen pharmacodynamics and pharmacokinetics in calves.
Brentnall, C; Cheng, Z; Lees, P; McKellar, QA, 2013
)
0.39
" After administration, blood samples were collected for up to 24 hours and plasma used for pharmacokinetic analysis."( Evaluation of pharmacokinetic and pharmacodynamic properties of cimicoxib in fasted and fed horses.
Della Rocca, G; Di Salvo, A; Giorgi, M; Kim, TW; Ryschanova, R; Sgorbini, M, 2015
)
0.42
" Similar to other reports, firocoxib exhibited a long elimination half-life (31."( Pharmacokinetics and pharmacodynamics of three formulations of firocoxib in healthy horses.
Barlow, BM; Blikslager, AT; Curling, A; Davis, JL; Fogle, C; Holland, B; Schirmer, J, 2015
)
0.42
"This study aimed to investigate the pharmacodynamic effects of indobufen and low-dose aspirin in patients with coronary atherosclerosis."( Pharmacodynamic effects of indobufen compared with aspirin in patients with coronary atherosclerosis.
Abdus, S; Bai, J; Eikelboom, JW; Gong, X; Gu, Q; Li, C; Lu, Y; Mei, L; Shi, L; Tan, C; Ullah, I; Wang, G; Yang, M; Ye, Z, 2021
)
0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
" We investigated whether salicylate and aspirin interact in platelets in humans at doses and plasma levels of clinical relevance."( Plasma levels of salicylate and aspirin in healthy volunteers: relevance to drug interaction on platelet function.
Bonati, M; Cerletti, C; de Gaetano, G; Dejana, E; del Maschio, A; Galletti, F; Tognoni, G, 1984
)
0.27
" All these drugs therefore appear to interact with the same site on platelet cyclo-oxygenase."( Non-steroidal anti-inflammatory drugs react with two sites on platelet cyclo-oxygenase. Evidence from "in vivo" drug interaction studies in rats.
Cerletti, C; De Gaetano, G; Livio, M, 1982
)
0.26
" However, when FRU was combined with NIM the gain obtained (209%) appeared superior to that reached when FRU was combined with ASA (180%) or INDO (126%)."( Protective effect of furosemide combined with non-steroidal anti-inflammatory drugs administered by inhalation route on guinea-pigs anaphylaxis model.
Berti, F; Mandelli, V; Robuschi, M; Rossoni, G, 1995
)
0.29
"In a prospective randomized trial in 42 patients undergoing coronary artery bypass surgery, we analyzed the long term platelet inhibiting effects of 50 mg acetylsalicylic acid (ASA) by itself and in combination with dipyridamole (2 x 200 mg), in comparison with phenprocoumon."( [Long term effects of 50 mg acetylsalicylic acid alone and in combination with dipyridamole on platelet function after coronary bypass surgery].
Hoffmann, MW; Rauhöft, C; Terres, W, 1998
)
0.3
" Since antiaggregation treatment with acetylsalicylic acid is a complex part of obligatory therapy of these patients, the authors studied the influence of ciprofibrate on chosen lipid parameters, fibrinogen and thromboxane in monotherapy, and also in combination with acetylsalicylic acid (ASA) in patients with advanced atherosclerosis and hyperlipoproteinemia."( [The effect of monotherapy with ciprofibrate and in combination with acetylsalicylic acid on the spectrum of lipids, thromboxane and fibrinogen in patients with atherosclerosis and hyperlipoproteinemia].
Cibulova, L; Fedelesova, V; Gajdos, M; Huttova, D; Krivosikova, Z; Mongiellova, V; Polak, F, 1999
)
0.3
"These results offer a strong case for exploring the possibility that in humans MMF combined with COX-2 inhibitors has a role in the treatment options for lupus nephritis."( Mycophenolate mofetil combined with a cyclooxygenase-2 inhibitor ameliorates murine lupus nephritis.
Abbate, M; Benigni, A; Casiraghi, F; Corna, D; Noris, M; Pagnoncelli, M; Remuzzi, G; Rottoli, D; Zoja, C, 2001
)
0.31
" After immunization with ovalbumin (OVA), a common dietary constituent, we evaluated the efficacy of pretreatment with histamine-receptor or serotonin-receptor blockers administered alone or in combination with a nitric oxide synthase inhibitor (L-NAME) on OVA-induced anaphylactic shock in Brown Norway rats."( Constitutive nitric oxide synthase inhibition combined with histamine and serotonin receptor blockade improves the initial ovalbumin-induced arterial hypotension but decreases the survival time in brown norway rats anaphylactic shock.
Bellou, A; Gerard, P; Gillois, P; Guéant, JL; Lambert, H; Longrois, D; Mallié, JP; Montémont, C; Sainte-Laudy, J; Vauthier, E, 2003
)
0.32
"To explore the interactive effect of low-dosage aspirin (ASA) combined with perindopril (PER), on prostacyclin (PGI2), thromboxone A2 (TXA2), and norepinephrine (NE) in the blood of arteriosclerosis rabbit models and the cardiac function."( [Effect of aspirin combined with perindopril on prostacyclin, thromboxone A2, and norepinephrine in the blood of arteriosclerosis rabbit models and the cardiac function].
Li, J; Liu, LH; Zhuang, HP, 2003
)
0.32
"The ratio of PGI2 to TXA2 increased, and the NE levels decreased significantly; meanwhile, the heart rate decreased and the cardiac function improved during the administration of aspirin combined with perindopril in arteriosclerosis rabbit models."( [Effect of aspirin combined with perindopril on prostacyclin, thromboxone A2, and norepinephrine in the blood of arteriosclerosis rabbit models and the cardiac function].
Li, J; Liu, LH; Zhuang, HP, 2003
)
0.32
" These results demonstrate that laropiprant does not enhance in vivo platelet reactivity, either alone or in combination with niacin."( Laropiprant in combination with extended-release niacin does not alter urine 11-dehydrothromboxane B2, a marker of in vivo platelet function, in healthy, hypercholesterolemic, and diabetic subjects.
Chao, A; Cote, J; Dishy, V; Gutierrez, M; Lai, E; Larson, P; Laterza, O; Lauring, B; Luo, WL; Patterson, J; Wagner, JA, 2009
)
0.58
"To explore the effects and mechanism of electroacupuncture combined with medium frequency therapy on lumbar nerve root compression."( [Experimental study on anti-inflammatory and analgesic effects of electroacupuncture combined with medium frequency therapy in model rats with lumbar nerve root compression].
Ai, BW; Gao, JY; Zhu, F, 2011
)
0.37
"Seventy-two Sprague-Dawley (SD) rats were randomly divided into a normal group, a sham operation group, a model group, an electroacupuncture group (EA group), a medium frequency group(MF group) and an electroacupuncture combined with medium frequency group (EA + MF group), twelve rats in each group."( [Experimental study on anti-inflammatory and analgesic effects of electroacupuncture combined with medium frequency therapy in model rats with lumbar nerve root compression].
Ai, BW; Gao, JY; Zhu, F, 2011
)
0.37
"n Electroacupuncture combined with medium frequency has anti-inflammatory and analgesic effects in model rats with lumbar nerve root compression, and its mechanism may be related with the regulation of homeostasis M between TXB 2 and PGF1alpha so as to improve microcirculation."( [Experimental study on anti-inflammatory and analgesic effects of electroacupuncture combined with medium frequency therapy in model rats with lumbar nerve root compression].
Ai, BW; Gao, JY; Zhu, F, 2011
)
0.37
" The in vivo antithrombotic property of ibudilast (CAS 50847-11-5), a phosphodiesterase 4 (PDE4) inhibitor, was evaluated in a photochemically-induced guinea pig carotid artery thrombosis model in combination with low-dose ASA."( Ibudilast, a phosphodiesterase inhibitor, in combination with low-dose aspirin potently inhibits guinea pig carotid artery thrombosis without extending bleeding time and causing gastric mucosal injury.
Hoshina, K; Manita, S; Matsuzawa, S; Miyata, Y; Ooie, T; Sasahara, T; Sueyoshi, S; Yasue, T, 2012
)
0.38
"To observe the effect of Zhuang-medical thread moxibustion combined with needle-pricking on vascular oxidative stress injury in oxidative stress injury rats."( [Effects of Zhuang-medical thread moxibustion combined with needle-pricking on vascular oxidative stress injury in the rat].
Dou, XB; Li, KM; Li, XH; Lian, CR; Shu, FY; Tang, HQ; Yang, YY; Zhao, YF; Zheng, JY, 2015
)
0.42
"Zhuang-medical thread moxibustion combined with needle-pricking of ST 36, GB 34 and GB 30 can reduce the expression of femoral artery COX-2 and regulate the balance of both plasma PGI 2/TXA 2 and plasma NO/ET in CCI-induced oxidative stress rats, which may contribute to its effect in suppressing oxidative stress-induced vascular intimal hyperplasia."( [Effects of Zhuang-medical thread moxibustion combined with needle-pricking on vascular oxidative stress injury in the rat].
Dou, XB; Li, KM; Li, XH; Lian, CR; Shu, FY; Tang, HQ; Yang, YY; Zhao, YF; Zheng, JY, 2015
)
0.42
"Previous studies have found that Panax quinquefolius saponins (PQS) combined with dual antiplatelet therapy (DAPT) of aspirin and clopidogrel enhances antithrombotic effects while reducing gastric mucosal injury induced by DAPT."( Panax quinquefolius saponins combined with dual antiplatelet drug therapy alleviate gastric mucosal injury and thrombogenesis through the COX/PG pathway in a rat model of acute myocardial infarction.
Kou, N; Miao, Y; Qu, H; Shi, DZ; Wang, MM; Xue, M; Yang, B; Yang, L; Zang, MX, 2018
)
0.48
"To explore the anti-platelet aggregation and anti-thrombotic mechanisms of Trichosanthis Fructus combined with aspirin based on network pharmacology and the validation of arteriovenous by pass model in rats."( [Anti-platelet aggregation and anti-thrombotic mechanism of Trichosanthis Fructus combined with aspirin based on network pharmacology].
Bian, YY; Wang, LL; Yan, HY; Zou, CC, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
"4 microM) inhibitory activities, was found to be orally bioavailable with a long duration of action and offered effective protection against mortality in a collagen-epinephrine-induced pulmonary thromboembolism model in mice."( 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Bruno, JJ; Hirschfeld, DR; Maloney, PJ; Martinez, GR; Walker, KA; Yang, DS, 1992
)
0.28
" The rate of absorption of ASA was faster and its peak plasma concentration was higher after the ingestion of CT."( The absorption of acetylsalicylic acid from an enteric-coated formulation and the inhibition of thromboxane formation.
Anttila, M; Kahela, P; Uotila, P, 1988
)
0.27
" Bioavailability was 50% due to a pronounced first-pass effect."( Single intravenous and oral doses of fenflumizole: pharmacokinetics and effects on prostanoid formation.
Arnold, E; Midskov, C; Rasmussen, SN; Vinge, E, 1985
)
0.27
"Recent studies evaluating the effect of slow releasing enteric-coated aspirin formulations have reported contradictory findings regarding the bioavailability of the active molecule in the circulating blood and the length of duration of the inhibitory effect on platelet function."( Enteric-coated aspirin, platelet cyclooxygenase activity and function.
Johnson, GJ; Radh, E; Rao, GH; White, JG, 1984
)
0.27
"When aspirin is administered by mouth in low doses, poor systemic bioavailability may contribute to its apparent dose-related "selective inhibition" of thromboxane A2 formation."( Dose-related kinetics of aspirin. Presystemic acetylation of platelet cyclooxygenase.
FitzGerald, GA; Pedersen, AK, 1984
)
0.27
"Studies were performed in fasted rats to establish if the propensity of 4 non-steroidal anti-inflammatory (NSAI) drugs to elicit varying degrees of gastric mucosal damage following oral administration is related to their rate of absorption by the mucosal and subsequent inhibitory effects on prostaglandin (PG) production in vivo."( Comparative effects of some non-steroidal anti-inflammatory drugs on the ultrastructural integrity and prostaglandin levels in the rat gastric mucosa: relationship to drug uptake.
Fox, SA; Osborne, DJ; Rainsford, KD, 1984
)
0.27
" Decreased concentrations in non-resuscitated patients may have been a result of exhaustion of the neuroendocrine and eicosanoid systems, or may be due to differences in bioavailability at the site of blood sampling based upon differences in hemodynamics."( Concentrations of prolactin and prostaglandins during and after cardiopulmonary resuscitation.
Bothner, U; Georgieff, M; Keller, A; Lindner, IM; Lindner, KH; Strohmenger, HU, 1995
)
0.29
" Each of the enantiomers achieved similar plasma bioavailability following administration as the racemate as they did following their separate administration."( Stereospecific pharmacodynamics and pharmacokinetics of carprofen in the dog.
Delatour, P; Lees, P; McKellar, QA, 1994
)
0.29
" Bioavailability was incomplete (F = 66."( High performance liquid chromatography and pharmacokinetics of the non-steroidal anti-inflammatory drug oxindanac in calves.
Hauffe, SA; King, JN; Le Goff, C; Mauron, C; Voirol, MJ, 1994
)
0.29
" Absolute bioavailability of the parent compound was 50%."( A prodrug of a 2,6-disubstituted 4-(2-arylethenyl)phenol is a selective and orally active 5-lipoxygenase inhibitor.
Farina, PR; Graham, AG; Gundel, RH; Hattox, SE; Homon, CA; Lazer, ES; Riska, PS; Wegner, CD, 1993
)
0.29
" Plateau concentrations of phenylbutazone in plasma were obtained between 2 and 12 h and mean bioavailability was 97%, although this was subject to wide inter-animal differences."( Phenylbutazone pharmacokinetics and bioavailability in the dromedary camel (Camelus dromedarius).
al Hadrami, G; Ali, BH; Bashir, AK; Kadir, A; Landoni, MF; Lees, P, 1997
)
0.3
" dosing, and the bioavailability after oral dosing was approximately 70%."( Pharmacokinetic-pharmacodynamic modelling of DP-1904, a novel thromboxane synthetase inhibitor in rabbits, based on an indirect response model.
Adachi, I; Horikoshi, I; Sato, H; Zheng, NX,
)
0.13
"4 mg/kg and its disposition and bioavailability and the disposition of its active metabolite, oxyphenbutazone, in plasma were investigated."( Pharmacokinetic and pharmacodynamic studies on phenylbutazone and oxyphenbutazone in goats.
Cheng, Z; McKellar, QA; Nolan, A; Welsh, E, 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 bioavailability of cutaneous aspirin was 4%-8% that of oral aspirin."( Effects of cutaneous aspirin on the human stomach and duodenum.
Cryer, B; Feldman, M; Kliewer, D; McAllister, L; Sie, H,
)
0.13
"We investigated whether use of low-dose enteric-coated (EC) aspirin for secondary prevention of cardiovascular events has sufficient bioavailability to achieve complete platelet cyclooxygenase (COX) inhibition in all individuals."( Platelet response to low-dose enteric-coated aspirin in patients with stable cardiovascular disease.
Conroy, RM; Cox, D; Crean, P; Curtin, RJ; Dooley, M; Fitzgerald, DJ; Maree, AO, 2005
)
0.33
" Lower bioavailability of these preparations and poor absorption from the higher pH environment of the small intestine may result in inadequate platelet inhibition, particularly in heavier subjects."( Effect of enteric coating on antiplatelet activity of low-dose aspirin in healthy volunteers.
Byrne, MF; Conroy, R; Cox, D; Dooley, M; Fitzgerald, DJ; Maree, AO, 2006
)
0.33
" Our study was aimed at investigating the role of enhanced AA bioavailability modulating the hepatic vascular tone of cirrhotic livers and identifying which prostanoid is involved."( Enhanced vasoconstrictor prostanoid production by sinusoidal endothelial cells increases portal perfusion pressure in cirrhotic rat livers.
Bosch, J; García-Calderó, H; García-Pagán, JC; Gracia-Sancho, J; Laviña, B; Rodríguez-Vilarrupla, A, 2007
)
0.34
" Basal nitric oxide (NO) bioavailability in the aorta was determined from the contractile response induced by the NO synthase inhibitor N(G)-nitro-L-arginine methyl ester (L-NAME, 10(-4) mol/L)."( Ferulic acid restores endothelium-dependent vasodilation in aortas of spontaneously hypertensive rats.
Fujii, A; Hase, T; Jokura, H; Saito, I; Suzuki, A; Tokimitsu, I; Yamamoto, M, 2007
)
0.34
"Ferulic acid restores endothelial function through enhancing the bioavailability of basal and stimulated NO in SHR aortas."( Ferulic acid restores endothelium-dependent vasodilation in aortas of spontaneously hypertensive rats.
Fujii, A; Hase, T; Jokura, H; Saito, I; Suzuki, A; Tokimitsu, I; Yamamoto, M, 2007
)
0.34
" These include patients with poor bioavailability or noncompliance, an impaired platelet response to ASA in vitro and an increased, TX-independent hyperreactivity to collagen."( Variable platelet response to aspirin in patients with ischemic stroke.
Boucher, M; Hohlfeld, T; Junghans, U; Schrör, K; Schumacher, M; Siebler, M; Weber, AA, 2007
)
0.34
"Systemic bioavailability and pharmacodynamics of topical diclofenac sodium gel 1% were compared with those of oral diclofenac sodium 50-mg tablets."( Systemic bioavailability of topical diclofenac sodium gel 1% versus oral diclofenac sodium in healthy volunteers.
Gold, M; Kienzler, JL; Nollevaux, F, 2010
)
0.36
" In this study, we investigated the effects of iloprost infusion on urinary 11-dehydro-TXB₂ and 8-iso-PGF(₂α) excretion rate, as in vivo indexes of thromboxane-dependent platelet activation and lipid peroxidation, respectively, and on platelet-derived proinflammatory sCD40L and nitric oxide bioavailability in 44 patients with CLI while on chronic treatment with low-dose aspirin."( Inflammation, oxidative stress and platelet activation in aspirin-treated critical limb ischaemia: beneficial effects of iloprost.
Cuccurullo, C; Davì, G; Di Iorio, P; Di Michele, D; Di Ruscio, P; Ferrante, E; Lattanzio, S; Laurora, G; Lessiani, G; Liani, R; Sgrò, G; Simeone, E; Vazzana, N, 2011
)
0.37
" Nitric oxide (NO) bioavailability and eNOS activation were measured in hepatic endothelial cells (HEC) isolated from cirrhotic rat livers."( PPARα activation improves endothelial dysfunction and reduces fibrosis and portal pressure in cirrhotic rats.
Bosch, J; García-Calderó, H; García-Pagán, JC; Laviña, B; Rodríguez-Vilarrupla, A; Roglans, N; Rosado, E; Russo, L, 2012
)
0.38
" Moreover, a reduction in COX-1 expression and TXB(2) production in rats receiving fenofibrate and a significant increase in NO bioavailability in HEC with fenofibrate were observed."( PPARα activation improves endothelial dysfunction and reduces fibrosis and portal pressure in cirrhotic rats.
Bosch, J; García-Calderó, H; García-Pagán, JC; Laviña, B; Rodríguez-Vilarrupla, A; Roglans, N; Rosado, E; Russo, L, 2012
)
0.38
" A nonlinear relationship between dose and bioavailability was observed which leads to a less than proportional increase in naproxen concentrations with increasing doses."( Model-based analysis of thromboxane B₂ and prostaglandin E₂ as biomarkers in the safety evaluation of naproxen.
Danhof, M; Della Pasqua, O; Sahota, T; Sanderson, I, 2014
)
0.4
" Bioavailability was 112% and 88% for the paste and tablet, respectively."( Pharmacokinetics and pharmacodynamics of three formulations of firocoxib in healthy horses.
Barlow, BM; Blikslager, AT; Curling, A; Davis, JL; Fogle, C; Holland, B; Schirmer, J, 2015
)
0.42
" While an aspirin prodrug exhibited comparable oral bioavailability and antiplatelet activity (i."( Gastric-sparing nitric oxide-releasable 'true' prodrugs of aspirin and naproxen.
Borhade, N; Burhan, A; Desai, DC; Dhiman, M; Gaikwad, P; Gund, M; Nemmani, KVS; Patil, M; Satyam, A; Sharma, A; Sharma, S; Sheikh, J; Thakre, G; Tipparam, SG, 2014
)
0.4
" We quantified inflammation, fibrosis, oxidative stress, nitric oxide (NO) bioavailability and thromboxane B2 levels."( Contribution of Cyclooxygenase End Products and Oxidative Stress to Intrahepatic Endothelial Dysfunction in Early Non-Alcoholic Fatty Liver Disease.
Abrante, B; Diaz-Flores, F; Gonzalez-Paredes, FJ; Hernández Mesa, G; Hernández-Guerra, M; Marcelino Reyes, R; Morales Arraez, D; Quintero, E; Salido, E, 2016
)
0.65
"Our study provides evidence that endothelial dysfunction at an early stage of NAFLD is associated with reduced NO bioavailability together with increased cyclooxygenase end products and oxidative stress, which suggests that both pathways are involved in the pathophysiology and may be worth exploring as therapeutic targets to prevent progression of the disease."( Contribution of Cyclooxygenase End Products and Oxidative Stress to Intrahepatic Endothelial Dysfunction in Early Non-Alcoholic Fatty Liver Disease.
Abrante, B; Diaz-Flores, F; Gonzalez-Paredes, FJ; Hernández Mesa, G; Hernández-Guerra, M; Marcelino Reyes, R; Morales Arraez, D; Quintero, E; Salido, E, 2016
)
0.43

Dosage Studied

Serum thromboxane B2 and aggregation studies in whole blood and platelet-rich plasma were measured before dosing and at 1, 4, 6, 8, and 24 h after dosing. Different dosages of aspirin were administered (by nasogastric tube) to 3 groups of 5 healthy adult horses. Perindopril alone tended to reduce serum and urinary thromboxesine B2 (TxB2) and to raise urinary 6-ketoPGF1 alpha and PGE2.

ExcerptRelevanceReference
" Lowering the antigen (ovalbumin) dosage from 400 microgram/ml to 10 microgram/ml reduced the control release of SRS-A by 70% and increased the inhibitory effect of prostaglandins I2, E1 and isoprenaline."( A possible modulatory role for prostacyclin (PGI2) INIgGa-induced release of slow-reacting substance of anaphylaxis in rats.
Burka, JF; Garland, LG, 1977
)
0.26
" The dose-response curves for NKA and SP were shifted to the left (three orders and one order of magnitude, respectively) in AMs isolated from sensitized animals, with no variation in maximal effects."( Enhanced responsiveness of ovalbumin-sensitized guinea-pig alveolar macrophages to tachykinins.
Brunelleschi, S; Ceni, E; Fantozzi, R; Giotti, A; Parenti, A, 1992
)
0.28
" 7e, 9e, 13a, 13d, 18, 20, 21, and 23, when dosed orally in conscious spontaneously hypertensive rats."( 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Bruno, JJ; Hirschfeld, DR; Maloney, PJ; Martinez, GR; Walker, KA; Yang, DS, 1992
)
0.28
" Perindopril alone tended to reduce serum and urinary thromboxane B2 (TxB2) and to raise urinary 6-ketoPGF1 alpha and PGE2 and inhibited serum ACE activity 24 h post dosing by about 85%."( Hemodynamic and humoral interactions between perindopril and indomethacin in essential hypertensive subjects.
Abdel-Haq, B; Favilla, S; Magagna, A; Salvetti, A, 1991
)
0.53
" Dose-response curves for platelet aggregation to collagen were obtained in the presence and absence of 1 nmol/L PGI2 to quantify the antiaggregation effects of PGI2."( Inhibition of platelet aggregation by prostacyclin is attenuated after exercise in patients with angina pectoris.
Ashikaga, T; Kishi, Y; Numano, F, 1992
)
0.28
"The pharmacokinetics of flurbiprofen (Ansaid Tablets, Upjohn Company of Canada, Don Mills, Ontario) were evaluated in both younger (40 to 60 years) and elderly (65 to 83 years) rheumatoid arthritic patients after both a 100-mg single-dose administration and at steady state during a 100-mg twice-a-day dosage regimen."( The pharmacokinetics of flurbiprofen in younger and elderly patients with rheumatoid arthritis.
Antal, EJ; Buchanan, WW; Cauvier, H; Grace, EM; Kean, WF; Rischke, J, 1992
)
0.28
" Linear regression analysis of the average for each dose from three different placentas was used to determine the dose-response relationship."( Dose-related action of gonadotropin-releasing hormone on basal prostanoid production from the human term placenta.
Forman, J; Kang, IS; Koong, MK; Siler-Khodr, TM, 1991
)
0.28
" PG and PS-liposomes, both of which were negatively charged, showed different dose-response curves, the two different types of neutral liposomes showed different responses, and PC-liposomes produced a small increase in pulmonary arterial pressure."( [Effects of differently composed liposomes on pulmonary arterial pressure in sheep--involvement of pulmonary intravascular macrophages].
Aida, A; Aoi, K; Kawakami, Y; Miyamoto, K; Nakano, T, 1991
)
0.28
"Infarct healing delay by prednisolone is dosage dependent, and smaller infarcts may be more sensitive to its effect."( Effect of prednisolone on myocardial infarct healing: characteristics and comparison with indomethacin.
Iimura, O; Ishimoto, R; Itoya, M; Miura, T; Shizukuda, Y, 1991
)
0.28
" Infusing endotoxin at a higher dosage (40 ng."( Imbalance between plasma levels of thromboxane B2 and 6-keto-prostaglandin F1 alpha during subacute endotoxin-induced hyperdynamic sepsis or multiple organ failure syndrome in sheep.
Morel, DR; Pittet, JF, 1991
)
0.56
"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
" Dosage of PGI2 was 2-5 ng/kg/min intravenous drip."( [Treatment of acute cerebral infarction with PGI2--evaluating the clinical effect and observation of dynamic changes in plasma TXB2 and 6-keto PGF1 alpha levels].
Zhao, J, 1991
)
0.28
"The effects of oral dosing with paracetamol (40 mg/kg/day for 3 days) on serum thromboxane B2 (TXB2), glomerular filtration rate (GFR), sodium homeostasis, urinary excretion of prostaglandin E2 (PGE2) and on some other renal function parameters were investigated in 10 healthy young controls aged 23-26 years, 9 healthy elderly persons with normal renal function aged 66-78 years and 9 patients with chronic stable impaired renal function."( Acute effects of paracetamol on prostaglandin synthesis and renal function in normal man and in patients with renal failure.
Berg, KJ; Djøseland, O; Gjellan, A; Hundal, O; Knudsen, ER; Rugstad, HE; Rønneberg, E, 1990
)
0.51
" 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
" We studied 34 hypertensive patients, whose blood pressure levels were controlled by Enalapril at a mean dosage of 12."( [The role of prostacyclin and thromboxane in the antihypertensive action of enalapril].
Castillo Ferrando, JR; Garrido Peralta, M; Oliván Martínez, J; Serrano Molina, J; Suárez Morano, J, 1990
)
0.28
" Platelet function and urinary prostaglandin production were assessed immediately before and on the seventh day of dosing in both studies and in the second study, repeated on the tenth day of dosing."( Selective inhibition of platelet cyclooxygenase with controlled release, low-dose aspirin.
McLeod, LJ; Roberts, MS; Seville, PR; Vial, JH, 1990
)
0.28
" The inhibitory effect of cilostazol on platelet aggregation was potentiated by the presence of endothelial cells, and the slope of the dose-response curves were identified to be as the same between both experiments in the presence and the absence of endothelial cells."( Potentiation of anti-platelet aggregating activity of cilostazol with vascular endothelial cells.
Chijiwa, T; Igawa, T; Kato, S; Kawamura, K; Kimura, Y; Shimidzu, S; Shiragiku, T; Tani, T; Unemi, F, 1990
)
0.28
" It showed that a larger dosage of CP, which could inhibited the synthesis of both TXA2 and PGI2, its mechanism of action needs further study."( [Effects of Codonopsis pilosulae on the synthesis of thromboxane A2 and prostacyclin].
Wang, S; Zhu, G, 1990
)
0.28
"A specific thromboxane synthetase inhibitor, 3-methyl-2 (3-pyridyl)-1-indoleoctanoic acid (CGS 12970) was administered orally to 6 healthy adult Beagles at a dosage of 30 mg/kg of body weight."( Effects of a specific thromboxane synthetase inhibitor on thromboxane generation and excretion in healthy dogs.
Culham, CA; Grauer, GF; Johnson, HC; Longhofer, SL; Schultz, KT, 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
" To assess their antiplatelet properties in vivo and to compare time and dosage requirements, we infused both IS-2-MN and IS-5-MN for 30 minutes, on 2 separate days, into nine patients with stable coronary artery disease, at rates of 4 mg/hr (n = 4) and 8 mg/hr (n = 5)."( Inhibition of platelet function during in vivo infusion of isosorbide mononitrates: relationship between plasma drug concentration and hemodynamic effects.
Bernini, W; De Caterina, R; Giannessi, D; Lazzerini, G; Lombardi, M; Mazzone, A; Moscarelli, E; Weiss, M, 1990
)
0.28
" After oral dosing in beagle dogs, 1 persistently inhibited TX production, although the elimination of the drug was relatively rapid from plasma."( Correlation between pharmacokinetics and pharmacologic effects of a new imidazole thromboxane synthetase inhibitor.
Iwata, T; Mikashima, H; Takamatsu, R, 1990
)
0.28
" With immunological activation of passively sensitized cells, histamine and PGD2 release had similar dose-response characteristics, but TXB2, LTC4, LTD4, and LTE4 release differed in reaching maximum at 50 micrograms/ml and declining at 125 micrograms/ml anti-human IgE."( The immunoglobulin E- and calcium-dependent release of histamine and eicosanoids from human dispersed mastocytosis spleen cells.
Agius, RM; Benyon, RC; Holgate, ST; Jones, DB; Robinson, C; Wright, DH, 1988
)
0.27
" Garlic extracts (MEE and material extracted in chloroform, MEC) at higher dosage inhibited the degradation of platelet phospholipids and reduced the formation of thromboxane (TxB2) and lipoxygenase-derived products from labelled platelets."( Isolation and effects of some garlic components on platelet aggregation and metabolism of arachidonic acid in human blood platelets.
Justesen, U; Srivastava, KC, 1989
)
0.28
"The effects on platelet function of a four-week administration of aspirin at a low dosage (100 mg daily) were compared in two groups, 14 healthy young volunteers and 14 patients with coronary heart disease."( [Effects of low-dose acetylsalicylic acid on thrombocytes in health subjects and in patients with coronary heart disease].
Bleifeld, W; Kupper, W; Schuster, O; Terres, W, 1989
)
0.28
" Thus, felodipine in modest therapeutic dosage decreases the plasma levels of B-TG and PF-4, indicating an inhibitory effect on platelet on release."( Effect of felodipine, a new calcium channel antagonist, on platelet function and fibrinolytic activity at rest and after exercise.
Sengeløv, H; Winther, K, 1989
)
0.28
" At concentrations lacking agonist activity U-75302 was an effective antagonist, displacing the LTB4 dose-response curve."( Receptor antagonism of leukotriene B4 myotropic activity by the 2,6 disubstituted pyridine analog U-75302: characterization on lung parenchyma strips.
Fitzpatrick, FA; Lawson, CF; Morris, J; Wishka, DG,
)
0.13
" Captopril when dosed to lower diastolic blood pressure 5-7 mm Hg did not significantly affect GFR, RPF or RVR."( Preliminary observations of the acute effects of selective serum thromboxane inhibition and angiotensin converting enzyme inhibition on blood pressure and renal hemodynamics in hypertensive humans.
Douglas, FL; Hoover, N; Klassen, DK; Weir, MR, 1989
)
0.28
"In a pilot study, 26 rheumatoid arthritic patients taking continuous, stable dosage regimens of nonsteroidal anti-inflammatory drugs and with developed gastric and duodenal lesions were administered sucralfate 1 g four times per day (14 patients) or cimetidine 400 mg twice daily (12 patients) in a single-blind regimen for six weeks."( Effect of sucralfate and cimetidine on rheumatoid patients with active gastroduodenal lesions who are taking nonsteroidal anti-inflammatory drugs. A pilot study.
Cox, N; Fine, D; Hillier, K; Jewell, R; Shepherd, HA, 1989
)
0.28
"10 micrograms/ml from 24 hours after drug administration at all dosage levels."( Flunixin pharmacokinetics and serum thromboxane inhibition in the dog.
Bogan, JA; Galbraith, EA; Hooke, RE; Lees, P; McKellar, QA; Russell, CS, 1989
)
0.28
" In aortic thrombus formation in rabbits, the platelet 5-HT release reaction and platelet destruction could be reduced by the compound, meanwhile aortic thrombosis was inhibited with a clear correlation between drug dosage and its efficacy."( [Inhibitory effects of new-breviscapine on thrombosis in vivo].
Wang, ZY, 1989
)
0.28
" Second, the dose-response curve for thromboxane A2, based on the amount of thromboxane B2 generated by lung strips contracted with leukotriene B4, was inconsistent with dose-response curves for lung strips contracted with a stable thromboxane A2 mimetic, U-46619 or with synthetic thromboxane A2 itself."( Myotropic activity of leukotriene B4 on lung parenchyma strips is not necessarily attributable to thromboxane A2 release.
Fitzpatrick, FA; Lawson, CF, 1988
)
0.5
" LTB4 alone caused an increase in serum thromboxane B2 (TxB2) from 130 +/- 35 to 320 +/- 17 pg/ml 3 minutes after dosing but did not increase TxB2 following pre-treatment with meclofenamate."( Meclofenamate blocks the pulmonary arterial vasopressor effects of leukotriene B4 in awake sheep.
Lefferts, PL; Miller, RF; Purvis, AW; Snapper, JR, 1988
)
0.54
" We investigated whether the maximal response plateau or the position of the dose-response curve is due to functional inhibition by neurogenic mechanisms or to prostaglandin release."( Limited maximal airway narrowing in nonasthmatic subjects. Role of neural control and prostaglandin release.
Daniel, EE; Hargreave, FE; Sterk, PJ; Zamel, N, 1985
)
0.27
" Etersalate inhibited at the lower dosage platelet function and decreased TXA2 levels, but PGI2 generation from rat aortic rings was stimulated when incubated with plasma from etersalate-treated donors."( Effect of etersalate on human platelet responsiveness. A study in healthy volunteers.
Armijo, M; Ortega, MP; Priego, JG; Sunkel, C, 1987
)
0.27
" During long-term dosing with the synthetic inhibitor, inhibition of thromboxane biosynthesis was incomplete, which would permit continued thromboxane-dependent platelet aggregation to occur."( Increased thromboxane biosynthesis in a human preparation of platelet activation: biochemical and functional consequences of selective inhibition of thromboxane synthase.
Doran, JB; FitzGerald, GA; Reilly, IA; Smith, B, 1986
)
0.27
" When the results should confirm themselves in long-term studies, a mackerel diet in practicable dosage can be recommended as non-medicamentous treatment of moderate hypertension."( [Changes in blood pressure and serum lipids with fish diets in patients with mild essential hypertension].
Gödicke, W; Hartrodt, W; Mest, HJ; Naumann, E; Richter-Heinrich, E; Singer, P; Taube, C; Voigt, S; Wirth, M, 1986
)
0.27
" The dose-response curves of NA were shifted to the right."( Vasoconstriction induced by noradrenaline and angiotensin II is antagonized by eicosapentaenoic acid independent of formation of trienoic eicosanoids.
Juan, H; Sametz, W, 1986
)
0.27
"OH) radical was observed to affect cyclooxygenase metabolism in a dose-response manner."( Gender-related variations and interaction of human neutrophil cyclooxygenase and oxidative burst metabolites.
Bellanti, JA; Mallery, SR; Ramwell, PW; Zeligs, BJ, 1986
)
0.27
" Short-term administration of sulindac at the recommended dosage is relatively safe in patients with chronic glomerular disease because of selective sparing of glomerular cyclo-oxygenase activity."( Renal effects of nonsteroidal anti-inflammatory drugs in chronic glomerular disease.
Patrono, C; Pierucci, A, 1986
)
0.27
" We conclude that long-term dosing with 27 mg ECA three times daily results in profound inhibition of platelet TXA2 production, and diminished in vitro and in vivo platelet reactivity."( Low-dose enteric-coated aspirin: a practical approach to continuous-release low-dose aspirin and presystemic acetylation of human platelet cyclooxygenase.
Deykin, D; Faigel, D; Jakubowski, JA; Stampfer, MJ; Vaillancourt, R, 1986
)
0.27
" Thus, these experiments suggest that thromboxane synthetase inhibition, within a narrow dosage range, potentiates furosemide-induced renin release while cyclooxygenase inhibition suppresses it."( Effect of cyclooxygenase and thromboxane synthetase inhibition on furosemide-stimulated plasma renin activity.
Datar, S; McCauley, FA; Wilson, TW, 1987
)
0.27
" However, twice daily dosing with dazoxiben was effective."( Prolongation of platelet survival in hypercholesterolaemic rabbits by CGS 12970 (3-methyl-2-(3-pyridyl)-1 indoleoctanoic acid) and dazoxiben.
Ambler, J; Butler, KD; Butler, PA; Shand, RA; Wallis, RB, 1987
)
0.27
"5 hr to 8 hr after dosing was more than 90%, and was 70-80% at 24 hr."( RS-5186, a novel thromboxane synthetase inhibitor with a potent and extended duration of action.
Asai, F; Ito, T; Matsuda, K; Oshima, T; Terada, A; Ushiyama, S; Yamazaki, M, 1988
)
0.27
" The importance of the findings for the clinical efficacy of this dosage schedule is considered."( Effects of a phenylbutazone paste in ponies: model of acute nonimmune inflammation.
Higgins, AJ; Lees, P, 1986
)
0.27
" At the end of each dosing interval we measured platelet aggregation and thromboxane formation in response to four aggregating agents and to whole blood coagulation."( A dose-ranging study of the antiplatelet effect of enteric coated aspirin in man.
Bochner, F; Duncan, EM; Herd, CM; Lloyd, JV; Rodgers, SE; Tunbridge, LJ, 1987
)
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
" One-step extraction of UTXB2 with an octadecylsilyl-silica column was sufficient as pretreatment for TXB2 radioimmunoassay because recovery of UTXB2 was good, the eluate was parallel with the dose-response curve, and the value coincided with that obtained by the conventional method."( Increased thromboxane B2 excretion in diabetes mellitus.
Inaba, M; Ishii, J; Katayama, S; Kawazu, S; Maruno, Y; Omoto, A, 1987
)
0.68
" 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
" In addition to these present results, AR 12463 reduced significantly the mean arterial blood pressure of spontaneously hypertensive rats (at a dosage of 20 mg/kg/d administered orally for 2 weeks) in contrast to the same dosage of trapidil."( [The effect of trapidil and the trapidil derivative AR 12463 on blood pressure and thromboxane formation in spontaneously hypertensive rats].
Mest, HJ; Steinborn, C; Taube, C, 1987
)
0.27
" Meanwhile by radioimmunoassay we dosed thromboxane B2, a stable product of thromboxane A2, released by platelets during activation, in 7 healthy subjects and 25 hyperlipemic subjects."( [Platelet aggregation in whole blood and thromboxane B2 in type II and IV hyperlipidemia].
Barbesti, S; Braconaro, F; Citella, C; Colombo, L; Craveri, A; Lanfredini, M; Marzocchi, B, 1987
)
0.81
"Different dosages of aspirin were administered (by nasogastric tube) to 3 groups of 5 healthy adult horses to determine the minimal effective dosage needed to decrease serum thromboxane B2 (TxB2) concentrations and to determine the duration of this decrease."( Effect of aspirin on ex vivo generation of thromboxane in healthy horses.
Baxter, GM; Moore, JN, 1987
)
0.47
" Blood samples were drawn 0, 2, 4, and 6 hours and 7 days after dosing for determination in serum (from untreated or in vitro indomethacin-treated portions of the blood) of TxA2 and PGI2 by radioimmunoassay of their stable metabolites (TxB2 and 6-keto-PGF1 alpha)."( Kinetics of ibuprofen effect on platelet and endothelial prostanoid release.
Beyers, BJ; Bowen, RJ; Longenecker, GL; Shah, AK; Swift, IA, 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
" Dose-response curves performed with thrombin and collagen revealed that increased stimulation resulted in higher ratios of 12-HETE/HHT."( Differential effect of external calcium on the oxygenated metabolism of endogenous and exogenous arachidonic acid in platelets.
Lagarde, M; Velardo, B, 1985
)
0.27
" Within the dosage range studied, linear pharmacokinetics were achieved."( Flunixin meglumine given in small doses: pharmacokinetics and prostaglandin inhibition in healthy horses.
Hardee, GE; Hardee, MM; Moore, JN; Semrad, SD, 1985
)
0.27
" Inhibition of LTB4-formation and cell migration by BW755C was dose-related, but the two dose-response curves were not parallel."( The effects of BW755C and other anti-inflammatory drugs on eicosanoid concentrations and leukocyte accumulation in experimentally-induced acute inflammation.
Moncada, S; Salmon, JA; Simmons, PM, 1983
)
0.27
" The daily dosage ceiling was increased to 10 mg."( Some biochemical correlates of panic attacks with agoraphobia and their response to a new treatment.
Coleman, JH; Greenblatt, DJ; Jones, KJ; Levine, PH; Orsulak, PJ; Peterson, M; Schildkraut, JJ; Sheehan, DV; Uzogara, E; Watkins, D, 1984
)
0.27
" Inhibition of aggregation by the beta-adrenoceptor antagonists was manifested as a parallel shift to the right in the dose-response curve."( Beta-adrenoceptor antagonists and human platelets: relationship of effects to lipid solubility.
Kerry, R; Scrutton, MC; Wallis, RB, 1984
)
0.27
" The relationship to dosage and possible mechanisms for this effect are discussed."( Nifedipine reduces arrhythmias but does not alter prostanoid release during coronary artery occlusion and reperfusion in anaesthetised greyhounds.
Coker, SJ; Parratt, JR,
)
0.13
" Treatment of 20:4 with soybean lipoxygenase did not abolish its capacity to induce O2- production; native and lipoxygenase-treated 20:4 exhibited similar dose-response ratios."( Unsaturated fatty acids as second messengers of superoxide generation by macrophages.
Bromberg, Y; Pick, E, 1983
)
0.27
" Serum thromboxane B2 and aggregation studies in whole blood and platelet-rich plasma were measured before dosing and at 1, 4, 6, 8, and 24 h after dosing."( Endogenous prostacyclin biosynthesis and platelet function during selective inhibition of thromboxane synthase in man.
Brash, AR; FitzGerald, GA; Oates, JA; Pedersen, AK, 1983
)
0.72
" The optimal optimal dosage in influencing vascular haemostatic regulation is still an open question in the literature."( [Venous prostacycline synthesis and plasma thromboxane B2 after low-dose aspirin].
Cromwell, M; Kaliman, J; Sinzinger, H, 1983
)
0.53
") failed to elicit mucosal damage either ultrastructurally or even visually up to 23 h after dosing and did not affect the content of PG's even though the drug was present in the mucosa in sufficient concentration to elicit reduction in prostaglandin synthesis in vitro."( Comparative effects of some non-steroidal anti-inflammatory drugs on the ultrastructural integrity and prostaglandin levels in the rat gastric mucosa: relationship to drug uptake.
Fox, SA; Osborne, DJ; Rainsford, KD, 1984
)
0.27
"001) in the dose-response relationship to submaximal concentrations of vasopressin (0."( Thromboxane and stable prostaglandin endoperoxide analogs stimulate water permeability in the toad urinary bladder.
Burch, RM; Halushka, PV, 1980
)
0.26
" Meclofenamate (10(-7)M) pretreatment of strips subjected to dose-response studies using PGF2 alpha, PGE2, bradykinin (B K) and angiotensin II (AII) revealed a significant reduction in tension developed to both BK and AII."( The actions of prostaglandins and cyclo-oxygenase inhibition on the resistance vessels supplying the human fetal placenta.
Tulenko, TN, 1981
)
0.26
" Platelet accumulation on the injured tissue was further reduced by increasing the dosage to 30 mg/kg."( The reduction of platelet thrombi on damaged vessel wall by a thromboxane synthetase inhibitor in rabbits.
Chen, YC; Hall, ER; Ho, T; Wu, KK, 1982
)
0.26
"Patients who underwent operations in which cardiopulmonary bypass was used had elevations of plasma fibrinopeptide A which did not return to normal during bypass despite conventional heparin anticoagulation, suggesting inadequate heparin dosage and continued thrombin activity during the operation."( Elevated plasma fibrinopeptide A and thromboxane B2 levels during cardiopulmonary bypass.
Davies, GC; Salzman, EW; Sobel, M, 1980
)
0.53
" In the light of a recently proposed critical balance of vascular antiaggregatory prostacyclin and platelet proaggregatory TXA2 very low dose ASA might offer advantages over conventional dosage of ASA and should be evaluated in thromboembolic disorders."( Effects of very low versus standard dose acetyl salicylic acid, dipyridamole and sulfinpyrazone on platelet function and thromboxane formation in man.
Lorenz, R; Siess, W; Weber, PC, 1981
)
0.26
"A comparison was made of the dose-response curves obtained in the measurement of the prostaglandin E- and thromboxane A2-like activities using a cascade system consisting of a rabbit aorta strip and mesenteric artery and a rat fundus strip."( Contractile characteristics of the rat stomach strip and the rabbit aorta and mesenteric artery.
Vincent, JE; Zijlstra, FJ, 1981
)
0.26
" The aim of this study was to investigate the rate of eicosanoid biosynthesis after oral dosing with nabumetone in nine healthy subjects."( Effects of nabumetone on prostanoid biosynthesis in humans.
Cipollone, F; Cuccurullo, F; Ganci, A; Greco, A; Panara, MR; Patrignani, P; Patrono, C, 1995
)
0.29
" However, we cannot exclude the possibility that intermittent bolus-like dosing of nicotine from cigarettes could have different effects from those produced by continually released transdermal nicotine."( Nicotine effects on eicosanoid formation and hemostatic function: comparison of transdermal nicotine and cigarette smoking.
Benowitz, NL; Fitzgerald, GA; Wilson, M; Zhang, Q, 1993
)
0.29
" The bronchoconstriction was positively related to the dosage of endothelin intravenously."( [The influence of endothelin to the airway tract of guinea pig and its relationship to the asthma].
Liu, ZL; Wang, CH; Zhang, SM, 1994
)
0.29
"01) suggest that a hypercoagulable state persists in low dosage OC users."( Large increase in plasmatic 11-dehydro-TxB2 levels due to oral contraceptives.
Donnez, J; Grandjean, P; Lavenne, E; Schlit, AF, 1995
)
0.29
" For each aggregating agent, ED50 value (agonist concentration necessary to induce a maximal aggregation of 50%) was determined in control samples and following addition of different picotamide concentrations on the basis of dose-response curves."( Studies on in vitro effect of picotamide on human platelet aggregation in platelet-rich plasma and whole blood.
Anfossi, G; Cavalot, F; Massucco, P; Mattiello, L; Mularoni, EM; Parisi, S; Russo, I; Trovati, M, 1995
)
0.29
" Increases in perfusion pressure in response to bolus injections of U46619 were used to construct dose-response curves."( Reduced thromboxane receptor affinity and vasoconstrictor responses in placentae from diabetic pregnancies.
Hollander, AM; Mento, PF; Wilkes, BM, 1994
)
0.29
" Initial doses were randomly assigned and dosing intervals were separated by 2 weeks."( Effects of low-dose aspirin on in vitro platelet aggregation in the early minutes after ingestion in normal subjects.
Dabaghi, SF; Kamat, SG; Kleiman, NS; Marks, GF; Payne, J; Roberts, R; Schafer, AI, 1994
)
0.29
" The dosage was high, as judged by side-effects reported (mainly headache)."( Effects of treatment with oral isosorbide dinitrate on platelet function in vivo; a double-blind placebo-controlled study in patients with stable angina pectoris.
Andersson, A; Hjemdahl, P; Wallén, NH, 1994
)
0.29
" As a supplement to the atherogenic diet, the first group received a daily oral dose of the fish oil (FO) concentrate MaxEPA, rich in n-3 fatty acids, while the second group received the same dosage of a control oil (CO) low in n-3 fatty acids but with the same ratio of polyunsaturated to monounsaturated to saturated fatty acids as MaxEPA."( n-3 fatty acid incorporation into LDL particles renders them more susceptible to oxidation in vitro but not necessarily more atherogenic in vivo.
Fish, JR; Rand, ML; Rogers, KA; Whitman, SC, 1994
)
0.29
" Indwelling catheters were placed on the day preceding the first and last flunixin doses and 2 ml blood samples were taken for flunixin and thromboxane B2 (TXB2) assay before dosing and at 1, 2, 3, 5, 7, and 24 h after the first and the last doses of flunixin."( Flunixin in the cat: a pharmacodynamic, pharmacokinetic and toxicological study.
Jefferies, R; Lees, P; Taylor, PM; Winnard, JG,
)
0.33
" Fish oil significantly reduced the slope of the dose-response curves for collagen-induced platelet aggregation to one-third the value observed with safflower oil."( Effects of a small quantity of omega-3 fatty acids on cardiovascular risk factors in NIDDM. A randomized, prospective, double-blind, controlled study.
Axelrod, L; Briones, E; Camuso, J; Kleinman, K; Schoenfeld, D; Williams, E, 1994
)
0.29
"We compared the effect of different aspirin schedules, dosages, and formulations on various bleeding time parameters including bleeding time, plasma and total blood volume, and levels of the stable metabolites of thromboxane A2 (TXA2) and prostacyclin (PGI2) (respectively, TXB2 and 6-keto-prostaglandin F1 alpha (6-keto-PGF1 alpha)) to determine the optimal dosage and formulation of aspirin to inhibit TXA2 production while sparing PGI2."( The effect of regular and enteric-coated aspirin on bleeding time, thromboxane, and prostacyclin.
Ebbeling, L; Gerrard, JM; Gow, JA, 1993
)
0.29
" The dose-response relationship of indomethacin for inhibition of prostaglandin formation and rebamipide-induced protection correlated well and 5 mg/kg indomethacin completely prevented the protective effect of rebamipide."( Stimulation of prostaglandin biosynthesis mediates gastroprotective effect of rebamipide in rats.
Kleine, A; Kluge, S; Peskar, BM, 1993
)
0.29
" Ex vivo platelet function was measured at baseline, 1 hour after the first dose at each dosage strength, and 1 hour after the last dose at each dosage."( Effect of oral nimodipine on platelet function.
Bruck, DC; Feinberg, WM, 1993
)
0.29
" Therefore the performance of further investigations using a varying dosage and multiple application can be recommended."( Influence of a single parenteral application of a 10% fish oil emulsion on plasma fatty acid pattern and the function of thrombocytes in young adult men.
Brandt, K; Elmadfa, I; Schlotzer, E; Stroh, S, 1993
)
0.29
" The optimal dose remains uncertain, but the initial dosage of 40-60 micrograms/day given in three to four doses for adult patients is considered to be acceptable."( [Short- and long-term effects of the new oral prostacyclin analogue, beraprost sodium, in patients with severe pulmonary hypertension].
Hashiguchi, R; Matsuo, N; Matsuura, H; Morishita, T; Muto, H; Nakayama, T; Ozawa, Y; Saito, T; Saji, T; Yamazaki, J, 1996
)
0.29
" The effects of four days' dosing of a selective thromboxane A2 (TXA2) synthetase inhibitor, DP-1904 (DP), on prostanoid metabolism, were also studied."( Abnormal prostanoid metabolism in lupus nephritis and the effects of a thromboxane A2 synthetase inhibitor, DP-1904.
Homma, M; Ichikawa, Y; Tojo, T; Yoshida, T, 1996
)
0.29
"We performed the following studies: (1) a cross-sectional comparison of smokers and control subjects, (2) an examination of the dose-response relationship, (3) an exploration of the effect of smoking cessation (3 weeks) and nicotine patch supplementation, (4) the effect of aspirin consumption, and (5) the effects of 5 days' dosing with vitamin E (100 and 800 U), vitamin C (2 g), and their combination."( Modulation of oxidant stress in vivo in chronic cigarette smokers.
Delanty, N; FitzGerald, GA; Lawson, JA; Reilly, M, 1996
)
0.29
" dosing, and the bioavailability after oral dosing was approximately 70%."( Pharmacokinetic-pharmacodynamic modelling of DP-1904, a novel thromboxane synthetase inhibitor in rabbits, based on an indirect response model.
Adachi, I; Horikoshi, I; Sato, H; Zheng, NX,
)
0.13
" Although its ability to inhibit the cyclooxygenase pathway was readily observed in whole blood and in vivo, tenidap's 5-LO blockade could not be demonstrated by ionophore stimulated human blood, nor after oral dosing in rat models in which peritoneal leukotriene products were measured after challenge with three different stimuli."( Tenidap inhibits 5-lipoxygenase product formation in vitro, but this activity is not observed in three animal models.
Carty, TJ; Cheng, JD; Ernest, MJ; Eskra, JD; Griffiths, RJ; Joseph, PA; Kadin, SB; Loose, LD; Moore, PF; Murase, S; Nagahisa, A; Pazoles, PP; Pillar, JS; Sweeney, FJ, 1997
)
0.3
"To observe the pathological changes of liver sinusoidal endothelial cells, the regional perfusion with different dosage of 5-FU was performed by using modified rat's model of ILP."( [The injury of liver sinusoidal endothelial cells in a rat's isolated liver perfusion (ILP) model for regional chemotherapy].
Xia, S; Xing, X, 1996
)
0.29
" The decline in mean arterial pressure after 4 weeks of stable dosing was 10 +/- 1, 12 +/- 1, and 11 +/- 1 mm Hg for captopril, enalapril, and fosinopril, respectively (p = NS)."( ACE inhibitor effects on platelet function in stages I-II hypertension.
Callahan, KS; Cheung, AK; Moser, L; Munger, MA; Stoddard, GJ, 1997
)
0.3
" Urinary 8-epi-PGF2 alpha was unchanged after 2-week dosing with aspirin and indobufen despite complete suppression of TX metabolite excretion."( In vivo formation of 8-Epi-prostaglandin F2 alpha is increased in hypercholesterolemia.
Alessandrini, P; Bon, GB; Bucciarelli, T; Ciabattoni, G; Cipollone, F; Costantini, F; Davi, G; Mezzetti, A; Minotti, G; Patrono, C, 1997
)
0.3
" NMDA shifted the dose-response curve of AA to the right."( Further insights into the anti-aggregating activity of NMDA in human platelets.
Alberti, L; De Montis, MG; Franconi, F; Miceli, M; Seghieri, G; Tagliamonte, A, 1998
)
0.3
" The actions of tolfenamic acid in inhibiting PGE2 synthesis and in attenuating two of the cardinal signs of inflammation (heat and swelling) suggest that a dosage of 2 mgkg-1 administered intramuscularly should be effective clinically as an anti-inflammatory agent."( Pharmacodynamics and pharmacokinetics of tolfenamic acid in ruminating calves: evaluation in models of acute inflammation.
Foot, R; Gettinby, G; Lees, P; McKellar, QA, 1998
)
0.3
"The 2 arthritis trials identified SC-58635 dosage levels that were consistently effective in treating the signs and symptoms of arthritis and were distinguished from placebo on standard arthritis scales."( Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor: efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects.
Geis, GS; Hubbard, RC; Isakson, PC; Lanza, FL; Lipsky, PE; Schwartz, BD; Simon, LS; Talwalker, S, 1998
)
0.3
" Dose-response curves were plotted, and calculations were performed to identify concentrations that caused 50% inhibition (IC50 [microM]) for each isozyme."( Evaluation of selective inhibition of canine cyclooxygenase 1 and 2 by carprofen and other nonsteroidal anti-inflammatory drugs.
Lundy, KM; Ricketts, AP; Seibel, SB, 1998
)
0.3
" 8-iso-PGF2alpha was unchanged after 2-week dosing with aspirin and indobufen despite profound suppression of TXM excretion."( In vivo formation of 8-iso-prostaglandin f2alpha and platelet activation in diabetes mellitus: effects of improved metabolic control and vitamin E supplementation.
Bucciarelli, T; Capani, F; Ciabattoni, G; Consoli, A; Costantini, F; Davì, G; Falco, A; Mezzetti, A; Patrono, C; Pennese, E; Santarone, S; Vitacolonna, E, 1999
)
0.3
" Vedaprofen, administered intravenously at a dosage of 1 mg/kg, produced significant and prolonged inhibition of ex vivo serum thromboxane B2 (TXB2) synthesis and short-lived inhibition of exudate prostaglandin E2 (PGE2) and TXB2 synthesis."( A pharmacodynamic and pharmacokinetic study with vedaprofen in an equine model of acute nonimmune inflammation.
Coert, A; Hoeijmakers, M; Lees, P; May, SA; Rens, PV, 1999
)
0.51
" Blood samples were taken before and up to 6 h after dosing and the plasma obtained from it was tested for its ability to inhibit prostanoid formation in IL-1beta-treated A549 cells (COX-2 system) and human washed platelets (COX-1 system)."( Ex vivo assay to determine the cyclooxygenase selectivity of non-steroidal anti-inflammatory drugs.
Giuliano, F; Warner, TD, 1999
)
0.3
" In study 1, AA-2414 + Px produced a dose-response inhibition of Px-induced increases in perfusion pressure, vascular resistance, and maternal secretion of lipid peroxides and TXB2."( AA-2414, an antioxidant and thromboxane receptor blocker, completely inhibits peroxide-induced vasoconstriction in the human placenta.
Killian, A; Walsh, SW; Wang, Y, 1999
)
0.3
" Before dosing and 24 h after the seventh dose of each regimen, heparinized whole blood samples were incubated with lipopolysaccharide (10 microgram/ml) for 24 h at 37 degrees C, and prostaglandin E2 was measured in plasma as an index of monocyte COX-2 activity."( Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects.
Di Giamberardino, M; Panara, MR; Patrignani, P; Patrono, C; Renda, G; Rotondo, MT; Santini, G; Sciulli, MG; Seta, F; Tacconelli, S, 1999
)
0.3
"To study the influence of meloxicam, a cyclooxygenase-2 (COX-2) preferential nonsteroidal anti-inflammatory drug, on serum thromboxane and platelet function in healthy volunteers with use of the maximum recommended daily dosage of 15 mg/day."( Meloxicam, 15 mg/day, spares platelet function in healthy volunteers.
de Meijer, A; de Metz, M; Novakova, I; Thomas, C; Verbruggen, B; Vollaard, H, 1999
)
0.3
"All healthy volunteers (n = 10) received a fractionated infusion of L-aspirin to establish individual dose-response curves."( Monitoring of aspirin (ASA) pharmacodynamics with the platelet function analyzer PFA-100.
Hergovich, N; Homoncik, M; Jilma, B; Panzer, S; Speiser, W; Stohlawetz, P, 2000
)
0.31
"5 h after multiple dosing with an accumulation ratio close to 2 for all doses."( Pharmacokinetics, COX-2 specificity, and tolerability of supratherapeutic doses of rofecoxib in humans.
Dallob, A; De Lepeleire, I; De Schepper, PJ; Depré, M; Ehrich, E; Gertz, BJ; Porras, A; Van Hecken, A; Wong, P, 2000
)
0.31
" Dose-response curves to bradykinin and sodium nitroprusside were obtained to test the endothelium-dependent and endothelium-independent vasorelaxation before and during the use of a nicotine (21 mg) patch."( Transdermal nicotine mimics the smoking-induced endothelial dysfunction.
Cittadino, M; Moreno, H; Rocha, JC; Sabha, M; Tanus-Santos, JE; Toledo, JC, 2000
)
0.31
" To address this hypothesis, we used dosing with nimesulide, which inhibited COX-2 ex vivo, depressed urinary 2,3 dinor 6-keto PGF(1alpha) by approximately 60% but had no effect on thromboxane formation by platelets, which only express COX-1."( Acceleration of atherogenesis by COX-1-dependent prostanoid formation in low density lipoprotein receptor knockout mice.
FitzGerald, GA; Li, H; Praticò, D; Tillmann, C; Zhang, ZB, 2001
)
0.31
"Clearances of inulin and PAH decreased progressively after CsA dosage while renal vascular resistance increased."( Pathophysiology of cyclosporine-induced nephrotoxicity in humans: a role for nitric oxide?
Bernemann, A; Bickeböller, R; Gossmann, J; Raab, HP; Radounikli, A; Schellinski, O; Scheuermann, EH, 2001
)
0.31
" Moreover, effects of ridogrel (RID, an antagonist of TxA 2/PGH2 receptors and inhibitor of thromboxane synthetase) were analysed by cumulative dose-response curves to SER in the presence and in the absence of the NO synthase inhibitor N(omega)-nitro-L-arginine (NOLA)."( Serotonin hypersensitivity in aorta of two kidney-two clip hypertensive rats: calcium contribution and prostanoids-nitric oxide interactions.
Celentano, MM; Damiano, PF; de la Riva, IJ; Puyó, AM; Rosón, MI; Speziale, E; Vega, GW, 2001
)
0.31
"Intravenous ASA in a dosage of 100 mg did not completely prevent TXA(2) production in AMI patients treated with streptokinase."( Incomplete thromboxane inhibition with 100 mg of intravenous acetylsalicylic acid in patients with acute ST elevation myocardial infarction: a placebo-controlled pilot trial.
Husted, SE; Jensen, HK; Kristensen, SD; Nielsen, HK; Vissinger, H; Ziegler, BK, 2001
)
0.31
" There was no dose-response effect between the 3 aspirin dose groups and urinary 11-DTB2 (P=0."( Aspirin and urinary 11-dehydrothromboxane B(2) in African American stroke patients.
Bang, NU; Bruno, A; Cohen, SN; Mansbach, HH; McConnell, JP; Tietjen, GE, 2002
)
0.31
"In African American stroke patients, aspirin use is associated with significantly lower urinary 11-DTB2 independent of other vascular factors, and there does not appear to be a dose-response effect for aspirin doses of 325 to 1300 mg daily."( Aspirin and urinary 11-dehydrothromboxane B(2) in African American stroke patients.
Bang, NU; Bruno, A; Cohen, SN; Mansbach, HH; McConnell, JP; Tietjen, GE, 2002
)
0.31
" Our studies with RIA showed that: at the dosage of inhibiting platelet aggregation, ASAA was found to inhibit the formation of cyclooxygenase pathway metabolites TXB2 in platelets."( [Effects of acetylsalvianolic acid A on arachidonic acid metabolism in platelets].
Xu, L; Yu, W, 1998
)
0.3
" In contrast to standard doses of 2 nonsteroidal antiinflammatory drugs (NSAIDs), a supratherapeutic valdecoxib dosage does not impair platelet function (COX-1)."( Valdecoxib does not impair platelet function.
Kent, JD; Leese, PT; Recker, DP; Talwalker, S, 2002
)
0.31
"The discovery of a functional single-nucleotide polymorphism in the cyclooxygenase 1 locus may ultimately improve the safe and effective use of acetylsalicylic acid by better tailoring of dosage with an individual's genetic variation."( Genetic variation in cyclooxygenase 1: effects on response to aspirin.
Halushka, MK; Halushka, PV; Walker, LP, 2003
)
0.32
"To determine whether urinary 11-dehydrothromboxane B2 (d-TXB2) is a marker of aspirin resistance and define the relationship between aspirin dosage and concentrations of this thromboxane metabolite."( Aspirin dosage and thromboxane synthesis in patients with vascular disease.
Bovill, E; Cornell, E; Feinberg, WM; Hart, RG; Leonard, AD; Pearce, LA; Talbert, RL, 2003
)
0.59
" However, the optimal dosage still remains problematic, and a recent trial found aspirin 160 mg/day to be more effective than 80 mg/day for secondary prevention of ischaemic stroke."( Pharmacokinetic and pharmacodynamic differences between two low dosages of aspirin may affect therapeutic outcomes.
Cerletti, C; de Gaetano, G; Dell'Elba, G; Di Castelnuovo, A; Feliziani, V; Manarini, S; Pecce, R; Scorpiglione, N, 2003
)
0.32
"Inhibition of serum TxB2 generation and of thromboxane metabolite urinary excretion by the lower dosage of aspirin, although substantial, still appeared incomplete."( Pharmacokinetic and pharmacodynamic differences between two low dosages of aspirin may affect therapeutic outcomes.
Cerletti, C; de Gaetano, G; Dell'Elba, G; Di Castelnuovo, A; Feliziani, V; Manarini, S; Pecce, R; Scorpiglione, N, 2003
)
0.32
" Thromboxane B(2) (TxB(2)) inhibition was measured prior to lumiracoxib dosing and 2 hours afterwards."( Lumiracoxib: pharmacokinetic and pharmacodynamic profile when coadministered with fluconazole in healthy subjects.
Laurent, A; Milosavljev, S; Rordorf, C; Scott, G; Yeh, CM; Yih, L, 2004
)
0.32
"3% (mean+/-SD), respectively, and of the urinary excretion of 11-dehydro-TXB2, an index of systemic biosynthesis of TXA2 in vivo, by 85+/-8% and 78+/-7%, respectively, that persisted throughout the dosing interval."( Clinical pharmacology of platelet, monocyte, and vascular cyclooxygenase inhibition by naproxen and low-dose aspirin in healthy subjects.
Capone, ML; Di Gregorio, P; Grana, M; Merciaro, G; Minuz, P; Patrignani, P; Patrono, C; Ricciotti, E; Sciulli, MG; Tacconelli, S, 2004
)
0.32
"A certain dosage of single leaf Asarum himalaicum caused acute renal failure in rabbits."( [Influence of single leaf Asarum himalaicum on renal function of rabbits].
Huang, SZ; Liu, JJ; Ming, HX, 2004
)
0.32
"The objective of this endoscopic study was to compare the effects on the gastroduodenal mucosa of healthy volunteers of different doses and dosing regimens of AZD3582, a cyclooxygenase-inhibiting nitric oxide donator (CINOD), with equimolar doses of naproxen."( Dose-effect comparisons of the CINOD AZD3582 and naproxen on upper gastrointestinal tract mucosal injury in healthy subjects.
Fornstedt-Wallin, B; Hedman, A; Jonzon, B; Karlsson, P; Wilder-Smith, CH, 2006
)
0.33
" We performed an open cross-over study comparing no treatment (baseline) with three aspirin dosage regimens--37."( Dose- and time-dependent antiplatelet effects of aspirin.
Fitzgerald, D; Hjemdahl, P; Perneby, C; Rooney, C; Wallén, NH, 2006
)
0.33
"Understanding the mechanisms underlying the analgesic effect of new cyclooxygenase inhibitors is essential to identify dosing requirements in early stages of drug development."( Correlation between in vitro and in vivo concentration-effect relationships of naproxen in rats and healthy volunteers.
Danhof, M; Della Pasqua, OE; Huntjens, DR; Spalding, DJ, 2006
)
0.33
"We prospectively studied the effect of aspirin dosing on platelet function in 125 stable outpatients with coronary artery disease randomized in a double-blind, double-crossover investigation (81, 162, and 325 mg/d for 4 weeks each over a 12-week period)."( Evaluation of dose-related effects of aspirin on platelet function: results from the Aspirin-Induced Platelet Effect (ASPECT) study.
Bliden, KP; Chaganti, SK; DiChiara, J; Etherington, A; Gesheff, T; Gurbel, PA; Neerchal, NK; Newcomer, J; Tantry, US; Weng, W, 2007
)
0.34
" Efficacy of medicine in groups with high dosage was stronger than those with low dosage."( [Physiological effects of cold and cool Chinese herbal medicine of channel tropism of stomach on rats with stomach-heat syndrome].
Guo, BJ; Li, XE; Li, XM; Liu, JZ; Sun, GB, 2007
)
0.34
" Increased aspirin dosing resulted in similar rates of resistance and platelet function levels between groups."( The effect of aspirin dosing on platelet function in diabetic and nondiabetic patients: an analysis from the aspirin-induced platelet effect (ASPECT) study.
Antonino, MJ; Bailon, O; Bliden, KP; DiChiara, J; Gurbel, PA; Hamed, MS; Singla, A; Suarez, TA; Tantry, US, 2007
)
0.34
" Platelet aggregation induced by ADP and dosing of prostanoid products 6-keto-PGF1alpha, TXB2, PGE2 and LTB4 were also performed."( Modifications produced by selective inhibitors of cyclooxygenase and ultra low dose aspirin on platelet activity in portal hypertension.
Aguejouf, O; Belon, P; Desplat, V; Doutremepuich, C; Eizayaga, FX, 2007
)
0.34
"This multicenter, double-blind, randomized, placebo-controlled, parallel-group study assessed renal function during dosing with etoricoxib 90 mg daily, celecoxib 200 mg twice daily, and naproxen 500 mg twice daily."( Effects of etoricoxib and comparator nonsteroidal anti-inflammatory drugs on urinary sodium excretion, blood pressure, and other renal function indicators in elderly subjects consuming a controlled sodium diet.
Gertz, BJ; Gottesdiener, KM; Hilliard, DA; Hreniuk, D; Lasseter, KC; Miller, J; Schwartz, JI; Snyder, KM; Thach, C, 2007
)
0.34
"We investigated (i) platelet aggregation in vivo in HIV-1-infected adult patients (n = 5) immediately before and 2 and 4 h after dosing of tipranavir/ritonavir 500/200 mg."( Significant effects of tipranavir on platelet aggregation and thromboxane B2 formation in vitro and in vivo.
Angioni, C; Babacan, E; Graff, J; Gute, P; Harder, S; Klauke, S; Kuczka, K; von Hentig, N, 2008
)
0.59
" Behavioural endpoints for inflammatory pain and blood samples for biomarkers were obtained at various time points before and after dosing to characterise the time course of drug effect and disease progression."( Differences in the sensitivity of behavioural measures of pain to the selectivity of cyclo-oxygenase inhibitors.
Danhof, M; Della Pasqua, OE; Huntjens, DR; Spalding, DJ, 2009
)
0.35
" The untested assumption was that exposure and the resultant pharmacological effects are similar for these two administration methods when dosing is normalized on the basis of mg/kg body weight/day."( Comparison of pharmacokinetic and pharmacodynamic profiles of aspirin following oral gavage and diet dosing in rats.
Bauer, KS; Kapetanovic, IM; Lindeblad, MO; Lubet, R; Lyubimov, A; Tessier, DM; Zakharov, AD, 2009
)
0.35
" The objectives of this study were: to quantify the inhibitory actions of robenacoxib on cyclooxygenase (COX) isoenzymes in feline whole blood assays; to establish blood concentration-time profiles of robenacoxib after intravenous and subcutaneous dosing in the cat and; to predict the time courses of inhibition of COX isoforms by robenacoxib."( Differential inhibition of cyclooxygenase isoenzymes in the cat by the NSAID robenacoxib.
Giraudel, JM; King, JN; Lees, P; Toutain, PL, 2009
)
0.35
" Blood samples were collected at various intervals after dosing to characterise naproxen pharmacokinetics and its effects on PGE(2) and TXB(2) production."( Impact of chronic inflammation on the pharmacokinetic-pharmacodynamic relationship of naproxen.
Danhof, M; Della Pasqua, OE; Huntjens, DR; Spalding, DJ, 2010
)
0.36
" Further research should consider increasing aspirin dosing frequency to twice daily, to allow sustained inhibition in such subjects."( Heterogeneity in platelet cyclooxygenase inhibition by aspirin in coronary artery disease.
Diodati, JG; Lordkipanidzé, M; Palisaitis, DA; Pharand, C; Schampaert, E, 2011
)
0.37
" Once-daily dosing of aspirin might not suffice to adequately inhibit platelet aggregation in patients with an increased platelet turnover."( Effect of platelet turnover on whole blood platelet aggregation in patients with coronary artery disease.
Grove, EL; Hvas, AM; Kristensen, SD; Larsen, SB; Mortensen, SB, 2011
)
0.37
"Twenty-four hours after the last dosing on day 6 in volunteers receiving aspirin alone or aspirin before naproxen, serum TXB(2) was almost completely inhibited (median [range] 99."( Low-dose naproxen interferes with the antiplatelet effects of aspirin in healthy subjects: recommendations to minimize the functional consequences.
Anzellotti, P; Bruno, A; Capone, ML; Di Francesco, L; Di Gregorio, P; Garcia Rodriguez, LA; Grossi, L; Jeyam, A; Merciaro, G; Patrignani, P; Price, TS; Renda, G; Tacconelli, S; Tontodonati, P, 2011
)
0.37
" This may be attributed to increased platelet turnover rates resulting in an increased proportion of non-aspirin-inhibited platelets during the daily dosing interval."( Pharmacodynamic effects of different aspirin dosing regimens in type 2 diabetes mellitus patients with coronary artery disease.
Angiolillo, DJ; Bass, TA; Capodanno, D; Capranzano, P; Darlington, A; Desai, B; Dharmashankar, K; Ferreiro, JL; Kodali, M; Patel, A; Seecheran, N; Tello-Montoliu, A; Tomasello, SD; Ueno, M, 2011
)
0.37
" When aspirin was administered once daily, there was no significant effect on platelet reactivity by increasing the once-daily dosing using aspirin-sensitive assays (collagen-induced aggregation and VerifyNow-Aspirin)."( Pharmacodynamic effects of different aspirin dosing regimens in type 2 diabetes mellitus patients with coronary artery disease.
Angiolillo, DJ; Bass, TA; Capodanno, D; Capranzano, P; Darlington, A; Desai, B; Dharmashankar, K; Ferreiro, JL; Kodali, M; Patel, A; Seecheran, N; Tello-Montoliu, A; Tomasello, SD; Ueno, M, 2011
)
0.37
"Aspirin dosing regimens are associated with different pharmacodynamic effects in platelets from T2DM patients and stable coronary artery disease, with a twice-daily, low-dose aspirin administration resulting in greater platelet inhibition than once-daily administration as assessed by aspirin-sensitive assays and a dose-dependent effect on serum TXB(2) levels."( Pharmacodynamic effects of different aspirin dosing regimens in type 2 diabetes mellitus patients with coronary artery disease.
Angiolillo, DJ; Bass, TA; Capodanno, D; Capranzano, P; Darlington, A; Desai, B; Dharmashankar, K; Ferreiro, JL; Kodali, M; Patel, A; Seecheran, N; Tello-Montoliu, A; Tomasello, SD; Ueno, M, 2011
)
0.37
" We tested if twice daily dosing of aspirin would be more effective in T2DM, possibly due to increased platelet turnover."( Twice daily dosing of aspirin improves platelet inhibition in whole blood in patients with type 2 diabetes mellitus and micro- or macrovascular complications.
Arnetz, L; Brismar, K; Hjemdahl, P; Li, N; Östenson, CG; Spectre, G, 2011
)
0.37
" Administration of aspirin at a dosage of 1 mg/kg, PO, every 24 hours for 7 days did not significantly decrease urinary 11-dehydroTXB(2) concentration, but administration of the single aspirin dose of 10 mg/kg did significantly decrease 11-dehydroTXB(2) concentration by a median of 45."( Evaluation of effects of low-dose aspirin administration on urinary thromboxane metabolites in healthy dogs.
Byron, JK; Hoh, CM; McMichael, MA; Smith, SA, 2011
)
0.37
" Serum docosahexaenoyl-glycerophosphocholine concentration was increased by feeding fish oil in a dose-response manner."( Dietary fish oil alters the lysophospholipid metabolomic profile and decreases urinary 11-dehydro thromboxane B₂ concentration in healthy Beagles.
Brockman, JA; Hall, JA; Jewell, DE, 2011
)
0.37
" The anti-platelet effect may be diminished by poor glycemic control or inadequate dosing of aspirin."( The influence of aspirin dose and glycemic control on platelet inhibition in patients with type 2 diabetes mellitus.
Bähler, L; Gerdes, VE; Hoekstra, JB; Holleman, F; Kamphuisen, PW; Lemkes, BA; Nieuwland, R; Stroobants, AK; Van Den Dool, EJ, 2012
)
0.38
" We hypothesized that faster recovery of platelet cyclooxygenase-1 activity may explain incomplete thromboxane (TX) inhibition during the 24-h dosing interval."( The recovery of platelet cyclooxygenase activity explains interindividual variability in responsiveness to low-dose aspirin in patients with and without diabetes.
Cardillo, C; Davì, G; Del Ponte, A; Ferrante, E; Ghirlanda, G; Lattanzio, S; Liani, R; Martini, F; Mattoscio, D; Mirabella, M; Morosetti, R; Mucci, L; Patrono, C; Petrucci, G; Pitocco, D; Rocca, B; Santilli, F; Vazzana, N; Vitacolonna, E; Zaccardi, F, 2012
)
0.38
" Interindividual variability in the recovery of platelet cyclooxygenase activity during the dosing interval may limit the duration of the antiplatelet effect of low-dose aspirin in patients with and without diabetes."( The recovery of platelet cyclooxygenase activity explains interindividual variability in responsiveness to low-dose aspirin in patients with and without diabetes.
Cardillo, C; Davì, G; Del Ponte, A; Ferrante, E; Ghirlanda, G; Lattanzio, S; Liani, R; Martini, F; Mattoscio, D; Mirabella, M; Morosetti, R; Mucci, L; Patrono, C; Petrucci, G; Pitocco, D; Rocca, B; Santilli, F; Vazzana, N; Vitacolonna, E; Zaccardi, F, 2012
)
0.38
" These data provide a basis for the rational use of carprofen with oxytetracycline in calves and indicate that no alteration to carprofen dosage is required when the drugs are co-administered."( Influence of oxytetracycline on carprofen pharmacodynamics and pharmacokinetics in calves.
Brentnall, C; Cheng, Z; Lees, P; McKellar, QA, 2013
)
0.39
"We investigated dosage regimens for aspirin therapy in regard to antiplatelet effects in patients without gastrointestinal lesions."( Theoretical investigation of aspirin dosage regimen to exhibit optimal antiplatelet effects and decrease risk of upper gastrointestinal lesions.
Kitagawa, Y; Suzuki, Y; Tokuoka, K; Watanabe, M; Yaguchi, T; Yamada, Y; Yokoyama, H, 2012
)
0.38
"The aim of this work was to measure the response to low-dose aspirin therapy (150 mg/day) among patients with unstable angina or non-ST-segment elevation myocardial infarction and to find out whether titrating aspirin dosage to 300 mg/day, would provide a better therapeutic response in the resistant cases."( Resistance to low-dose aspirin therapy among patients with acute coronary syndrome in relation to associated risk factors.
ElSafady, LA; Morad, AR; Sabri, NA; Salama, MM; Saleh, MA; Zaki, MM, 2012
)
0.38
" The objectives of this study were to evaluate in Thai healthy volunteers: i) the inhibition of whole blood cyclooxygenase(COX)-2 and COX-1 activity by floctafenine and its metabolite floctafenic acid in vitro and ex vivo after dosing with floctafenine; ii) the possible interference of floctafenine administration with aspirin antiplatelet effects."( Clinical pharmacology of cyclooxygenase inhibition and pharmacodynamic interaction with aspirin by floctafenine in Thai healthy subjects.
Archararit, N; Aryurachai, K; Del Boccio, P; Di Francesco, L; Maenthaisong, R; Patrignani, P; Sacchetta, P; Sritara, P; Suthisisang, C; Tacconelli, S,
)
0.13
" We investigated if the effect of aspirin declined during the 24-hour dosing interval in patients with coronary artery disease and type 2 diabetes, and whether this correlated with increased platelet turnover."( Reduced antiplatelet effect of aspirin during 24 hours in patients with coronary artery disease and type 2 diabetes.
Christensen, KH; Grove, EL; Hvas, AM; Kristensen, SD; Würtz, M, 2015
)
0.42
" Our data suggest that measurement of urinary 11-dTxB2 may be a useful method to optimise statin dosing in order to reduce thrombotic risk."( Statin therapy and thromboxane generation in patients with coronary artery disease treated with high-dose aspirin.
Bliden, KP; Ens, G; Franzese, CJ; Gesheff, MG; Gurbel, PA; Guyer, K; Singh, M; Singla, A; Stapleton, D; Tabrizchi, A; Tantry, US; Toth, PP, 2014
)
0.4
" After chronic dosing with aspirin, the pharmacokinetics of acetylsalicylic acid was completely dissociated from pharmacodynamics."( Reappraisal of the clinical pharmacology of low-dose aspirin by comparing novel direct and traditional indirect biomarkers of drug action.
Del Boccio, P; Di Francesco, L; Dovizio, M; Guillem-Llobat, P; Lanas, A; Marcantoni, E; Patrignani, P; Patrono, C; Piazuelo, E; Sostres, C; Tacconelli, S; Zucchelli, M, 2014
)
0.4
" Further investigations are required to establish an optimal dosage regimen and safety profile before clinical trials are initiated."( Evaluation of pharmacokinetic and pharmacodynamic properties of cimicoxib in fasted and fed horses.
Della Rocca, G; Di Salvo, A; Giorgi, M; Kim, TW; Ryschanova, R; Sgorbini, M, 2015
)
0.42
" Therefore, aspirin dosage can be adjusted individually to reach maximum effect of platelet inhibition."( Aspirin resistance in children and young adults with splenectomized thalassemia diseases.
Chuansumrit, A; Kadegasem, P; Sirachainan, N; Soisamrong, A; Wijarn, P; Wongwerawattanakoon, P, 2015
)
0.42
" Inflammatory bowel disease was induced by replacing drinking water with 3 % DSS solution during the last 7 d of the AA dosing period."( Effects of arachidonic acid intake on inflammatory reactions in dextran sodium sulphate-induced colitis in rats.
Aoki, S; Furuya, M; Harauma, A; Iwai, N; Ji, X; Miyazawa, D; Moriguchi, T; Nagata, T; Naito, Y; Ohara, N; Tachibana, S; Tazura, Y, 2015
)
0.42
" The final model was then used to simulate a proof-of-concept study and to explore suitable dosing ranges in case of hepatic dysfunction or metabolic induction."( Biomarker exposure-response relationships as the basis for rational dose selection: Lessons from a simulation exercise using a selective COX-2 inhibitor.
Danhof, M; Della Pasqua, O; Oosterholt, SP; Taneja, A, 2016
)
0.43
" Peak inhibition of urinary metabolite excretion across 8 hours following dosing was the primary end point."( Inhibition of prostacyclin and thromboxane biosynthesis in healthy volunteers by single and multiple doses of acetaminophen and indomethacin.
Gottesdiener, KM; Greenberg, HE; Mehta, A; Musser, BJ; Schwartz, JI; Taggart, WV; Tanaka, WK, 2015
)
0.42
" The optimal dosage of ASA is not known."( Platelet function one and three months after coronary bypass surgery in relation to once or twice daily dosing of acetylsalicylic acid.
Ander, C; Dalén, M; Hjemdahl, P; Ivert, T; Lordkipanidzé, M; Näsman, P; Stålesen, R, 2017
)
0.46
" We tested whether more frequent dosing improves aspirin (ASA) response following CABG surgery."( Once versus twice daily aspirin after coronary bypass surgery: a randomized trial.
Chan, NC; Eikelboom, JW; Ginsberg, JS; Hirsh, J; Paikin, JS; Pare, G; Weitz, JI; Whitlock, RP, 2017
)
0.46
"Electrospray ionization and chromatographic separation were optimized for the simultaneous dosage of serotonin and TxB2."( Development and validation of a liquid chromatography/tandem mass spectrometry method for the simultaneous quantification of serotonin and thromboxane B2 from activated platelets.
Dogné, JM; Evrard, J; Minet, V; Mullier, F; Pochet, L; Vancraeynest, C, 2018
)
0.68
" It has been proposed that shortening the ASA dosing interval may overcome the time-dependent renewal of the drug target, leading to a greater antiplatelet effect."( Once- versus Twice-Daily Aspirin in Patients at High Risk of Thrombotic Events: Systematic Review and Meta-Analysis.
Caldeira, D; Costa, J; Duarte, GS; Ferreira, J; Mainoli, B, 2021
)
0.62
" The collection days (CD) were the second and seventh days after stable aspirin dosing and then a convalescent time point 2-9 months later."( Urinary 11-dehydrothromboxane B2 aspirin efficacy testing is sensitive to perioperative inflammation in pediatric solid-organ transplant patients.
Boucher, AA; Francisco, BJ; Luchtman-Jones, L; Martin, J; Martin, M; Nathan, JD; Pfeiffer, A; Shova, A; Tiao, GM, 2022
)
1.06
" Guidelines are also inconsistent in the recommendation of routine ASA use for primary prevention of CVD, but advocate dosing as a "one-size-fits-all" approach."( Prospective, randomized, controlled, trial to assess ASA DOSing by body mass index in HEalthy volunteers (DOSE study).
Hutchinson, D; Kim, K; Kirkham, A; Kroencke, R; Munger, M; Nay, I; Rondina, M; Tolley, ND; Trujillo, T, 2023
)
0.91
"An intention-to-treat, double-blind, randomized, controlled, clinical trial comparing three treatment arms of ASA 81, 325, and 500 mg daily dosed for 14 days were evenly randomized across the dosing categories to measure the impact of dosing by body mass index (BMI) (20-24."( Prospective, randomized, controlled, trial to assess ASA DOSing by body mass index in HEalthy volunteers (DOSE study).
Hutchinson, D; Kim, K; Kirkham, A; Kroencke, R; Munger, M; Nay, I; Rondina, M; Tolley, ND; Trujillo, T, 2023
)
0.91
"Change in ASA reactivity unit (ARU), salicylate levels, and thromboxane B2 (TxB2) levels were measured across BMI dosing categories and time."( Prospective, randomized, controlled, trial to assess ASA DOSing by body mass index in HEalthy volunteers (DOSE study).
Hutchinson, D; Kim, K; Kirkham, A; Kroencke, R; Munger, M; Nay, I; Rondina, M; Tolley, ND; Trujillo, T, 2023
)
1.15
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[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
thromboxanes B
[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 (53)

PathwayProteinsCompounds
Metabolism14961108
Metabolism of lipids500463
Fatty acid metabolism113203
Arachidonic acid metabolism3682
Synthesis of Prostaglandins (PG) and Thromboxanes (TX)1135
Arachidonic Acid Metabolism2966
Leukotriene C4 Synthesis Deficiency2966
Piroxicam Action Pathway2967
Acetylsalicylic Acid Action Pathway2967
Etodolac Action Pathway2967
Ketoprofen Action Pathway2967
Ibuprofen Action Pathway5076
Rofecoxib Action Pathway2967
Diclofenac Action Pathway2967
Sulindac Action Pathway2967
Celecoxib Action Pathway3573
Ketorolac Action Pathway2967
Suprofen Action Pathway2967
Bromfenac Action Pathway2967
Indomethacin Action Pathway3067
Mefenamic Acid Action Pathway2967
Oxaprozin Action Pathway2967
Nabumetone Action Pathway2967
Naproxen Action Pathway2967
Diflunisal Action Pathway2967
Meloxicam Action Pathway2967
Valdecoxib Action Pathway2967
Antipyrine Action Pathway2967
Antrafenine Action Pathway2967
Carprofen Action Pathway2967
Etoricoxib Action Pathway2967
Fenoprofen Action Pathway2967
Flurbiprofen Action Pathway2967
Magnesium Salicylate Action Pathway2967
Lumiracoxib Action Pathway2967
Lornoxicam Action Pathway2967
Phenylbutazone Action Pathway2967
Nepafenac Action Pathway2967
Trisalicylate-Choline Action Pathway2967
Tolmetin Action Pathway2967
Tiaprofenic Acid Action Pathway2967
Tenoxicam Action Pathway2967
Salsalate Action Pathway2967
Salicylate-Sodium Action Pathway2967
Salicylic Acid Action Pathway2967
Acetaminophen Action Pathway2967
Eicosanoid metabolism via cyclooxygenases (COX)137
Arachidonic acid (AA, ARA) oxylipin metabolism076
Folic acid network070
Selenium micronutrient network095
Vitamin B12 metabolism050
Eicosanoid synthesis026
Folate metabolism156
Arachidonic acid metabolism via COX (Cyclooxygenase) pathway035

Protein Targets (2)

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier organic anion transporter family member 2A1Rattus norvegicus (Norway rat)Km0.42300.07001.65207.5690AID681576
Solute carrier organic anion transporter family member 2A1Homo sapiens (human)K1/20.18200.08200.10780.1820AID682149
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (4)

Processvia Protein(s)Taxonomy
lipid transportSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
lipid transporter activitySolute carrier organic anion transporter family member 2A1Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 2A1Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
lysosomeSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
membraneSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 2A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID681367TP_TRANSPORTER: uptake in Xenopus laevis oocytes2003American journal of physiology. Renal physiology, Dec, Volume: 285, Issue:6
Molecular characterization of human and rat organic anion transporter OATP-D.
AID682149TP_TRANSPORTER: uptake in PGT-expressing HeLa cells1996The Journal of clinical investigation, Sep-01, Volume: 98, Issue:5
Cloning, in vitro expression, and tissue distribution of a human prostaglandin transporter cDNA(hPGT).
AID681576TP_TRANSPORTER: uptake in PGT-expressing HeLa cells1995Science (New York, N.Y.), May-12, Volume: 268, Issue:5212
Identification and characterization of a prostaglandin transporter.
AID681092TP_TRANSPORTER: inhibition of alaninyl-d4TMP in the presence of Thromboxane B2 at a concentration of 20uM in membrane vesicles from MRP1-expressing Sf9 cells2003Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16
The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs.
AID681173TP_TRANSPORTER: uptake in Xenopus laevis oocytes2000Biochemical and biophysical research communications, Sep-07, Volume: 275, Issue:3
Molecular identification of a rat novel organic anion transporter moat1, which transports prostaglandin D(2), leukotriene C(4), and taurocholate.
AID681870TP_TRANSPORTER: inhibition of alaninyl-d4TMP by Thromboxane B2 at a concentration of 20uM in membrane vesicle from MRP5-expressing HEK293 cells2003Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16
The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs.
AID680416TP_TRANSPORTER: inhibition of alaninyl-d4TMP by Thromboxane B2 at a concentration of 20uM in membrane vesicle from MRP3-expressing Sf9 cells2003Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16
The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs.
AID681886TP_TRANSPORTER: inhibition of alaninyl-d4TMP in the presence of Thromboxane B2 at a concentration of 20uM in membrane vesicles from MRP4-expressing Sf9 cells2003Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16
The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs.
AID681342TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999The Journal of biological chemistry, Jun-11, Volume: 274, Issue:24
Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7,209)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903182 (44.14)18.7374
1990's2583 (35.83)18.2507
2000's896 (12.43)29.6817
2010's504 (6.99)24.3611
2020's44 (0.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.90

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index24.90 (24.57)
Research Supply Index9.01 (2.92)
Research Growth Index4.24 (4.65)
Search Engine Demand Index39.34 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.90)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials715 (9.55%)5.53%
Reviews118 (1.58%)6.00%
Case Studies60 (0.80%)4.05%
Observational15 (0.20%)0.25%
Other6,575 (87.87%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]