Page last updated: 2024-12-05

trapidil

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Description

Trapidil: A coronary vasodilator agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5531
CHEMBL ID132767
CHEBI ID32254
SCHEMBL ID33563
MeSH IDM0021847

Synonyms (95)

Synonym
BRD-K95763993-001-03-7
MLS000567667 ,
trapidil
rocornal
smr000154170
cas-15421-84-8
NCGC00016715-01
BPBIO1_001281
BSPBIO_001163
PRESTWICK2_001012
AB00457635
D01220
rocornal (tn)
trapidil (jp17/inn)
15421-84-8
ar 12008
7-diethylamino-5-methyl-s-triazolo(1,5-a)pyrimidine
n,n-diethyl-5-methyl-(1,2,4)triazolo(1,5-a)pyrimidine-7-amine
einecs 239-434-2
5-methyl-7-diethylamino-s-triazolo-(1,5-a)-pyrimidine
(1,2,4)triazolo(1,5-a)pyrimidin-7-amine, n,n-diethyl-5-methyl-
s-triazolo(1,5-a)pyrimidin-7-amine, n,n-diethyl-5-methyl-
trapymin
5-methyl-7-diaethylamino-s-triazolo(1.5-a)pyrimidin [german]
trapidilum [inn-latin]
brn 0186842
SPBIO_003034
PRESTWICK0_001012
PRESTWICK1_001012
PRESTWICK3_001012
NCGC00016715-02
MLS000881142
ar-12008
CHEMBL132767
AKOS001093408
HMS1571K05
HMS1735K19
n,n-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
HMS2098K05
5-methyl-7-diaethylamino-s-triazolo(1.5-a)pyrimidin
eyg5y6355e ,
trapidilum
unii-eyg5y6355e
trapidil [inn:ban:jan]
dtxcid8025416
tox21_110578
dtxsid0045416 ,
[1,2,4]triazolo[1,5-a]pyrimidin-7-amine,n,n-diethyl-5-methyl-
HMS2231G07
S4736
trapymine
avantrin
trapidil [inn]
trapidil [jan]
7-(diethylamino)-5-methyl-s-triazolo(1,5-a)pyrimidine.
trapidil [mart.]
trapidil [ep monograph]
trapidil [who-dd]
trapidil [mi]
HMS3372J09
CCG-221012
AB00457635-12
SCHEMBL33563
NCGC00016715-04
tox21_110578_1
HS-0048
CS-4529
n,n-diethyl-4-methyl-1,5,7,9-tetrazabicyclo[4.3.0]nona-2,4,6,8-tetraen-2-amine
GSNOZLZNQMLSKJ-UHFFFAOYSA-N
7-(diethylamino)-5-methyl-2-triazolo[1,5-a]pyrimidine
5-methyl-7-diethylamino-s-triazolo(1,5-a)pyrimidine
[1,2,4]triazolo[1,5-a]pyrimidin-7-amine, n,n-diethyl-5-methyl-
5-methyl-7-(diethylamino)-s-triazolo[1,5-a]pyrimidine
n,n-diethyl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine #
HY-B1016
AC-32565
OPERA_ID_461
mfcd00193104
DB09283
SR-01000673280-3
sr-01000673280
trapidil, european pharmacopoeia (ep) reference standard
trapidil, >=98% (hplc)
CHEBI:32254
HMS3715K05
Z56791867
A927178
FT-0763046
F31376
trapidil,(s)
Q2449982
diethyl-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)amine
BCP09350
NCGC00016715-03
EN300-227431

Research Excerpts

Overview

Trapidil is a triazolopyrimidine that has been found to prevent restenosis after vascular injury. It is an antiplatelet drug with specific platelet-derived growth factor antagonism and antiproliferative effects in the rat and rabbit models after balloon angioplasty.

ExcerptReferenceRelevance
"Trapidil is an antianginal compound with a broad spectrum of pharmacological activities. "( Protective effect of trapidil on long-term histologic damage in a rat model of testicular ischemia-reperfusion injury.
Acar, D; Aktas, S; Bozlu, M; Cayan, S; Tunckiran, A, 2009
)
2.11
"Trapidil is a triazolopyrimidine that has been found to prevent restenosis after vascular injury. "( Trapidil inhibits monocyte CD40 expression by preventing IFN-gamma-induced STAT1 S727 phosphorylation.
Chatelain, P; Goldman, M; Mordvinov, VA; Pradier, O; Schandené, L; Stordeur, P; Zhou, L, 2004
)
3.21
"Trapidil is an antiplatelet agent and several studies demonstrate the beneficial effect of trapidil in various forms of tissue injury."( The role of trapidil on neuronal apoptosis in neonatal rat model of hypoxic ischemic brain injury.
Atici, A; Bozlu, G; Nayci, A; Okuyaz, C; Polat, A; Taskinlar, H; Turhan, AH, 2008
)
1.45
"Trapidil was expected to be an effective antithrombotic agent."( Antithrombotic activity and the mechanism of action of trapidil (Rocornal).
Kitamura, Y; Ohnishi, H; Shimada, S; Suzuki, Y; Yamaguchi, K, 1982
)
1.23
"Trapidil is a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells, U251MG. "( The mechanism of growth-regulation of glioma cells by trapidil.
Kuratsu, J; Morioka, M; Saitoh, Y; Sato, K; Takeshima, H; Ushio, Y, 1995
)
1.98
"Trapidil is an antiplatelet drug with specific platelet-derived growth factor antagonism and antiproliferative effects in the rat and rabbit models after balloon angioplasty."( Trapidil (triazolopyrimidine), a platelet-derived growth factor antagonist, reduces restenosis after percutaneous transluminal coronary angioplasty. Results of the randomized, double-blind STARC study. Studio Trapidil versus Aspirin nella Restenosi Corona
Balducelli, M; Cantini, L; Casari, A; Chioin, R; De Servi, S; Fabbri, M; Fontanelli, A; Maresta, A; Monici Preti, PA; Repetto, S, 1994
)
3.17
"Trapidil is an inhibitor of phosphodiesterase I-IV with resulting positive lusitropic, vasodilating, and antiplatelet effects."( Double-blind randomized multicenter study on the efficacy of trapidil versus isosorbide dinitrate in stable angina pectoris.
Bussmann, WD; Raubach, KH; Vlahov, V; Wolter, K, 1997
)
1.98
"Trapidil, which is an anti-PDGF agent, inhibits the effect of PDGF, especially the proliferative effects on the glial and tumoral cells in vitro."( The effect of trapidil on the reactive astrocytic proliferation following spinal cord trauma in rats: light and electron microscopic findings.
Cetinalp, E; Göçer, AI; Haciyakupoglu, S; Kaya, M; Ozel, S; Polat, S; Tuna, M, 1998
)
1.38
"Trapidil (Tra) is a potent coronary vasodilator. "( Antiproliferative effects of trapidil in vascular smooth muscle cells are associated by inhibition of MAPK and P34(cdc2) activity.
Chen, H; Cheng, Y; Liu, P; Zeng, F, 2000
)
2.04

Effects

Trapidil has various properties including vasodilatation, inhibition of lipid peroxidation and platelet aggregation as well as, and reduction of, the inflammatory response to injury. It has been shown to prevent restenosis after PTCA.

ExcerptReferenceRelevance
"Trapidil has a particularly unfavourable effect, if it is given after isoprenalin."( [Modification of the isoprenaline-induced myocardial necrosis using trapidil].
Lampe, D; Lange, B; Mai, I, 1976
)
1.21
"Trapidil has been described to improve the redox balance and cardiac conditions."( Trapidil improves hemodynamic, echocardiographic and redox state parameters of right ventricle in monocrotaline-induced pulmonary arterial hypertension model.
Belló-Klein, A; Carraro, CC; Colombo, R; da Rosa Araujo, AS; de Lima-Seolin, BG; Lacerda, DS; Poletto Bonetto, JH; Schenkel, PC; Teixeira, RB; Türck, P, 2018
)
2.64
"Trapidil has various properties including vasodilatation, inhibition of lipid peroxidation and platelet aggregation as well as, and reduction of, the inflammatory response to injury. "( Effects of trapidil on the healing of colonic anastomoses in an experimental rat model.
Aydin, S; Colak, T; Comelekoglu, U; Kanik, A; Nayci, A; Polat, A; Polat, G; Turkmenoglu, O, 2003
)
2.15
"Trapidil has been shown to prevent restenosis after PTCA."( Starc II, a multicenter randomized placebo-controlled double-blind clinical trial of trapidil for 1-year clinical events and angiographic restenosis reduction after coronary angioplasty and stenting.
Balducelli, M; Barlera, S; Bernardi, G; Latini, R; Maggioni, AP; Maresta, A; Moccetti, T; Monici Preti, A; Ribeiro da Silva, EE; Sosa, C; Varani, E, 2005
)
1.27
"Trapidil has various properties, such as inhibition of platelet aggregation and lipid peroxidation as well as reduction of the inflammatory response to injury."( Protective effect of trapidil against oxidative organ damage in burn injury.
Aksöyek, S; Avlan, D; Camdeviren, H; Ozturhan, H; Oztürk, C; Tamer, L; Taşkinlar, H, 2005
)
1.37
"Trapidil has been shown to possess the protective effects in the treatment of ischemia and reperfusion injury in the peripheral nervous system. "( Effects of low dose trapidil on electrical properties of a rat peripheral nerve after crush injury.
Büyükakilli, B; Güneş, S; Taşdelen, B, 2007
)
2.11
"Trapidil has shown a more complete antithrombocytic activity than other antiaggregating drugs; as a matter of fact it inhibits the formation of TXA2 through a mechanism of receptorial antagonism and at the same time it favours an increase of prostacyclina from the arterial walls."( [Trapidil after one year].
Agus, GB, 1993
)
1.92
"Trapidil has been shown to attenuate intimal hyperplasia in rat and hamster models of balloon arterial injury and to inhibit restenosis after percutaneous transluminal coronary angioplasty in several small clinical trials."( Trapidil inhibits monocyte chemoattractant protein-1 and macrophage accumulation after balloon arterial injury in rabbits.
Cohen, J; Fallon, JT; Poon, M; Siddiqui, Z; Taubman, MB, 1999
)
2.47
"Trapidil has a particularly unfavourable effect, if it is given after isoprenalin."( [Modification of the isoprenaline-induced myocardial necrosis using trapidil].
Lampe, D; Lange, B; Mai, I, 1976
)
1.21

Actions

Trapidil inhibited the increase of total lipid (TL), total cholesterol (TC), free cholesterol (FC) and phospholipid (PL) Trapidil produced an increase in myocardial oxygen consumption but virtually no change in coronary arteriovenous oxygen difference.

ExcerptReferenceRelevance
"Trapidil inhibited the increase of total lipid (TL), total cholesterol (TC), free cholesterol (FC) and phospholipid (PL) by the cholesterol diet in all groups."( [Effect of trapidil on experimental hyperlipemia and atherosclerosis induced by cholesterol diet in SPF Japanese white rabbits].
Gotoh, H; Nakayama, S; Sakamoto, K; Tonooka, M, 1983
)
1.38
"Trapidil produced an increase in myocardial oxygen consumption but virtually no change in coronary arteriovenous oxygen difference."( Mechanism of cardiovascular action of trapidil.
Endoh, M; Satoh, K; Taira, N; Yamashita, S, 1980
)
1.25
"Trapidil showed an increase in retrograde blood flow while dipyridamole, nifedipine, diltiazem and dilazep did not."( [Pharmacological properties of trapidil: comparison with other coronary vasodilators (author's transl)].
Funato, H; Itoh, C; Itoh, R; Kitamura, Y; Kosuzume, H; Ohnishi, H; Sato, M; Suzuki, K; Suzuki, Y; Umehara, S; Yamaguchi, K, 1980
)
1.27
"Trapidil could inhibit these effects of 5-HT or phenylephrine."( Analysis of relaxant effects of trapidil in isolated dog coronary artery.
Fukai, R; Higuchi, M; Hirata, A; Kondoh, G; Sakanashi, M; Yoshikawa, Y, 1980
)
1.27
"Trapidil and suramin inhibit this growth factor-stimulated glioma cell growth, but the mechanisms are not fully understood."( Effects of trapidil and suramin on growth factor-induced calcium response and tyrosine phosphorylation in human glioma cells.
Bando, K; Kannuki, S; Matsumoto, K; Rokutan, K; Shouno, M, 1995
)
1.4
"Trapidil did not produce any tachyarrhythmias or contractures."( Effects of the triazolopyrimidine trapidil on force of contraction, beating frequency and phosphodiesterase I--IV activity in guinea-pig hearts.
Bethke, T; Mehl, H; Meyer, W; Schmitz, W; Scholz, H; Thomas, K; Wenzlaff, H, 1991
)
1.28

Treatment

Trapidil treatment either before or after hypoxia results in significant reduction of the numbers of apoptotic cells in both hemispheres. Treatment with trapidil or L-arginine diminished the renal and hepatic CsA-induced toxicity.

ExcerptReferenceRelevance
"Trapidil treatment significantly reduced in biochemical parameters, as well as serum TNF-alpha levels."( Protective effect of trapidil against oxidative organ damage in burn injury.
Aksöyek, S; Avlan, D; Camdeviren, H; Ozturhan, H; Oztürk, C; Tamer, L; Taşkinlar, H, 2005
)
1.37
"Trapidil treatment groups were administrated a single dose of trapidil (8 mg/kg) intraperitoneally just after the injury."( Effects of trapidil after crush injury in peripheral nerve.
Aktekin, M; Bagdatoglu, C; Bagdatoglu, O; Camdeviren, H; Kurtoglu, Z; Ozturk, AH; Polat, G; Sargon, M; Uzmansel, D, 2005
)
1.44
"The trapidil-treated samples showed significantly decreased platelet aggregation compared to the control samples (24.2%+/-12.6% vs 66.7%+/-11.7%; P<.001)."( Trapidil decreases the aggregation of platelets from heart transplant recipients ex vivo.
Frass, O; Friedel, A; Heidinger, K; Jovin, A; Jovin, IS; Klövekorn, WP; Müller-Berghaus, G; Schreiner, K; Segieth, I; Szalay, Z; Taborski, U, 2006
)
2.26
"Trapidil treatment significantly reduced in biochemical parameters, as well as serum urea, AST, and TNF-alpha levels."( Effects of trapidil on renal ischemia-reperfusion injury.
Aksöyek, S; Avlan, D; Ayaz, L; Camdeviren, H; Ozturhan, H; Oztürk, C; Polat, A; Tamer, L, 2006
)
1.45
"Trapidil treatment either before or after hypoxia results in significant reduction of the numbers of apoptotic cells in both hemispheres, when it is compared with saline treatment group. "( The role of trapidil on neuronal apoptosis in neonatal rat model of hypoxic ischemic brain injury.
Atici, A; Bozlu, G; Nayci, A; Okuyaz, C; Polat, A; Taskinlar, H; Turhan, AH, 2008
)
2.17
"Trapidil treatment groups were administrated a single dose of trapidil (8 mg/kg) intraperitoneally just after the injury."( Effects of low dose trapidil on electrical properties of a rat peripheral nerve after crush injury.
Büyükakilli, B; Güneş, S; Taşdelen, B, 2007
)
1.38
"Treatment with trapidil or L-arginine diminished the renal and hepatic CsA-induced toxicity. "( Protective effect of trapidil and l-arginine against renal and hepatic toxicity induced by cyclosporine in rats.
El-Dayem, WA; Eladl, M; Elgalaly, H; Kamel, M; Maarouf, AM; Radwan, M; Salem, EA; Salem, NA, 2010
)
1.03

Toxicity

ExcerptReferenceRelevance
" Coadministration of trapidil + L-arginine significantly ameliorated the toxic effect of CsA, but did not differ significantly from the effect of trapidil alone."( Protective effect of trapidil and l-arginine against renal and hepatic toxicity induced by cyclosporine in rats.
El-Dayem, WA; Eladl, M; Elgalaly, H; Kamel, M; Maarouf, AM; Radwan, M; Salem, EA; Salem, NA, 2010
)
1

Pharmacokinetics

This paper describes a suitable and cost-saving method for quantitative analysis of trapidil (5-methyl-7-diethylamino-s-triazolo [1,5-a]pyrimidine) and its desethyl metabolite in plasma and urine.

ExcerptReferenceRelevance
" The pharmacokinetic parameters were compared with the parameters of 12 healthy volunteers, investigated by Weiss [1991]."( Pharmacokinetics of trapidil (Rocornal) in patients with chronic liver disease.
Berndt, A; Pönicke, K; Weiss, M, 1992
)
0.61
"This paper describes a suitable and cost-saving method for quantitative analysis of trapidil (5-methyl-7-diethylamino-s-triazolo [1,5-a]pyrimidine) and its desethyl metabolite in plasma and urine for pharmacokinetic and bioavailability investigations."( Gas chromatographic evaluation of trapidil and its desethyl metabolite in biological fluids for pharmacokinetic and bioavailability investigations.
Maggi, GC; Marzo, A; Pasotti, V, 1987
)
0.78
" Pharmacokinetic parameters of trapidil (an antagonist of platelet derived growth factor) were evaluated in 12 healthy male subjects (study I) and in a group of 10 patients with liver cirrhosis (Child B) and five control subjects, respectively (study II)."( Pharmacokinetics of trapidil, an antagonist of platelet derived growth factor, in healthy subjects and in patients with liver cirrhosis.
Benjaminov, A; Harder, S; Hellstern, A; Thürmann, PA, 1996
)
0.9
" Mean pharmacokinetic parameters were compared with those found in a previous study of 12 healthy volunteers."( Pharmacokinetics of trapidil in patients with chronic liver disease.
Berndt, A; Looby, M; Pönicke, K; Weiss, M; Zipprich, B, 1996
)
0.62
" In one patient (group B) receiving tamoxifen comedication markedly elevated plasma concentrations of trapidil and desethyltrapidil occurred, suggesting a pharmacokinetic interaction."( Pharmacokinetics of the PDGF-antagonist trapidil in patients with and without renal impairment.
Fritschka, E; Harder, S; Münck, AC; Thürmann, PA; Wolter, K, 1997
)
0.78
" These drugs must be administered parenterally and have a half-life of only a few minutes."( Clinical pharmacokinetics of vasodilators. Part II.
Heintz, B; Kirsten, D; Kirsten, R; Nelson, K, 1998
)
0.3

Bioavailability

Trapidil from Rosupol U suppositories was inferior in four of the five test subjects.

ExcerptReferenceRelevance
" Complete bioavailability was obtained and a mean absorption time of 66."( Bioavailability of trapidil tablets.
Fahr, A; Mest, HJ; Pönicke, K; Schobess, M; Sziegoleit, W; Weiss, M, 1989
)
0.61
"This paper describes a suitable and cost-saving method for quantitative analysis of trapidil (5-methyl-7-diethylamino-s-triazolo [1,5-a]pyrimidine) and its desethyl metabolite in plasma and urine for pharmacokinetic and bioavailability investigations."( Gas chromatographic evaluation of trapidil and its desethyl metabolite in biological fluids for pharmacokinetic and bioavailability investigations.
Maggi, GC; Marzo, A; Pasotti, V, 1987
)
0.78
"In a study with five healthy persons designed to compare the bioavailability of Trapidil from Rosupol U suppositories with that from Witepsol H 15 suppositories, the availability of Trapidil from the Rosupol U suppositories was inferior in four of the five test subjects."( [The bioavailability of trapidil from suppositories (author's transl)].
Bornschein, M; Grohmann, A; Grune, D; Hackenberger, F, 1981
)
0.8
" In one example, the analysis of bioavailability data of an extended-release formulation, as well as the mean dissolution times estimated in vivo and in vitro with the use of the inverse Gaussian function, is well in accordance, suggesting that the inverse Gaussian function indeed accounts for the in vivo dissolution process."( A note on population analysis of dissolution-absorption models using the inverse Gaussian function.
D'Argenio, DZ; Wang, J; Weiss, M, 2008
)
0.35
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Trapidil clearance is a parameter that is very sensitive to alterations in hepatic clearance caused by liver cirrhosis. Patients received either trapidil 100 mg TID or aspirin at the same dosage at least 3 days before angioplasty and for 6 months thereafter.

ExcerptRelevanceReference
" In a dosage of 300 mg a day orally trapymin had no clear influence on the non-esterified fatty acids."( [Influence of coronary-effective substances on the concentration of nonesterified fatty acids in the serum of patients with angina pectoris].
Heiland, G; Modersohn, D; Pankau, H; Urbaszek, W, 1975
)
0.25
" The dose-response curve of TM was parallel to that of nitroglycerin and papaverine and steeper than that of dipyridamol or adenosine."( [Pharmacology of cornary dilator agent, trapymin. (2) Analysis of its mode of action].
Ogawa, N; Ohnishi, H; Tsukuda, S; Yamaguchi, K, 1975
)
0.25
" It might be concluded from this study, that dosage adjustments are necessary in treatment of patients with cirrhosis."( Pharmacokinetics of trapidil (Rocornal) in patients with chronic liver disease.
Berndt, A; Pönicke, K; Weiss, M, 1992
)
0.61
" Thus, in clinical use of aspirin or ticlopidine, it may be expected that the lower dosage of aspirin or ticlopidine with lower frequencies of side effects inhibits platelet aggregation effectively with the combination of trapidil rather than dipyridamole."( Effect of the combination of antiplatelet agents in man: combination of aspirin, trapidil, ticlopidine and dipyridamole.
Akedo, Y; Nagakawa, Y; Orimo, H; Yano, H, 1990
)
0.69
" 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
)
0.81
" Dose-response curves for tracheal vasodilatation to the three drugs were all parallel together, and trapidil was about 2700 time less potent than isoproterenol and about 3 times more potent than theophylline on a weight basis in producing tracheal vasodilatation."( Effects of trapidil on musculature and vasculature of the dog trachea in situ.
Maruyama, M; Satoh, K; Taira, N, 1981
)
0.87
" Patients received either trapidil 100 mg TID or aspirin at the same dosage at least 3 days before angioplasty and for 6 months thereafter."( Trapidil (triazolopyrimidine), a platelet-derived growth factor antagonist, reduces restenosis after percutaneous transluminal coronary angioplasty. Results of the randomized, double-blind STARC study. Studio Trapidil versus Aspirin nella Restenosi Corona
Balducelli, M; Cantini, L; Casari, A; Chioin, R; De Servi, S; Fabbri, M; Fontanelli, A; Maresta, A; Monici Preti, PA; Repetto, S, 1994
)
2.03
"Trapidil reduces restenosis after PTCA at the dosage of 100 mg TID and favorably influences the clinical outcome thereafter."( Trapidil (triazolopyrimidine), a platelet-derived growth factor antagonist, reduces restenosis after percutaneous transluminal coronary angioplasty. Results of the randomized, double-blind STARC study. Studio Trapidil versus Aspirin nella Restenosi Corona
Balducelli, M; Cantini, L; Casari, A; Chioin, R; De Servi, S; Fabbri, M; Fontanelli, A; Maresta, A; Monici Preti, PA; Repetto, S, 1994
)
3.17
" It can be concluded that trapidil clearance is a parameter that is very sensitive to alterations in hepatic clearance caused by liver cirrhosis, and that the dosage of trapidil should be adjusted accordingly in such patients."( Pharmacokinetics of trapidil in patients with chronic liver disease.
Berndt, A; Looby, M; Pönicke, K; Weiss, M; Zipprich, B, 1996
)
0.92
"Solid dispersion (SD) of indomethacin with crospovidone (CrosPVP) shows useful characteristics for preparation of dosage forms."( Effect of characteristics of compounds on maintenance of an amorphous state in solid dispersion with crospovidone.
Fujii, M; Kokudai, M; Kondoh, M; Noda, S; Okada, H; Shibata, Y; Watanabe, Y, 2007
)
0.34
" In the three similar studies with oral medications dose-response curves for venoconstriction by locally infused norepinephrine were established before and 1 h, 2 h and 3 h after oral medication and ED50 values of norepinephrine were calculated."( Influence of systemically given placebo, trapidil and isosorbide dinitrate on norepinephrine-evoked hand vein constriction in healthy subjects.
Dannenberg, K; Konschak, A; Lautenschläger, C; Presek, P; Sziegoleit, W, 2007
)
0.61
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
triazolopyrimidines
[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]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency43.64860.002541.796015,848.9004AID1347395
USP1 protein, partialHomo sapiens (human)Potency39.81070.031637.5844354.8130AID504865
AR proteinHomo sapiens (human)Potency29.54660.000221.22318,912.5098AID1259243; AID1259247
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency26.11660.001022.650876.6163AID1224838; AID1224893
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency26.10720.001530.607315,848.9004AID1224848; AID1224849; AID1259403
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
mitogen-activated protein kinase 1Homo sapiens (human)Potency7.07950.039816.784239.8107AID1454
gemininHomo sapiens (human)Potency5.27680.004611.374133.4983AID624296; AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency13.78940.005612.367736.1254AID624032
lamin isoform A-delta10Homo sapiens (human)Potency0.03160.891312.067628.1838AID1487
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)627.80000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (95)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID180080Hypotensive index (HI) measured as the area under the time-hypotensive response curve for 6-h period at 30 mg/kg, po1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID231867Inhibition of bovine heart phosphodiesterase1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
2-(Alkylthio)-1,2,4-triazolo[1,5-a]pyrimidines as adenosine cyclic 3',5'-monophosphate phosphodiesterase inhibitors with potential as new cardiovascular agents.
AID77136Integrated vasodilating potency (IVP) (the product of compound-induced maximum percent decrease in the perfusion pressure and the duration of the effect in minutes at 100 ug (ia))1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID61751Maximum percent decrease in mean blood pressure in anesthetized dogs after intravenous administration at 3 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID62981Increase in coronary blood flow in anesthetized dogs was measured after intravenous administration of 3 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID61750Maximum percent decrease in mean blood pressure in anesthetized dogs after intravenous administration at 0.3 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID62101Percent increase in coronary blood flow in anesthetized dogs after intravenous administration at 1.0 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID62100Percent increase in coronary blood flow in anesthetized dogs after intravenous administration at 0.3 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID61921Time taken for increase in coronary blood flow in anesthetized dogs after intravenous administration at 0.3 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID62980Increase in coronary blood flow in anesthetized dogs was measured after intravenous administration of 1 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID62102Percent increase in coronary blood flow in anesthetized dogs after intravenous administration at 3 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID61923Time taken for increase in coronary blood flow in anesthetized dogs after intravenous administration at 3 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID61749Maximum percent decrease in mean blood pressure in anesthetized dogs after intravenous administration at 0.1 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID61922Time taken for increase in coronary blood flow in anesthetized dogs after intravenous administration at 1 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID62979Increase in coronary blood flow in anesthetized dogs was measured after intravenous administration of 0.3 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (284)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990123 (43.31)18.7374
1990's78 (27.46)18.2507
2000's46 (16.20)29.6817
2010's27 (9.51)24.3611
2020's10 (3.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.26

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 Index31.26 (24.57)
Research Supply Index5.78 (2.92)
Research Growth Index4.26 (4.65)
Search Engine Demand Index42.51 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials25 (8.36%)5.53%
Reviews14 (4.68%)6.00%
Case Studies2 (0.67%)4.05%
Observational0 (0.00%)0.25%
Other258 (86.29%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
OCT Evaluation of Stent Struts Re-endothelization in Patients With Acute Coronary Syndromes: a Comparison of the Intrepide™ Stent vs. Taxus™ [NCT00914420]Phase 440 participants (Anticipated)Interventional2009-06-30Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]