Page last updated: 2024-12-04

pyrrolidonecarboxylic acid

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Pyrrolidonecarboxylic Acid: A cyclized derivative of L-GLUTAMIC ACID. Elevated blood levels may be associated with problems of GLUTAMINE or GLUTATHIONE metabolism. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

5-oxo-L-proline : An optically active form of 5-oxoproline having L-configuration. [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]

oxoproline : A pyrrolidinemonocarboxylic acid consisting of proline bearing a single oxo substituent. [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 CID7405
CHEMBL ID397976
CHEBI ID18183
SCHEMBL ID15790
MeSH IDM0018279
PubMed CID499
CHEMBL ID284718
CHEBI ID16010
SCHEMBL ID15791
MeSH IDM0018279

Synonyms (243)

Synonym
AC-15173
CHEBI:18183 ,
(-)-2-pyrrolidone-5-carboxylic acid
(s)-pyroglutamic acid
(s)-(-)-2-pyrrolidone-5-carboxylic acid
(2s)-5-oxopyrrolidine-2-carboxylic acid
nsc-11742
nsc9966 ,
nsc-9966
nsc11742
pyroglutamic acid, (l)
5-carboxy-2-pyrrolidinone
pyrrolidone-5-carboxylic acid
l-glutamic acid gamma-lactam
einecs 202-700-3
2-l-pyrrolidone-5-carboxylic acid
2-pyrrolidone-5-carboxylate
(s)-5-oxo-2-pyrrolidinecarboxylic acid
l-proline, 5-oxo-
2-pyrrolidinone-5-carboxylic acid
l-glutimic acid
l-pyrrolidinonecarboxylic acid
proline, 5-oxo-, l-
acide pidolique [inn-french]
l-2-pyrrolidone-5-carboxylic acid
5-pyrrolidinone-2-carboxylic acid
ajidew a-100
l-5-oxoproline
(5s)-2-oxopyrrolidine-5-carboxylic acid
l-pyrrolidonecarboxylic acid
l-5-oxo-2-pyrrolidinecarboxylic acid
pyrrolidonecarboxylic acid
l-5-carboxy-2-pyrrolidinone
nsc 143034
acidum pidolicum [inn-latin]
acido pidolico [inn-spanish]
l-glutiminic acid
pidolic acid [inn]
2-oxopyrrolidine-5-carboxylic acid
glutiminic acid
proline, 5-oxo-
2-benzothiazolesulfenic acid morpholide
pyrrolidinonecarboxylic acid
nsc 9966
pidolic acid
pyroglutamate
l-pyroglutamic acid
5-pyrrolidone-2-carboxylic acid
pyroglutamic acid
98-79-3
5-oxo-l-proline
l-5-pyrrolidone-2-carboxylic acid
5-oxoproline ,
C01879
nsc-143034
l-pyroglutamic acid, 97%
l-pyroglutamic acid, bioxtra
l-pyrrolidone carboxylic acid
glutimic acid
NCGC00160613-01
5-l-oxoproline
DB03088
P-8490
MLS001332421
smr000857158
MLS001332422
l-pyroglutamate
l-pyroglutamic acid, >=99.0% (t)
E478F48D-E369-43AE-8132-08D819242518
l-pca
pidolidone
pyroglutamic acid, l-
nsc-760414
CHEMBL397976
(s)-2-pyrrolidone-5-carboxylic acid
(s)-5-oxopyrrolidine-2-carboxylic acid
P0573
h-pyr-oh
l-glutamic acid lactam
pyroglu
A845910
HMS3264E20
M03204
cas-98-79-3
dtxsid6046260 ,
dtxcid4026260
tox21_111936
pharmakon1600-01506185
nsc760414
HMS2231L11
CCG-36432
szb83o1w42 ,
unii-szb83o1w42
pidolic acid [inn:ban]
acide pidolique
oxo-proline
acidum pidolicum
pidolate
acido pidolico
BP-12844
pidolic acid [who-dd]
l-pyroglutamic acid [mi]
pyroglutamic acid [usp-rs]
pca [inci]
AKOS015855330
S5823
CS-M0659
AM83732
SCHEMBL15790
NCGC00160613-02
tox21_111936_1
(s)-5-oxo-pyrrolidine-2-carboxylic acid
pglu
l-pyro-glutamic acid
(s)-5-oxopyrolidine-2-carboxylic acid
(l)-pyroglutamic acid
(2s)-5-pyrrolidone-2-carboxylic acid
pglu-oh
pyr-oh
(s)-(-)-pyroglutamic acid
F8889-8712
l-glutamic acid .gamma.-lactam
(5s)-2-xopyrrolidine-5-carboxylic acid
AB00514366_07
mfcd00005272
(s)-(-)-2-pyrrolidinone-5-carboxylic acid
pyroglutamic acid, united states pharmacopeia (usp) reference standard
P17107
pidolic acid, european pharmacopoeia (ep) reference standard
(-)-2-pyrrolidone-5-carboxylate
(s)-pyroglutamate
pyrrolidinonecarboxylate
pyrrolidone-5-carboxylate
l-pyrrolidinonecarboxylate
l-glutiminate
oxopyrrolidinecarboxylic acid
(-)-pyroglutamate
ajidew a 100
(s)-5-oxo-2-pyrrolidinecarboxylate
(s)-(-)-g-butyrolactam-g-carboxylic acid
2-oxopyrrolidine-5(s)-carboxylate
l-2-pyrrolidone-5-carboxylate
l-glutimate
l-5-oxo-2-pyrrolidinecarboxylate
l-pyrrolidonecarboxylate
5-pyrrolidinone-2-carboxylate
(s)-2-pyrrolidone-5-carboxylate
(s)-(-)-gamma-butyrolactam-gamma-carboxylic acid
2-l-pyrrolidone-5-carboxylate
glutiminate
(5s)-2-oxopyrrolidine-5-carboxylate
glutimate
2-oxopyrrolidine-5(s)-carboxylic acid
(s)-(-)-g-butyrolactam-g-carboxylate
(-)-pyroglutamic acid
oxopyrrolidinecarboxylate
(s)-(-)-2-pyrrolidone-5-carboxylate
(s)-(-)-gamma-butyrolactam-gamma-carboxylate
l-glutamic acid g-lactam
2-pyrrolidinone-5-carboxylate
HY-76082
pyrrolidone car-boxylic acid
Q60998677
rec-pga 273k
EN300-72896
STR02331
pidolic-acid
GEO-04256
Z1154378309
BB 0241896
5-oxo-dl-proline
2-pyrrolidone-5-carboxylic acid
GLP ,
CHEBI:16010 ,
dl-pyroglutamic acid
149-87-1
nsc-40887
dl-proline, 5-oxo-
nsc40887
5-oxopyrrolidine-2-carboxylic acid
oxoproline
16891-48-8
nsc143034
5-oxo-2-pyrrolidinecarboxylic acid
STK290904
2-pyrrolidone-5-carboxylic acid, 99%
smr000112493
MLS001304098
2027729E-091C-4F23-87AA-2D40D8A5C67C
CHEMBL284718
h-dl-pyr-oh
G0061
dl-glutamic acid lactam
AKOS000119789
A808971
5-oxopyrrolidine-2-carboxylic acid;dl-pyroglutamic acid
6vt1yzm21h ,
nsc 40887
einecs 205-748-3
unii-6vt1yzm21h
dl-pidolic acid
BBL011576
HMS2269D08
FT-0605097
FT-0628008
FT-0613406
AM20080373
pyroglutamic acid, dl-
pidolic acid, dl-
(+/-)-pyroglutamic acid
proline, 5-oxo-, dl-
(+/-)-2-pyrrolidone-5-carboxylic acid
dl-pyrrolidonecarboxylic acid
dl-2-pyrrolidinone-5-carboxylic acid
dl-2-pyrrolidone-5-carboxylic acid
AKOS016338215
gtpl4703
HMS3372F13
AB00443776-07
SCHEMBL15791
SY002490
PS-6138
d,l-pyroglutamic acid
5-oxo-pyrrolidine-2-carboxylic acid
NCGC00263467-03
Q-100175
dl-5-oxoproline
5-oxoproline #
mfcd00064322
F2190-0001
sr-01000830710
SR-01000830710-3
2-pyrrolidone-5-carboxylicacid
CS-W013454
DTXSID80859174
Q27887010
D77751
dl-pyroglutamicacid
PB42767
HY-W012738
proline-2,3,3,4,4-d5,5-oxo- (9ci)
EN300-19515
Z104474096

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Administration of a toxic dose of precocene II (175 mg/kg) to male Sprague-Dawley rats rapidly depleted hepatic GSH, produced histopathological changes in the liver, and induced increases in serum aminotransferase activity."( Alteration of precocene II-induced hepatotoxicity by modulation of hepatic glutathione levels.
Duddy, SK; Hsia, MT, 1989
)
0.28
"Hymenoxon and helenalin are toxic sesquiterpene lactones present in the toxic range plants Hymenoxys odorata and Helenium microcephalum."( Role of glutathione in the toxicity of the sesquiterpene lactones hymenoxon and helenalin.
Hayes, MA; Kim, HL; Merrill, JC; Murray, CA; Safe, S, 1988
)
0.27
" In this investigation, we have found that sensitivity to CHCl3 correlates with the capacity of the kidney to metabolize CHCl3 to the toxic metabolite phosgene (COCl2)."( Strain and sex differences in chloroform-induced nephrotoxicity. Different rates of metabolism of chloroform to phosgene by the mouse kidney.
George, JW; Pohl, LR; Satoh, H,
)
0.13
" Pretreatment with phenobarbital enhanced the toxic response of renal cortical slices to CHCl3 in vitro as indicated by decreased p-aminohippurate and tetraethylammonium accumulation."( Mechanism of chloroform nephrotoxicity. IV. Phenobarbital potentiation of in vitro chloroform metabolism and toxicity in rabbit kidneys.
Bailie, MB; Hook, JB; Newton, JF; Smith, JH, 1984
)
0.27
" Two groups could be distinguished: PMA, EMT and MMC are one order of magnitude more toxic than MC, MN and MA."( Cytotoxicity of mercury compounds in LLC-PK1, MDCK and human proximal tubular cells.
Bohets, HH; D'Haese, PC; De Broe, ME; Dierickx, PJ; Nouwen, EJ; Van der Biest, I; Van Landeghem, GF; Van Thielen, MN, 1995
)
0.29
" Spermine proved highly toxic and growth rates were reduced compared with controls when even ."( Toxicity and growth-promoting potential of spermine when fed to chicks.
Smith, TK; Sousadias, MG, 1995
)
0.29
" No adverse effects have been noted from continuous infusions of the peptide."( Reduction in the duration of myelotoxicity associated with radioimmunotherapy with infusions of the hemoregulatory peptide, HP5b in mice.
Alisauskas, RM; Blumenthal, RD; Goldenberg, DM; Sharkey, RM, 1997
)
0.3
"Amino acids (AA) which were proposed as an alternative osmotically active agents in dialysates are toxic to human peritoneal mesothelial cells (HPMC) due to disturbance of the antioxidant-oxidant balance in cells by reducing level of glutathione."( In vitro effect of glutathione precursors on cytotoxicity of amino acids to human mesothelial cells.
Grzybowski, AE, 1999
)
0.3
"No significant toxic effect was observed in the 400 mg/kg group."( [Reproductive toxicity of metadoxine in rats].
Chen, JG; Lai, WQ; Mei, S; Wang, Y; Zhang, WY; Zhang, X; Zhu, HJ, 2003
)
0.32
" Because OTZ reduced the toxic effects of GDP on mesothelial cells, this compound may improve biocompatibility of peritoneal dialysis fluids."( L-2-oxothiazolidine-4-carboxylic acid reduces in vitro cytotoxicity of glucose degradation products.
Breborowicz, A; Oreopoulos, D; Polubinska, A; Pyda, M; Witowski, J, 2004
)
0.32
" Prolonged exposure to 10 microM 3Me-H TRH was not toxic to the cells, whereas neurons exposed to 500 microM Glu resulted in maximal cell death."( An analog of thyrotropin-releasing hormone (TRH) is neuroprotective against glutamate-induced toxicity in fetal rat hippocampal neurons in vitro.
Jackson, J; Kubek, MJ; Lahiri, DK; Veronesi, MC; Yard, M, 2007
)
0.34
" Cytotoxicity and cell proliferation assays were performed to elucidate the adverse effects of formaldehyde on U2OS cells."( Cytotoxicity of formaldehyde on human osteoblastic cells is related to intracellular glutathione levels.
Chang, YC; Ho, YC; Huang, FM, 2007
)
0.34
"Cytotoxicity, cell proliferation and collagen synthesis assays were performed to elucidate the toxic effects of CHX on the human osteoblastic cell line U2OS."( Cytotoxicity of chlorhexidine on human osteoblastic cells is related to intracellular glutathione levels.
Chang, YC; Chou, MY; Hu, CC; Lee, SS; Lee, TH, 2010
)
0.36
" Metadoxine ER was generally well tolerated, with nausea (17% [10/58] vs 0% [0/59]), fatigue (31% [18/58] vs 27% [16/59]), and headaches (29% [17/58] vs 39% [23/59]) being the most frequently reported adverse effects for the metadoxine ER and placebo groups, respectively."( A randomized, double-blind, placebo-controlled, multicenter study evaluating the efficacy, safety, and tolerability of extended-release metadoxine in adults with attention-deficit/hyperactivity disorder.
Adler, LA; Aharon-Peretz, J; Ben-Hayun, R; Biederman, J; Daniely, Y; Manor, I; Megiddo, D; Newcorn, JH; Salomy, D; Weizman, A, 2012
)
0.38
"Plants detoxify toxic metals through a GSH-dependent pathway."( A γ-glutamyl cyclotransferase protects Arabidopsis plants from heavy metal toxicity by recycling glutamate to maintain glutathione homeostasis.
Chhikara, S; Coomey, J; Dhankher, OP; Jung, HI; Paulose, B; Vatamaniuk, O, 2013
)
0.39
" The Panel concluded that PCA and its salts are safe in cosmetics in the present practices of use and concentration; additionally, these ingredients should not be used in cosmetic products in which N-nitroso compounds can be formed."( Safety Assessment of PCA (2-Pyrrolidone-5-Carboxylic Acid) and Its Salts as Used in Cosmetics.
Belsito, DV; Bergfeld, WF; Fiume, MM; Gill, LJ; Heldreth, B; Hill, RA; Klaassen, CD; Liebler, DC; Marks, JG; Shank, RC; Slaga, TJ; Snyder, PW,
)
0.13
" At each follow-up visit, peak expiratory flow (PEF) and asthma symptom score and medicine adverse effects were recorded."( Efficacy and Safety of Pidotimod in Persistent Asthma: A Randomized Triple-Blinded Placebo-Controlled Trial.
Deglurkar, R; Mathew, JL; Singh, M, 2022
)
0.72
" Secondary outcomes were PEF at each follow-up visit, asthma symptom score at each visit, change in asthma symptom score at 12 weeks, and adverse event profile."( Efficacy and Safety of Pidotimod in Persistent Asthma: A Randomized Triple-Blinded Placebo-Controlled Trial.
Deglurkar, R; Mathew, JL; Singh, M, 2022
)
0.72
" There were no significant adverse effects observed."( Efficacy and Safety of Pidotimod in Persistent Asthma: A Randomized Triple-Blinded Placebo-Controlled Trial.
Deglurkar, R; Mathew, JL; Singh, M, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" After a 60- to 90-min infusion of the appropriate peptide into rats, the MCR, half-life of disappearance (t 1/2), and volume of distribution were calculated."( The pharmacokinetics of thyrotropin-releasing hormone (TRH) and deamido-TRH in the rat.
Alex, S; Emerson, CH; Matys, R; Safran, M; Wu, CF, 1984
)
0.27
"The pharmacokinetic studies on pidotimod ((R)-3-[(S)-(5-oxo-2-pyrrolidinyl) carbonyl]-thiazolidine-4-carboxylic acid, PGT/1A, CAS 121808-62-6) a new biological response modifier, following intravenous, intramuscular or oral administrations in rats and dogs are reported in this paper."( Pharmacokinetics of pidotimod in rats and dogs.
Coppi, G; Silingardi, S, 1994
)
0.29
"Pidotimod ((R)-3-[(S)-(5-oxo-2-pyrrolidinyl) carbonyl]-thiazolidine-4-carboxylic acid, PGT/1A, CAS 121808-62-6), a new biological response modifier, was investigated in 3 different pharmacokinetic experiments in healthy volunteers."( Pharmacokinetics and oral bioavailability of pidotimod in humans.
Coppi, G; Mailland, F; Silingardi, S, 1994
)
0.29
" No differences in absorption, excretion and pharmacokinetic parameters was evident between old volunteers and the youngs of a previous work."( Pharmacokinetics of pidotimod in elderly volunteers and in renal failure patients.
Biffi, M; Coppi, G; Mailland, F; Silingardi, S; Spotti, D, 1994
)
0.29
"In 13 subjects with ALS, we studied the safety and pharmacokinetic properties of Procysteine, a cysteine prodrug that increases levels of intracellular glutathione."( The pharmacokinetics and pharmaco-dynamics of Procysteine in amyotrophic lateral sclerosis.
Brown, RH; Cudkowicz, ME; Ellis, T; Gwilt, PR; Hayden, DL; Sexton, PM; Whalen, J, 1999
)
0.3
"A selective, rapid and sensitive high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed for the first time to determine pidotimod in human plasma and applied to a pharmacokinetic study."( High-performance liquid chromatography-tandem mass spectrometry for the determination of pidotimod in human plasma and its application to a pharmacokinetic study.
Li, F; Liu, W; Lu, S; Qin, F; Xiong, Z; Zhang, Y, 2009
)
0.35
"A selective, rapid and sensitive hydrophilic interaction liquid chromatography-tandem mass spectrometry (HILIC-MS/MS) method was developed for the first time to determine adefovir in human plasma and applied to a pharmacokinetic study."( Hydrophilic interaction liquid chromatography-tandem mass spectrometry for the determination of adefovir in human plasma and its application to a pharmacokinetic study.
Li, F; Qin, F; Qin, T; Xiong, Z; Yang, S; Zhang, Y, 2010
)
0.36
"This study was aimed at exploring the accuracy of population pharmacokinetic method in evaluating the bioequivalence of pidotimod with sparse data profiles and whether this method is suitable for bioequivalence evaluation in special populations such as children with fewer samplings."( Advantage of population pharmacokinetic method for evaluating the bioequivalence and accuracy of parameter estimation of pidotimod.
Chen, J; He, Y; Huang, J; Li, M; Lv, Y; Wang, J; Wang, K; Xu, L; Yang, J; Zheng, Q, 2016
)
0.43
"The 90% confidence intervals (CIs) for AUC0-12h, AUC0-∞, and Cmax were 97."( Advantage of population pharmacokinetic method for evaluating the bioequivalence and accuracy of parameter estimation of pidotimod.
Chen, J; He, Y; Huang, J; Li, M; Lv, Y; Wang, J; Wang, K; Xu, L; Yang, J; Zheng, Q, 2016
)
0.43
"The population pharmacokinetic modeling method was used to assess the bioequivalence of two pidotimod formulations with relatively few sampling points and further validated the bioequivalence of the two formulations."( Advantage of population pharmacokinetic method for evaluating the bioequivalence and accuracy of parameter estimation of pidotimod.
Chen, J; He, Y; Huang, J; Li, M; Lv, Y; Wang, J; Wang, K; Xu, L; Yang, J; Zheng, Q, 2016
)
0.43

Compound-Compound Interactions

ExcerptReferenceRelevance
" The drug did not show antimicrobial or antifungal activities nor interact with some of the most common therapeutics (antibiotics, tolbutamide, pentobarbital, antihypertensives, chlorothiazide, warfarin, non-steroidal antiinflammatory agents)."( General pharmacology of pidotimod and testing for drug interactions.
Coppi, G; Falcone, A; Ieva, G; Manzardo, S; Pinzetta, A, 1994
)
0.29
" The MTD for magnesium pidolate used in combination with hydroxycarbamide was 125 mg/kg/d."( Phase I study of magnesium pidolate in combination with hydroxycarbamide for children with sickle cell anaemia.
Brugnara, C; Hankins, JS; Hillery, CA; Li, CS; Wang, WC; Wynn, LW, 2008
)
0.35
" Under these conditions, an antiischemic drug combination produced a pronounced but short increase in the local circulation in cortex of cerebrum (decreased by hemorrhagic stroke), with the subsequent decrease in the local flow."( [Effects of an antiischemic drug combination and nimodipine on cerebral blood supply in a hemorrhagic stroke model in rats].
Bero, RS; Gan'shina, TS; Kurdiumov, IN; Mirzoian, NR,
)
0.13
"To gain new insight into the functional interaction between dendritic cells and methionine encephalin (MENK) combined with pidotimod (PTD), we have analyzed the effect of MENK plus PTD on the morphology, phenotype and functions of murine bone-marrow derived dendritic cells (BMDCs) in vitro."( Synergistic effect of methionine encephalin (MENK) combined with pidotimod(PTD) on the maturation of murine dendritic cells (DCs).
Meng, Y; Plotnikoff, NP; Shan, F; Wang, E; Wang, Q; Zhang, Z, 2013
)
0.39

Bioavailability

ExcerptReferenceRelevance
"Experiments were conducted to: (a) compare the bioavailability of betamethasone benzoate in a quick-break aerosol foam and semisolid dosage forms, (b) compare the activity of betamethasone benzoate, betamethasone valerate, clobetasol propionate, triamcinolone acetonide, desonide, flumethasoid reservoir formation in skin, and (d) assess the effect of a natural moisturizer."( Bioavailability and activity of topical corticosteroids from a novel drug delivery system, the aerosol quick-break foam.
Barry, BW; Woodford, R, 1977
)
0.26
" Over 60% of the cerebral radioactivity was present as [3H]pyroglutamate demonstrating that pyroglutamate is not only well absorbed but also penetrates in significant amounts into the brain."( Brain penetration of orally administered sodium pyroglutamate.
Audran, M; Briley, M; Chanal, JL; Sicard, MT, 1988
)
0.27
"To assess directly the effect of ionic dissociation on the bioavailability of calcium, we used the double isotope inverse convolution method to compare the absorption of calcium gluconate and calcium pyrrolidone carboxylate, an organic, highly dissociated salt."( Influence of accompanying anion on intestinal radiocalcium absorption.
Duquesnoy, B; Gilquin, B; Marchandise, X; Pagniez, D; Wemeau, JL; Ythier, H, 1987
)
0.27
" It is concluded that the increased potency in neuropharmacological tests results from enhanced bioavailability to CNS sites and that a similar rationale can be used to explain the CNS selectively claimed in the literature for other analogues of TRH."( Thyrotropin-releasing hormone (TRH) analogues show enhanced CNS selectivity because of increased biological stability.
Brewster, D; Dettmar, PW; Havler, ME; Lynn, AG; Metcalf, G, 1981
)
0.26
" Bioavailability was 100% in the intramuscular route and 27% in the oral route."( Pharmacokinetics of pidotimod in rats and dogs.
Coppi, G; Silingardi, S, 1994
)
0.29
" The intake of a standard meal before pidotimod administration, either as sachet or as ampoule, reduced the bioavailability of the drug, probably due to an interference at the absorption level."( Effect of food on the bioavailability of pidotimod in healthy volunteers.
Caravaggi, M; Crema, A; Crema, F; D'Angelo, L; De Ponti, F, 1994
)
0.29
" These results taken together with hydrolysis and bioavailability data show that ester is a potential candidate as a prodrug of paracetamol."( Synthesis, physical properties, toxicological studies and bioavailability of L-pyroglutamic and L-glutamic acid esters of paracetamol as potentially useful prodrugs.
Bousquet, E; Marrazzo, A; Puglisi, G; Spadaro, A; Tirendi, S, 1996
)
0.29
"Several calcium supplements are currently available and many of them are marketed without proper comparison of the bioavailability of the actual preparations."( Acute changes in serum calcium and parathyroid hormone circulating levels induced by the oral intake of five currently available calcium salts in healthy male volunteers.
Albert, A; Deroisy, R; Meurmans, L; Micheletti, MC; Nelissenne, N; Reginster, JY; Zartarian, M, 1997
)
0.3
" The pharmacokinetics of pyrrolidone monitored upon its combined administration with pyroglutamic acid shows that this drug, as a component of the composition, is characterized by a high absolute bioavailability and permeability trough the blood-brain barrier."( [Correlations of pharmacokinetics and pharmacodynamics of a combined preparation containing pyrrolidone and pyroglutamic acid].
Lun'shina, EV; Mirzoian, NR; Sariev, AK; Zherdev, VP,
)
0.13
" Diminished antioxidant capacity increases vascular superoxide levels, which reduce NO bioavailability and promote peroxynitrite generation."( Vascular oxidative stress and nitric oxide depletion in HIV-1 transgenic rats are reversed by glutathione restoration.
Dikalov, S; Guidot, DM; Hart, CM; Jones, DP; Kleinhenz, DJ; Kline, ER; Liang, B; Sutliff, RL, 2008
)
0.35
"Water-in-oil-in-water (w/o/w) double emulsions are potential for enhancing oral bioavailability of drugs with high solubility and low permeability, but their industrial application is limited due to the instability."( Self-double-emulsifying drug delivery system (SDEDDS): a new way for oral delivery of drugs with high solubility and low permeability.
Hu, Z; Qi, X; Wang, L; Zhang, J; Zhu, J, 2011
)
0.37
"The aims of this study were to prepare fine pidotimod-containing water-in-oil-in-water (W/O/W) double emulsions and to investigate the possibility of those emulsions as a delivery system for promoting the oral bioavailability of pidotimod."( Water-in-oil-in-water double emulsions: an excellent delivery system for improving the oral bioavailability of pidotimod in rats.
Qi, X; Wang, L; Zhu, J, 2011
)
0.37
"The differing bioavailability of magnesium salts remains an open question, both at the cellular and systemic level."( Effects of supplementation with different Mg salts in cells: is there a clue?
Cappadone, C; Castiglioni, S; Cazzaniga, A; Farruggia, G; Iotti, S; Maier, JA; Marraccini, C; Merolle, L; Sargenti, A,
)
0.13
"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
" Among several magnesium salts available to treat magnesium deficiency, magnesium pidolate may have high bioavailability and good penetration at the intracellular level."( Headaches and Magnesium: Mechanisms, Bioavailability, Therapeutic Efficacy and Potential Advantage of Magnesium Pidolate.
Cazzaniga, A; Giacomoni, E; Maier, JA; Pellegrino, P; Pickering, G, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
"Experiments were conducted to: (a) compare the bioavailability of betamethasone benzoate in a quick-break aerosol foam and semisolid dosage forms, (b) compare the activity of betamethasone benzoate, betamethasone valerate, clobetasol propionate, triamcinolone acetonide, desonide, flumethasoid reservoir formation in skin, and (d) assess the effect of a natural moisturizer."( Bioavailability and activity of topical corticosteroids from a novel drug delivery system, the aerosol quick-break foam.
Barry, BW; Woodford, R, 1977
)
0.26
" The amide free peptide pyroglutamylglutamylglycylserylaspartic acid which inhibited the tumor growth in all the models showed a curvilinear dose-response relationship with a maximal effect at 1000 pmol/animal in mice and at 100 pmol/animal in rats."( The synthetic hepatic peptides pyroglutamylglutamylglycylserylasparagine and pyroglutamylglutamylglycylserylaspartic acid inhibit growth of MH1C1 rat hepatoma cells transplanted into Buffalo rats or athymic mice.
Elgjo, K; Hall, KS; Paulsen, JE; Reichelt, KL; Rugstad, HE, 1992
)
0.28
" Both the biological peptide isolated from mouse liver and the synthetic homolog showed bell-shaped dose-response curves."( The peptide pyroGlu-Gln-Gly-Ser-Asn, isolated from mouse liver, inhibits growth of rat hepatoma cells in vitro.
Elgjo, K; Endresen, L; Paulsen, JE; Reichelt, KL; Rugstad, HE; Sundby-Hall, K, 1991
)
0.28
" sexta was gained by comparing the dose-response curves for synthetic Manduca AKH with curves from gland extracts."( Biological effects of synthetic AKH in Manduca sexta and estimates of the amount of AKH in corpora cardiaca.
Ziegler, R, 1990
)
0.28
" with 950 mg/kg of OTC 4 hours before dosing with 5-FU."( Effects of L-2-oxothiazolidine-4-carboxylate, a cysteine pro-drug, on teratogenicity of 5-fluorouracil in mice.
Deguchi, T; Mataki, Y; Naya, M; Noguchi, M; Yasuda, M, 1990
)
0.28
" CMI showed a bell-shaped dose-response relationship as previously shown, whereas the mitotic rate was not reduced in the colonic epithelium after treatment with either an epidermal mitosis inhibitory pentapeptide, or the dipeptide pGlu-GlyOH, or an analogue of luteinizing hormone-releasing hormone."( Further studies on the biological characteristics of an endogenous colon mitosis inhibitor: comparison with some structurally related peptides.
Reichelt, KL; Skraastad, O, 1989
)
0.28
" The dose-response relationship was bell-shaped with loss of inhibitory effect at high or low doses."( An endogenous colon mitosis inhibitor reduces proliferation of colon carcinoma cells (HT 29) in serum-restricted medium.
Reichelt, KL; Skraastad, O, 1989
)
0.28
" Dose-response studies revealed that the gastric acid secretion induced by submaximal but not high doses of RX 77368 was elevated significantly by p-CPA pretreatment."( Serotonin depletion potentiates gastric secretory and motor responses to vagal but not peripheral gastric stimulants.
Garrick, T; Stephens, RL; Taché, Y; Weiner, H, 1989
)
0.28
" A dose-response experiment indicated that 20 microM ascorbate was capable of producing 50% of the maximum observable increase in culture TRH immunoactivity; this concentration is similar to the Km value for ascorbate uptake obtained in adrenal chromaffin and pituitary cells."( Ascorbic acid increases the thyrotropin-releasing hormone content of hypothalamic cell cultures.
Gibson, TR; Glombotski, CC; Manaker, S; Winokur, A, 1986
)
0.27
" A similar order of potency in increasing plasma TSH (Analogue I greater than TRH greater than Analogue II) was found in vivo, as shown by dose-response curves."( In vitro and in vivo TSH releasing activity of two new analogues of TRH.
Astier, H; Klingler, W; Roussel, JP; Tapia-Arancibia, L, 1987
)
0.27
"Thyrotrophin-releasing hormone (TRH) occurs in high concentrations in the rat ventral prostate and its concentrations is regulated in a positive dose-response manner by testosterone in castrated rats."( Thyroid hormone modulation of thyrotrophin-releasing hormone (TRH) and TRH-Gly levels in the male rat reproductive system.
Bhasin, S; Hershman, JM; Pekary, AE; Smith, V; Sugawara, M; Swerdloff, RS, 1987
)
0.27
" Dose-response curves revealed that adult animals were more than 10-fold less sensitive to NMDA than their younger counterparts."( Characterization and possible opioid modulation of N-methyl-D-aspartic acid induced increases in serum luteinizing hormone levels in the developing male rat.
Bell, RD; Cicero, TJ; Meyer, ER, 1988
)
0.27
" Most importantly, however, we showed that the GPT-LHRH produced equivalent, parallel shifts to the right in the dose-response curves for LHRH and naloxone, indicative of competitive inhibition."( Luteinizing hormone releasing hormone mediates naloxone's effects on serum luteinizing hormone levels in normal and morphine-sensitized male rats.
Cicero, TJ; Meyer, ER; Miller, BT; Schmoeker, PF, 1985
)
0.27
" The dose-response curves for these long term effects on hormone synthesis were similar to the dose-response curves for the first phase of release."( Thyrotropin-releasing hormone rapidly stimulates a biphasic secretion of prolactin and growth hormone in GH4C1 rat pituitary tumor cells.
Aizawa, T; Hinkle, PM, 1985
)
0.27
" N-Acetyl-L-cysteine, L-2-oxothiazolidine-4-carboxylate or the L- or D-isomers of 2-methylthiazolidine-4-carboxylate were administered to male mice immediately after a hepatotoxic dosage of acetaminophen (5."( Effects of cysteine pro-drugs on acetaminophen-induced hepatotoxicity.
Hazelton, GA; Hjelle, JJ; Klaassen, CD, 1986
)
0.27
" In rats the compound caused release of prolactin but the dose-response relationship was bi-phasic, so that large doses caused only a diminished response."( The ability of RX 77368 - a stabilised analogue of TRH - to provoke the secretion of prolactin and TSH in vivo.
Clifford, JM; Dettmar, PW; Lynn, AG; Metcalf, G, 1982
)
0.26
" SR 48968 (10(-6) M shifted the [Pro9]SP dose-response curve but did not modify the septide dose-response curve."( Involvement of septide-sensitive tachykinin receptors in inositol phospholipid hydrolysis in the rat urinary bladder.
Beaujouan, JC; Glowinski, J; Saffroy, M; Torrens, Y, 1995
)
0.29
" The dose-response curves of myotropic and non-myotropic factors indicate that (i) proctolin, L-glutamate, octopamine, leucokinin-VI, leucopyrokinin, ecdysone and 20-hydroxy-ecdysone, or equivalent structures, might be involved in Galleria mellonella oviposition control, and (ii) that only the novel wax moth neuropeptide has the ability to trigger egg laying in that insect."( Separation of oviposition-stimulating peptides and myotropic factors from head extracts of Galleria mellonella L.: comparative effects of myotropic and non-myotropic factors on egg laying.
Abdoun, K; Baudry-Partiaoglou, N; Cohen, P; Mesnier-Sabin, M; Nicolas, P, 1995
)
0.29
"5 times the maximum dosage intended for clinical use."( Toxicological evaluation of pidotimod.
Amico-Roxas, M; Bertè, F; Bussi, R; Coppi, G; Gnemi, P; Harling, RJ; Mailland, F; Manzardo, S; Massey, JE; Spencer-Briggs, DJ, 1994
)
0.29
" During the first 8-day phase (D0-D8), 68 patients received 800 mg pidotimod orally (one sachet) twice daily and an antibiotic treatment (amoxycillin plus clavulanic acid: 1 g twice daily), while 69 patients received placebo (one sachet) and antibiotic according to the same dosage schedule."( Pidotimod in the treatment of patients affected by bacterial exacerbations of chronic bronchitis.
Cirianni, C; Dolcetti, A; Fugazza, L; Moreo, G; Orlandi, O; Piacenza, G; Pozzi, E; Rampulla, C; Scarpazza, G, 1994
)
0.29
" Increases in whole-blood glutathione were observed in the highest dosage group after 6 weeks of therapy."( A phase I/II trial of intravenous L-2-oxothiazolidine-4-carboxylic acid (procysteine) in asymptomatic HIV-infected subjects.
Borum, PR; Chance, M; Emgushov, RT; Jackson, JB; Kalayjian, RC; Mayer, KH; Skowron, G; Spell, SA; Webb, LS; Yen-Lieberman, B, 1994
)
0.29
" A bell-shaped dose-response curve with maximal effect at 1 pmol/animal/injection was seen."( The synthetic colon peptide pyroGlu-His-GlyOH inhibits growth of human colon carcinoma cells (HT-29) transplanted subcutaneously into athymic mice.
Paulsen, JE, 1993
)
0.29
" In one study, acute high dosage survivorship was compared for approximately equimolar cysteine dosages of L-cysteine and Procysteine."( Toxicity evaluations of L-cysteine and Procysteine, a cysteine prodrug, given once intravenously to neonatal rats.
Glosson, JA; Goldberg, DI; Madsen, DC; Rowe, WB; White, RD; Wilson, DM, 1993
)
0.29
" This unusually high concentration of 5OXP in the urine and its prevention by methionine indicates that chronic high level paracetamol dosing leads to severe depletion of sulphur-containing amino acids including cysteine with consequent disruption of the glutathione cycle."( Induction of 5-oxoprolinuria in the rat following chronic feeding with N-acetyl 4-aminophenol (paracetamol).
Beales, D; Ghauri, FY; McLean, AE; Nicholson, JK; Wilson, ID, 1993
)
0.29
" Further studies are needed to investigate optimal dosage scheme, mechanism of action, and interference with anti-tumor activity and prevention of long-term side effects of cyclophosphamide."( Protective effects of L-2-oxothiazolidine-4-carboxylate treatment on cyclophosphamide-induced cystitis in rats.
Gordon, D; Leaf, C; Rice, D; Safron, J; White, R, 1997
)
0.3
" Dose-response curves to the hormone were determined in the absence and in the presence of several drugs that affect sequential steps of the Ca(2+)-dependent signalling pathway."( Cellular signalling of PCH-induced pigment aggregation in the crustacean Macrobrachium potiuna erythrophores.
Castrucci, AM; da Silva, MA; Josefsson, L; Nery, LE, 1997
)
0.3
"A randomized double-blind, placebo-controlled study was conducted in 37 asymptomatic HIV-infected individuals (mean CD4 count 707 cells/mm3) to characterize the safety, pharmacokinetics, and effect on blood thiols of three dosage levels of a cysteine prodrug, L-2-oxothiazolidine-4-carboxylic acid (OTC; Procysteine; Clintec Technologies, Deerfield, IL)."( A phase I/II evaluation of oral L-2-oxothiazolidine-4-carboxylic acid in asymptomatic patients infected with human immunodeficiency virus.
Barditch-Crovo, P; Borum, P; Buier, R; Goldberg, D; Kalayjian, RC; Lederman, M; Lietman, P; Noe, D; Rowe, WB; Skowron, G, 1998
)
0.3
" increasing dose intensity, and 4) the possibility of using preclinical data to optimize the frequency of dosing in patient trials."( Myelosuppressive changes from single or repeated doses of radioantibody therapy: effect of bone marrow transplantation, cytokines, and hematopoietic suppression.
Alisauskas, R; Blumenthal, RD; Goldenberg, DM; Lew, W; Sharkey, RM, 1998
)
0.3
" Procysteine enters CSF after both IV and oral dosing and accumulates to significant levels in CSF."( The pharmacokinetics and pharmaco-dynamics of Procysteine in amyotrophic lateral sclerosis.
Brown, RH; Cudkowicz, ME; Ellis, T; Gwilt, PR; Hayden, DL; Sexton, PM; Whalen, J, 1999
)
0.3
" In massed training, which led to lower levels of learning as compared with spaced training, the dipeptide improved contextual memory, while in spaced training, which led to higher initial learning levels, dosage with dipeptide improved reproduction of the habit."( Modulation of long-term memory by delayed administration of the amide of L-pyroglutamyl-D-alanine, a nootropic agent, in spaced and massed training in rats.
Anokhin, KV; Gudasheva, TA; Ostrovskaya, RU; Vysotskii, AL; Vysotskii, DL,
)
0.13
" Dose-response curves showed that septide was a more potent bronchoconstrictor than [Sar(9),Met(O(2))(11)]SP to cause bronchoconstriction."( Role of nitric oxide and septide-insensitive NK(1) receptors in bronchoconstriction induced by aerosolised neurokinin A in guinea-pigs.
Amadesi, S; Bertrand, C; Geppetti, P; Nadel, JA; Ricciardolo, FL; Trevisani, M, 2000
)
0.31
" This peptide is over 20,000 times less potent than Lom-AKH-III in the in vitro assay, and also results in an unusual dose-response curve in the in vivo assay."( Potencies of naturally-occurring AKH/RPCH peptides in Locusta migratoria in the acetate uptake assay in vitro and comparison with their potencies in the lipid mobilisation assay in vivo.
Gäde, G; Goldsworthy, GJ; Kellner, R; Lee, MJ, 2000
)
0.31
" We then investigated antagonism between second messengers: dose-response curves were constructed for stimulation of Tenebrio molitor tubules by cyclic AMP and their inhibition by cyclic GMP."( Antagonistic control of fluid secretion by the Malpighian tubules of Tenebrio molitor: effects of diuretic and antidiuretic peptides and their second messengers.
Eigenheer, RA; Nicolson, SW; Schooley, DA; Wiehart, UI, 2002
)
0.31
" The dosage of 1 600 mg/kg caused significant paralysis of hind legs, emaciation, and reduced weight gain."( [Reproductive toxicity of metadoxine in rats].
Chen, JG; Lai, WQ; Mei, S; Wang, Y; Zhang, WY; Zhang, X; Zhu, HJ, 2003
)
0.32
" Between lampreys from the Atlantic Ocean and Great Lakes sites, two of seven GnRH form and dosage comparisons showed between-site differences, but were not believed to represent an overall between-site difference."( 15alpha-hydroxytestosterone induction by GnRH I and GnRH III in Atlantic and Great Lakes sea lamprey (Petromyzon marinus L.).
Bryan, MB; Li, W; Scott, AP; Sower, SA; Young, BA, 2004
)
0.32
" Male Han-Wistar rats were dosed with bromobenzene (1."( Integrated metabonomic analysis of bromobenzene-induced hepatotoxicity: novel induction of 5-oxoprolinosis.
Farrant, RD; Holmes, E; Nicholson, JK; Waterfield, CJ; Waters, NJ, 2006
)
0.33
" One of these is the increase in 5-oxoproline and ophthalmic acid concentrations with increased dosage of paracetamol."( A mathematical modelling approach to assessing the reliability of biomarkers of glutathione metabolism.
du Preez, FB; Geenen, S; Kenna, JG; Nijhout, HF; Reed, M; Snoep, JL; Westerhoff, HV; Wilson, ID, 2012
)
0.38
" No clear dose-response relationship existed between the quantity of paracetamol ingested and the observed concentrations of 5-oxoproline."( What is the clinical significance of 5-oxoproline (pyroglutamic acid) in high anion gap metabolic acidosis following paracetamol (acetaminophen) exposure?
Liss, DB; Mullins, ME; Paden, MS; Schwarz, ES, 2013
)
0.39
"We firstly showed that high dosage of Pidotimod could be an effective and safe to reduce the PFAPA attacks in children."( Proposal for a new therapeutic high dosage of Pidotimod in children with periodic fever, aphthous stomatitis, pharyngitis, adenitis (PFAPA) syndrome: a randomized controlled study.
Barone, P; Filosco, F; Finocchiaro, GG; Giugno, A; Leonardi, S; Manti, S; Papale, M; Parisi, GF, 2020
)
0.56
" This study shows that the proper dosing interval and drug dose both are important to eradicate the viral infection."( A Model for SARS-CoV-2 Infection with Treatment.
Al Basir, F; Chatterjee, AN, 2020
)
0.56
"Donanemab (an antibody specific for the N-terminal pyroglutamate β-amyloid epitope) dosing was every 4 weeks: 700 mg for the first 3 doses, then 1400 mg for up to 72 weeks."( Association of Amyloid Reduction After Donanemab Treatment With Tau Pathology and Clinical Outcomes: The TRAILBLAZER-ALZ Randomized Clinical Trial.
Andersen, SW; Brooks, DA; Evans, CD; Gueorguieva, I; Hauck, PM; Lu, M; Mintun, MA; Pontecorvo, MJ; Shcherbinin, S; Sims, JR; Willis, BA, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
algal metaboliteAny eukaryotic metabolite produced during a metabolic reaction in algae including unicellular organisms like chlorella and diatoms to multicellular organisms like giant kelps and brown algae.
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
[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 (6)

ClassDescription
5-oxoprolineAn oxoproline having the oxo group placed at the 5-position. It is an intermediate metabolite in the glutathione cycle.
L-proline derivativeA proteinogenic amino acid derivative resulting from reaction of L-proline at the amino group or the carboxy group, or from the replacement of any hydrogen of L-proline by a heteroatom.
non-proteinogenic L-alpha-amino acidAny L-alpha-amino acid which is not a member of the group of 23 proteinogenic amino acids.
oxoprolineA pyrrolidinemonocarboxylic acid consisting of proline bearing a single oxo substituent.
pyrrolidinemonocarboxylic acid
pyrrolidin-2-onesA pyrrolidinone in which the oxo group is at position 2 of the pyrrolidine ring.
[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 (11)

PathwayProteinsCompounds
Glutathione Metabolism1121
Glutathione Synthetase Deficiency1121
5-Oxoprolinuria1121
gamma-Glutamyltransferase Deficiency1121
5-Oxoprolinase Deficiency1121
gamma-Glutamyltranspeptidase Deficiency1121
Oxidative stress and redox pathway019
Glutathione and one-carbon metabolism010
Glutathione metabolism013
Trans-sulfuration, one-carbon metabolism and related pathways053
One-carbon metabolism and related pathways038
Gamma-glutamyl cycle for the biosynthesis and degradation of glutathione, including diseases69

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency2.66280.000811.382244.6684AID686979
Smad3Homo sapiens (human)Potency35.48130.00527.809829.0929AID588855
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency2.39140.000214.376460.0339AID720691
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.40530.005612.367736.1254AID624032
lamin isoform A-delta10Homo sapiens (human)Potency0.00560.891312.067628.1838AID1487
Chain A, Beta-lactamaseEscherichia coli K-12Potency39.81070.044717.8581100.0000AID485294
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency25.92900.00419.984825.9290AID504444
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (82)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID289446Antisecretory activity in rat pylorus ligation-induced ulcer model determined by ratio of total acidity inhibition in drug treated to untreated control2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID768710Toxicity in chloroquine-sensitive Plasmodium berghei NK-173 infected Swiss albino mouse assessed as mortality at 100 mg/kg, ip administered 4 times per day for 3 days measured up to 4 days2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives.
AID768715Antimalarial activity against chloroquine-sensitive Plasmodium berghei NK-173 infected in Swiss albino mouse assessed as quantal survival at 100 mg/kg, ip administered 4 times per day for 3 days measured on day 142013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives.
AID768731Antimalarial activity against chloroquine-sensitive Plasmodium berghei NK-173 infected in Swiss albino mouse assessed as quantal survival at 100 mg/kg, ip administered 4 times per day for 3 days measured on day 72013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives.
AID1399739Antifungal activity against Pseudoperonospora cubensis2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead.
AID768722Antimalarial activity against chloroquine-sensitive Plasmodium berghei NK-173 infected in Swiss albino mouse assessed as quantal survival at 100 mg/kg, ip administered 4 times per day for 3 days measured on day 102013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives.
AID1399727Antifungal activity against Phytophthora infestans assessed as inhibition of zoospore release at 100 ug/ml after 4 hrs relative to control2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead.
AID768704Antimalarial activity against chloroquine-sensitive Plasmodium berghei NK-173 infected in Swiss albino mouse assessed as host survival at 100 mg/kg, ip administered 4 times per day for 3 days measured on day 302013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives.
AID289444Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 10 umol2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID1399732Antibacterial activity against Bacillus thuringiensis at 2 mg/ml after 4 to 10 hrs by filter paper dispersion method2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead.
AID289445Antisecretory activity in rat pylorus ligation-induced ulcer model determined by ratio of free acidity inhibition in drug treated to untreated control2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID768728Antimalarial activity against chloroquine-sensitive Plasmodium berghei NK-173 infected in Swiss albino mouse assessed as quantal survival at 100 mg/kg, ip administered 4 times per day for 3 days measured on day 82013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives.
AID1399735Antibacterial activity against Ralstonia solanacearum at 2 mg/ml after 4 to 10 hrs by filter paper dispersion method2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead.
AID1399728Antifungal activity against Phytophthora infestans assessed as inhibition of zoospore release after 4 hrs2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead.
AID1399738Antifungal activity against Phytophthora infestans2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1224817Assays to identify small molecules inhibitory for eIF4E expression2015Chemistry & biology, Jul-23, Volume: 22, Issue:7
Internal Ribosome Entry Site-Based Bicistronic In Situ Reporter Assays for Discovery of Transcription-Targeted Lead Compounds.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID24381Inhibition of pyroglutamylaminopeptidase at a dose of 6.51 mM relative to 2-Oxo-hexahydro-pyrimidine-4-carboxylic acid1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Substrate specificity of pyroglutamylaminopeptidase.
AID24382Inhibition of pyroglutamylaminopeptidase at a dose of 6.51 mM relative to Pyrrolidin-2-one-CO-Gly-Ile1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Substrate specificity of pyroglutamylaminopeptidase.
AID227699Virtual screen for compounds with anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID24379Inhibition of pyroglutamylaminopeptidase at a dose of 13.02 mM relative to 2-Oxo-hexahydro-pyrimidine-4-carboxylic acid1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Substrate specificity of pyroglutamylaminopeptidase.
AID24380Inhibition of pyroglutamylaminopeptidase at a dose of 13.02 mM relative to Pyrrolidin-2-one-CO-Gly-Ile1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Substrate specificity of pyroglutamylaminopeptidase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,846)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990632 (22.21)18.7374
1990's881 (30.96)18.2507
2000's606 (21.29)29.6817
2010's571 (20.06)24.3611
2020's156 (5.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.90

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 Index28.90 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.04 (4.65)
Search Engine Demand Index42.07 (26.88)
Search Engine Supply Index2.76 (0.95)

This Compound (28.90)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials101 (3.36%)5.53%
Trials0 (0.00%)5.53%
Reviews176 (5.86%)6.00%
Reviews0 (0.00%)6.00%
Case Studies91 (3.03%)4.05%
Case Studies0 (0.00%)4.05%
Observational1 (0.03%)0.25%
Observational0 (0.00%)0.25%
Other2,636 (87.72%)84.16%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]