Compounds > diquafosol
Page last updated: 2024-12-08

diquafosol

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Description

diquafosol: purinoceptor P2Y(2) receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

P(1),P(4)-bis(uridin-5'-yl) tetraphosphate : A pyrimidine ribonucleoside 5'-tetraphosphate compound having 5'-uridinyl residues at the P(1)- and P(4)-positions. [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 CID148197
CHEMBL ID221326
CHEBI ID27791
SCHEMBL ID561378
MeSH IDM0356370

Synonyms (37)

Synonym
diquafosol
gtpl1736
[[[[(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] [(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl hydrogen phosphate
ins-365
C06198
uppppu
p1,p4-bis(5'-uridyl) tetraphosphate
CHEBI:27791 ,
59985-21-6
p(1),p(4)-bis(uridin-5'-yl) tetraphosphate
p1,p4-bis(5'-uridyl) tetrahydrogen tetraphosphate
CHEMBL221326 ,
[[(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate
p(1),p(4)-bis(uridin-5''-yl) tetraphosphate
bdbm50205413
p1,p4-bis(5''-uridyl) tetrahydrogen tetraphosphate
diquafosol sodium
unii-7828vc80fj
7828vc80fj ,
diquafosol [inn:ban]
kpy 998
SCHEMBL561378
diquafosol [who-dd]
uridine, 5'-(pentahydrogen tetraphosphate), p'''->5'-ester with uridine
diquafosol [mi]
diquafosol [inn]
p1, p4-di(uridine 5'-tetraphosphate), tetrasodium salt
uridine(5')tetraphospho(5')uridine
p1,p4-di(uridine 5'-tetraphosphate), tetrasodium salt
DTXSID40208689
{[(2r,3s,4r,5r)-5-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}({[({[({[(2r,3s,4r,5r)-5-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}(hydroxy)phosphoryl)oxy](hydroxy)phosphoryl}oxy)(hydroxy
Q5280143
AC-36640
[[(2r,3r,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-oxolan-2-yl]methoxy-hydroxy-phosphoryl]oxy-[[[(2r,3r,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-oxolan-2-yl]methoxy-hydroxy-phosphoryl]o
diquafosol sodium salt
uridine 5'-(pentahydrogen tetraphosphate), p'''->5'-ester with uridine sodium salt
p1,p4-diuridine 5'- tetraphosphate sodium salt

Research Excerpts

Overview

Diquafosol is a pharmaceutical drug used for dry eye treatment with a novel mechanism of action. It stimulates secretion of aqueous tear components from conjunctival epithelial cells and secretion of mucin from goblet cells.

ExcerptReferenceRelevance
"Diquafosol is a pharmaceutical drug used for dry eye treatment with a novel mechanism of action. "( Effect of Diquafosol on Hyperosmotic Stress-induced Tumor Necrosis Factor-α and Interleukin-6 Expression in Human Corneal Epithelial Cells.
Gum, SI; Jung, JC; Kim, BA; Kim, YH; Lee, GJ; Nguyen, LTH; Park, YJ; Yang, IJ; Yu, S, 2020)		2.4
"Diquafosol is a P2Y2 purinergic receptor agonist that stimulates secretion of aqueous tear components from conjunctival epithelial cells and secretion of mucin from conjunctival goblet cells."( Conjunctival expression of the P2Y2 receptor and the effects of 3% diquafosol ophthalmic solution in dogs.
Amasaki, H; Hara, Y; Harada, Y; Kohara, Y; Nezu, Y; Soeta, S; Tagawa, M; Terakado, K; Yogo, T, 2014)		1.36
"Diquafosol is a dinucleotide, purinoreceptor P2Y(2) receptor agonist. "( Diquafosol ophthalmic solution for dry eye treatment.
Imanaka, T; Nakamura, M; Sakamoto, A, 2012)		3.26

Effects

Diquafosol has potential as a treatment option for contact lens-related dry eye. The drug has high clinical efficacy and is well tolerated with a good safety profile.

ExcerptReferenceRelevance
"Diquafosol has a favorable risk/benefit profile in a broad spectrum of patients with dry eye disease and is a novel topical treatment of dry eye."( Double-masked, placebo-controlled safety and efficacy trial of diquafosol tetrasodium (INS365) ophthalmic solution for the treatment of dry eye.
Bokosky, JE; Davitt, WF; Kellerman, DJ; LaVange, LM; Mills-Wilson, MC; Nichols, KK; Schaberg, AE; Tauber, J; Yerxa, BR, 2004)		1.28
"Diquafosol has potential as a treatment option for contact lens-related dry eye."( Diquafosol Ophthalmic Solution Increases Pre- and Postlens Tear Film During Contact Lens Wear in Rabbit Eyes.
Koh, S; Mano, H; Nagahara, Y; Nagano, T; Nishida, K; Oshita, Y; Watanabe, H, 2017)		2.62
"Diquafosol has high clinical efficacy and is well tolerated with a good safety profile."( A randomised, double-masked comparison study of diquafosol versus sodium hyaluronate ophthalmic solutions in dry eye patients.
Ohashi, Y; Takamura, E; Tsubota, K; Watanabe, H, 2012)		1.36
"Diquafosol has a favorable risk/benefit profile in a broad spectrum of patients with dry eye disease and is a novel topical treatment of dry eye."( Double-masked, placebo-controlled safety and efficacy trial of diquafosol tetrasodium (INS365) ophthalmic solution for the treatment of dry eye.
Bokosky, JE; Davitt, WF; Kellerman, DJ; LaVange, LM; Mills-Wilson, MC; Nichols, KK; Schaberg, AE; Tauber, J; Yerxa, BR, 2004)		1.28

Actions

Diquafosol promotes secretion of tear fluid and mucin at the ocular surface. It is administered for treatment of dry eye (DE). Diquafsol eye drops activate P2Y2 receptors on the surface of the eye.

ExcerptReferenceRelevance
"Diquafosol promotes secretion of tear fluid and mucin at the ocular surface and is administered for treatment of dry eye (DE). "( Tear film lipid layer increase after diquafosol instillation in dry eye patients with meibomian gland dysfunction: a randomized clinical study.
Arita, R; Fukuoka, S, 2019)		2.23
"Diquafosol eye drops activate P2Y2 receptors on the surface of the eye and inner eyelids, enhancing the natural process of tear secretion."( Diquafosol: DE 089, diquafosol tetrasodium, INS 365, INS 365 Ophthalmic, INS 365 Respiratory, KPY 998.
, 2003)		2.48

Treatment

Treatment with diquafosol ophthalmic solution significantly improved dry eye symptoms, corneal staining, BUT, and tear meniscus height at 1 month and maintained the effectiveness for 6 months. Diquafsol treatment reduced intracellular ROS levels, apoptosis, and inflammation, all of which were increased in the dry eye model through desiccation.

ExcerptReferenceRelevance
"Diquafosol treatment reduced intracellular ROS levels, apoptosis, and inflammation, all of which were increased in the dry eye model through desiccation."( Diquafosol Sodium Inhibits Apoptosis and Inflammation of Corneal Epithelial Cells Via Activation of Erk1/2 and RSK: In Vitro and In Vivo Dry Eye Model.
Kang, DH; Kang, SS; Kim, JY; Moon, SH; Park, JH; Tchah, H; Um, HJ, 2018)		3.37
"Treatment with diquafosol ophthalmic solution significantly improved dry eye symptoms, corneal staining, BUT, and tear meniscus height at 1 month and maintained the effectiveness for 6 months. "( Long-term results of treatment with diquafosol ophthalmic solution for aqueous-deficient dry eye.
Ikeda, C; Koh, S; Maeda, N; Nishida, K; Takai, Y; Watanabe, H, 2013)		1.02
"Treatment with diquafosol ophthalmic solution significantly improved dry eye symptoms, corneal staining and BUT. "( Effect of diquafosol ophthalmic solution on the optical quality of the eyes in patients with aqueous-deficient dry eye.
Ikeda, C; Koh, S; Maeda, N; Nishida, K; Oie, Y; Soma, T; Tsujikawa, M; Watanabe, H, 2014)		1.16
"Treatment with diquafosol 3% with preservative-free sodium hyaluronate 0.1% was more effective than diquafosol 3% monotherapy or treatment with preserved sodium hyaluronate 0.1% in dry eye syndrome. "( Additive Effect of preservative-free sodium hyaluronate 0.1% in treatment of dry eye syndrome with diquafosol 3% eye drops.
Hwang, HS; Kim, EC; Lee, WS; Sung, YM, 2014)		0.97

Toxicity

Eye drops of 3% diquafosol may be an effective and safe treatment for the management of cataract surgery-induced dry eye aggravation in patients with preexisting dry eye.

ExcerptReferenceRelevance
" The predominant adverse events were cough, wheezing, chest tightness, and a decrease in FEV(1) (occurring in 8/48 adults, and 5/36 pediatric patients), which occurred predominantly in the 80-mg and 100-mg dose cohorts."( Safety of aerosolized INS 365 in patients with mild to moderate cystic fibrosis: results of a phase I multi-center study.
Accurso, F; Aitken, ML; Boyle, M; Dovey, M; Gibson, R; Hamblett, N; Johnson, C; Kellerman, D; Konstan, MW; Milgram, L; Mundahl, J; Noone, PG; Ramsey, B; Retsch-Bogort, G; Rodman, D; Williams-Warren, J; Wilmott, RW; Zeitlin, P, 2001)		0.31
" Safety measures were clinical blood and urine examination and recording of adverse events."( Efficacy and safety of diquafosol ophthalmic solution in patients with dry eye syndrome: a Japanese phase 2 clinical trial.
Matsumoto, Y; Ohashi, Y; Tsubota, K; Watanabe, H, 2012)		0.69
" No significant differences between the treatment groups were observed in relation to the occurrence of adverse events."( Efficacy and safety of diquafosol ophthalmic solution in patients with dry eye syndrome: a Japanese phase 2 clinical trial.
Matsumoto, Y; Ohashi, Y; Tsubota, K; Watanabe, H, 2012)		0.69
"Both 1% and 3% diquafosol ophthalmic solutions are considered effective and safe for the treatment of dry eye syndrome."( Efficacy and safety of diquafosol ophthalmic solution in patients with dry eye syndrome: a Japanese phase 2 clinical trial.
Matsumoto, Y; Ohashi, Y; Tsubota, K; Watanabe, H, 2012)		1.04
" Data evaluation was based on endpoints including Schirmer test, tear film break-up time, ocular surface staining score, subjective symptom score, and adverse events."( Efficacy and safety of topical diquafosol ophthalmic solution for treatment of dry eye: a systematic review of randomized clinical trials.
Chen, WQ; Li, R; Wang, Y; Wu, D, 2015)		0.7
"Topical diquafosol seems to be a safe therapeutic option for the treatment of dry eye."( Efficacy and safety of topical diquafosol ophthalmic solution for treatment of dry eye: a systematic review of randomized clinical trials.
Chen, WQ; Li, R; Wang, Y; Wu, D, 2015)		1.14
"Eye drops of 3% diquafosol may be an effective and safe treatment for the management of cataract surgery-induced dry eye aggravation in patients with preexisting dry eye."( Clinical Effects and Safety of 3% Diquafosol Ophthalmic Solution for Patients With Dry Eye After Cataract Surgery: A Randomized Controlled Trial.
Chung, JK; Lee, SJ; Park, DH; Seo, DR, 2016)		1.06
" The incidence of adverse drug reactions was investigated for safety evaluation."( Efficacy and Safety of the Long-Acting Diquafosol Ophthalmic Solution DE-089C in Patients with Dry Eye: A Randomized, Double-Masked, Placebo-Controlled Phase 3 Study.
Hori, Y; Inai, M; Oka, K, 2022)		0.99
" Commonly (incidence ≥ 1%) reported adverse drug reactions in the DE-089C group were eye irritation (3."( Efficacy and Safety of the Long-Acting Diquafosol Ophthalmic Solution DE-089C in Patients with Dry Eye: A Randomized, Double-Masked, Placebo-Controlled Phase 3 Study.
Hori, Y; Inai, M; Oka, K, 2022)		0.99
" Adverse events also will be monitored and documented."( Protocol for a parallel assignment prospective, randomised, comparative trial to evaluate the safety and efficacy of intense pulsed light (IPL) combined with 3% diquafosol (DQS) ophthalmic solution in dry eye syndrome.
Che, H; Chen, J; He, W; He, X; Huang, H; Li, L; Moore, JE; Moutari, S; Pazo, EE; Qi, Y; Qin, G; Wu, Y; Xia, Y; Xu, L; Yang, L; Yu, S; Zhang, Q, 2023)		1.11

Compound-Compound Interactions

360 dry eye disease patients will be equally divided randomly into the IPL group, DQS group and IPL+group. Management of dry eye with IPL combined with 3% diquafosol ophthalmic solution, registered on 23 January 2023.

ExcerptReferenceRelevance
" 360 dry eye disease patients will be equally divided randomly into the IPL group, DQS group (3% diquafosol ophthalmic solution eye-drops) and IPL+group (IPL combined with 3% diquafosol eye-drops)."( Protocol for a parallel assignment prospective, randomised, comparative trial to evaluate the safety and efficacy of intense pulsed light (IPL) combined with 3% diquafosol (DQS) ophthalmic solution in dry eye syndrome.
Che, H; Chen, J; He, W; He, X; Huang, H; Li, L; Moore, JE; Moutari, S; Pazo, EE; Qi, Y; Qin, G; Wu, Y; Xia, Y; Xu, L; Yang, L; Yu, S; Zhang, Q, 2023)		1.32
"Management of dry eye with IPL combined with 3% diquafosol ophthalmic solution, registered on 23 January 2023."( Protocol for a parallel assignment prospective, randomised, comparative trial to evaluate the safety and efficacy of intense pulsed light (IPL) combined with 3% diquafosol (DQS) ophthalmic solution in dry eye syndrome.
Che, H; Chen, J; He, W; He, X; Huang, H; Li, L; Moore, JE; Moutari, S; Pazo, EE; Qi, Y; Qin, G; Wu, Y; Xia, Y; Xu, L; Yang, L; Yu, S; Zhang, Q, 2023)		1.36

Dosage Studied

ExcerptRelevanceReference
"The efficacy and safety of DE-089C administered three times daily at half the dosage of DQS in patients with dry eye were confirmed in this study."( Efficacy and Safety of the Long-Acting Diquafosol Ophthalmic Solution DE-089C in Patients with Dry Eye: A Randomized, Double-Masked, Placebo-Controlled Phase 3 Study.
Hori, Y; Inai, M; Oka, K, 2022)		0.99
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
P2Y2 receptor agonistA compound that exhibits agonist activity at the P2Y2 receptor.
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
pyrimidine ribonucleoside 5'-tetraphosphate
uridine 5'-phosphate
[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 (1)

PathwayProteinsCompounds
Pyrimidine metabolism038

Protein Targets (4)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
P2Y purinoceptor 2Homo sapiens (human)EC50 (µMol)74.55890.00560.682810.0000AID280297; AID350668; AID350672; AID350678; AID350679; AID350683; AID350686; AID350688; AID350690; AID350692; AID350694; AID350696; AID350698; AID404832; AID460573; AID647894
P2Y purinoceptor 1Homo sapiens (human)EC50 (µMol)20.00000.00130.42027.2000AID304929
P2Y purinoceptor 4Homo sapiens (human)EC50 (µMol)0.13000.02301.362310.0000AID280298; AID404834
P2Y purinoceptor 6Homo sapiens (human)EC50 (µMol)10.58000.01302.393020.0000AID280301; AID404830
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
intracellular monoatomic ion homeostasisP2Y purinoceptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
positive regulation of mucus secretionP2Y purinoceptor 2Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 2Homo sapiens (human)
blood vessel diameter maintenanceP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
positive regulation of protein phosphorylationP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
monoatomic ion transportP2Y purinoceptor 1Homo sapiens (human)
cell surface receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationP2Y purinoceptor 1Homo sapiens (human)
glial cell migrationP2Y purinoceptor 1Homo sapiens (human)
regulation of cell shapeP2Y purinoceptor 1Homo sapiens (human)
response to mechanical stimulusP2Y purinoceptor 1Homo sapiens (human)
negative regulation of norepinephrine secretionP2Y purinoceptor 1Homo sapiens (human)
signal transduction involved in regulation of gene expressionP2Y purinoceptor 1Homo sapiens (human)
platelet activationP2Y purinoceptor 1Homo sapiens (human)
positive regulation of inositol trisphosphate biosynthetic processP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
eating behaviorP2Y purinoceptor 1Homo sapiens (human)
positive regulation of monoatomic ion transportP2Y purinoceptor 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIP2Y purinoceptor 1Homo sapiens (human)
positive regulation of hormone secretionP2Y purinoceptor 1Homo sapiens (human)
establishment of localization in cellP2Y purinoceptor 1Homo sapiens (human)
positive regulation of penile erectionP2Y purinoceptor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeP2Y purinoceptor 1Homo sapiens (human)
response to growth factorP2Y purinoceptor 1Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 1Homo sapiens (human)
cellular response to purine-containing compoundP2Y purinoceptor 1Homo sapiens (human)
protein localization to plasma membraneP2Y purinoceptor 1Homo sapiens (human)
relaxation of muscleP2Y purinoceptor 1Homo sapiens (human)
blood vessel diameter maintenanceP2Y purinoceptor 1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationP2Y purinoceptor 1Homo sapiens (human)
regulation of synaptic vesicle exocytosisP2Y purinoceptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationP2Y purinoceptor 4Homo sapiens (human)
transepithelial chloride transportP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 4Homo sapiens (human)
cellular response to prostaglandin E stimulusP2Y purinoceptor 4Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationP2Y purinoceptor 4Homo sapiens (human)
regulation of synaptic vesicle exocytosisP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
phagocytosisP2Y purinoceptor 6Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
activation of phospholipase C activityP2Y purinoceptor 6Homo sapiens (human)
positive regulation of smooth muscle cell migrationP2Y purinoceptor 6Homo sapiens (human)
transepithelial chloride transportP2Y purinoceptor 6Homo sapiens (human)
positive regulation of inositol 1,4,5-trisphosphate-sensitive calcium-release channel activityP2Y purinoceptor 6Homo sapiens (human)
positive regulation of inositol trisphosphate biosynthetic processP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeP2Y purinoceptor 6Homo sapiens (human)
cellular response to prostaglandin E stimulusP2Y purinoceptor 6Homo sapiens (human)
cellular response to purine-containing compoundP2Y purinoceptor 6Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationP2Y purinoceptor 6Homo sapiens (human)
cellular response to pyrimidine ribonucleotideP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
protein bindingP2Y purinoceptor 2Homo sapiens (human)
signaling receptor activityP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 2Homo sapiens (human)
A1 adenosine receptor bindingP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled ADP receptor activityP2Y purinoceptor 1Homo sapiens (human)
protein bindingP2Y purinoceptor 1Homo sapiens (human)
ATP bindingP2Y purinoceptor 1Homo sapiens (human)
signaling receptor activityP2Y purinoceptor 1Homo sapiens (human)
ADP bindingP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled ATP receptor activityP2Y purinoceptor 1Homo sapiens (human)
protein heterodimerization activityP2Y purinoceptor 1Homo sapiens (human)
scaffold protein bindingP2Y purinoceptor 1Homo sapiens (human)
A1 adenosine receptor bindingP2Y purinoceptor 1Homo sapiens (human)
protein bindingP2Y purinoceptor 4Homo sapiens (human)
ATP bindingP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled ADP receptor activityP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled receptor activityP2Y purinoceptor 6Homo sapiens (human)
protein bindingP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled UDP receptor activityP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
plasma membraneP2Y purinoceptor 2Homo sapiens (human)
plasma membraneP2Y purinoceptor 2Homo sapiens (human)
plasma membraneP2Y purinoceptor 1Homo sapiens (human)
ciliumP2Y purinoceptor 1Homo sapiens (human)
cell surfaceP2Y purinoceptor 1Homo sapiens (human)
postsynaptic densityP2Y purinoceptor 1Homo sapiens (human)
basolateral plasma membraneP2Y purinoceptor 1Homo sapiens (human)
apical plasma membraneP2Y purinoceptor 1Homo sapiens (human)
dendriteP2Y purinoceptor 1Homo sapiens (human)
cell bodyP2Y purinoceptor 1Homo sapiens (human)
postsynaptic membraneP2Y purinoceptor 1Homo sapiens (human)
presynaptic active zone membraneP2Y purinoceptor 1Homo sapiens (human)
glutamatergic synapseP2Y purinoceptor 1Homo sapiens (human)
plasma membraneP2Y purinoceptor 1Homo sapiens (human)
plasma membraneP2Y purinoceptor 4Homo sapiens (human)
basolateral plasma membraneP2Y purinoceptor 4Homo sapiens (human)
apical plasma membraneP2Y purinoceptor 4Homo sapiens (human)
presynaptic active zone membraneP2Y purinoceptor 4Homo sapiens (human)
glutamatergic synapseP2Y purinoceptor 4Homo sapiens (human)
plasma membraneP2Y purinoceptor 4Homo sapiens (human)
plasma membraneP2Y purinoceptor 6Homo sapiens (human)
basolateral plasma membraneP2Y purinoceptor 6Homo sapiens (human)
apical plasma membraneP2Y purinoceptor 6Homo sapiens (human)
plasma membraneP2Y purinoceptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID460573Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
5-OMe-UDP is a potent and selective P2Y(6)-receptor agonist.
AID280297Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
AID350668Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID280301Agonist activity at human recombinant P2Y6 receptor expressed in 1321N1 cells assessed as intracellular calcium mobilization2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
AID350696Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350687Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350686Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID404832Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
AID350690Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350672Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor S296A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350699Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID304929Agonist activity at human cloned P2Y1 receptor expressed in human 1321N1 by FLIPR assay2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Novel nucleotide triphosphates as potent P2Y2 agonists.
AID350683Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350685Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID644880Stability of the compound assessed as human e-NPP1-mediated hydrolysis at pH 8.5 after 20 mins by HPLC analysis2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Boranophosphate isoster controls P2Y-receptor subtype selectivity and metabolic stability of dinucleoside polyphosphate analogues.
AID350708Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID404834Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
AID350671Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor S296A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350697Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350679Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID280298Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
AID350712Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level up to 300 uM relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID647894Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Boranophosphate isoster controls P2Y-receptor subtype selectivity and metabolic stability of dinucleoside polyphosphate analogues.
AID350673Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350678Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350689Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350694Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350665Ratio of EC50 for N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant to EC50 for wild type 3 human P2Y2 receptor2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350684Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350691Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350688Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID404830Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
AID350698Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350692Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID350918Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level relative to carbachol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
AID1347028Human P2Y2 receptor (P2Y receptors)2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates.
AID1346348Human P2Y4 receptor (P2Y receptors)2006Current medicinal chemistry, , Volume: 13, Issue:3
P2 receptors activated by uracil nucleotides--an update.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (119)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (0.84)18.2507
2000's25 (21.01)29.6817
2010's72 (60.50)24.3611
2020's21 (17.65)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.96

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

MetricThis Compound (vs All)
Research Demand Index37.96 (24.57)
Research Supply Index5.11 (2.92)
Research Growth Index6.26 (4.65)
Search Engine Demand Index91.51 (26.88)
Search Engine Supply Index3.56 (0.95)

This Compound (37.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials38 (30.16%)5.53%
Reviews20 (15.87%)6.00%
Case Studies1 (0.79%)4.05%
Observational4 (3.17%)0.25%
Other63 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chlorine
chloride : A halide anion formed when chlorine picks up an electron to form an an anion.		2.0110halide anion;
monoatomic chlorine		cofactor;
Escherichia coli metabolite;
human metabolite
opc 12759
rebamipide: structure in first source; RN refers to (+-)-isomer; inhibits gastric xanthine oxidase		6.9981secondary carboxamide
ticlopidine
Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.		3.110monochlorobenzenes;
thienopyridine		anticoagulant;
fibrin modulating drug;
hematologic agent;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		2.0510ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
pilocarpine
Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.		7.4110pilocarpineantiglaucoma drug
alanine
Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.		6.9981alanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid		EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
adenosine diphosphate
Adenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.		3.110adenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate		fundamental metabolite;
human metabolite
uridine
[no description available]		5.0750uridinesdrug metabolite;
fundamental metabolite;
human metabolite
uridine diphosphate
Uridine Diphosphate: A uracil nucleotide containing a pyrophosphate group esterified to C5 of the sugar moiety.		2.9540pyrimidine ribonucleoside 5'-diphosphate;
uridine 5'-phosphate		Escherichia coli metabolite;
mouse metabolite
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		6.9981monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
adenosine monophosphate
Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.		3.110adenosine 5'-phosphate;
purine ribonucleoside 5'-monophosphate		adenosine A1 receptor agonist;
cofactor;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
EC 3.1.3.11 (fructose-bisphosphatase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
uridine triphosphate
Uridine Triphosphate: Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.		4.7490pyrimidine ribonucleoside 5'-triphosphate;
uridine 5'-phosphate		Escherichia coli metabolite;
mouse metabolite
phenylalanine
Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.		2.1710amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
quinuclidines
Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group.		2.4110quinuclidines;
saturated organic heterobicyclic parent
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		2.4110mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
d-alpha tocopherol
Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.		2.3110alpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
fluorescein
Fluorescein: A phthalic indicator dye that appears yellow-green in normal tear film and bright green in a more alkaline medium such as the aqueous humor.. fluorescein (lactone form) : A xanthene dye that is highly fluorescent, detectable even when present in minute quantities. Used forensically to detect traces of blood, in analytical chemistry as an indicator in silver nitrate titrations and in microscopy.		10.621582-benzofurans;
gamma-lactone;
organic heteropentacyclic compound;
oxaspiro compound;
polyphenol;
xanthene dye		fluorescent dye;
radioopaque medium
diadenosine tetraphosphate
P(1),P(4)-bis(5'-adenosyl) tetraphosphate : A diadenosyl tetraphosphate compound having the two 5'-adenosyl residues attached at the P(1)- and P(4)-positions.		2.7430diadenosyl tetraphosphateEscherichia coli metabolite;
mouse metabolite
ozone
Ozone: The unstable triatomic form of oxygen, O3. It is a powerful oxidant that is produced for various chemical and industrial uses. Its production is also catalyzed in the ATMOSPHERE by ULTRAVIOLET RAY irradiation of oxygen or other ozone precursors such as VOLATILE ORGANIC COMPOUNDS and NITROGEN OXIDES. About 90% of the ozone in the atmosphere exists in the stratosphere (STRATOSPHERIC OZONE).. ozone : An elemental molecule with formula O3. An explosive, pale blue gas (b.p. -112degreeC) that has a characteristic, pungent odour, it is continuously produced in the upper atmosphere by the action of solar ultraviolet radiation on atmospheric oxygen. It is an antimicrobial agent used in the production of bottled water, as well as in the treatment of meat, poultry and other foodstuffs.		2.2110elemental molecule;
gas molecular entity;
reactive oxygen species;
triatomic oxygen		antiseptic drug;
disinfectant;
electrophilic reagent;
greenhouse gas;
mutagen;
oxidising agent;
tracer
clopidogrel
Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.		3.110methyl ester;
monochlorobenzenes;
thienopyridine		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		3.110adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
deoxyuridine triphosphate
[no description available]		2.0310deoxyuridine phosphate;
pyrimidine 2'-deoxyribonucleoside 5'-triphosphate		Arabidopsis thaliana metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite
carboxypolymethylene
carbomer: high molecular polyanionic substance		3.5311
methylthio-adp
[no description available]		2.0710
diadenosine triphosphate
[no description available]		2.4620diadenosyl triphosphatemouse metabolite
uridine 5'-tetraphosphate
[no description available]		2.0410
n-acetylneuraminic acid
N-Acetylneuraminic Acid: An N-acyl derivative of neuraminic acid. N-acetylneuraminic acid occurs in many polysaccharides, glycoproteins, and glycolipids in animals and bacteria. (From Dorland, 28th ed, p1518). N-acetylneuraminic acid : An N-acylneuraminic acid where the N-acyl group is specified as acetyl.		2.1110N-acetylneuraminic acidsantioxidant;
bacterial metabolite;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
human metabolite;
mouse metabolite
nitro-bis(2,4-pentanedionato)(pyridine)cobalt(iii)
nitro-bis(2,4-pentanedionato)(pyridine)cobalt(III): structure given in first source. P(1),P(5)-bis(5'-adenosyl) pentaphosphate : A diadenosyl pentaphosphate having the two 5'-adenosyl residues attached at the P(1)- and P(5)-positions.		2.0710diadenosyl pentaphosphateEscherichia coli metabolite;
vasoconstrictor agent
TTP
[no description available]		2.0310pyrimidine ribonucleoside 5'-triphosphate
bromochloroacetic acid
Keratins: A class of fibrous proteins or scleroproteins that represents the principal constituent of EPIDERMIS; HAIR; NAILS; horny tissues, and the organic matrix of tooth ENAMEL. Two major conformational groups have been characterized, alpha-keratin, whose peptide backbone forms a coiled-coil alpha helical structure consisting of TYPE I KERATIN and a TYPE II KERATIN, and beta-keratin, whose backbone forms a zigzag or pleated sheet structure. alpha-Keratins have been classified into at least 20 subtypes. In addition multiple isoforms of subtypes have been found which may be due to GENE DUPLICATION.. bromochloroacetic acid : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by bromine while a second is replaced by chlorine. A low-melting (27.5-31.5degreeC), hygroscopic crystalline solid, it can be formed during the disinfection (by chlorination) of water that contains bromide ions and organic matter, so can occur in drinking water as a byproduct of the disinfection process.		2.17102-bromocarboxylic acid;
monocarboxylic acid;
organochlorine compound
Reactive blue 2
[no description available]		3.1310anthraquinone
4-thiouridine triphosphate
[no description available]		3.1310
cangrelor
cangrelor: platelet P(2T) receptor antagonist. cangrelor : A nucleoside triphosphate analogue that is 5'-O-[({[dichloro(phosphono)methyl](hydroxy)phosphoryl}oxy)(hydroxy)phosphoryl]adenosine carrying additional 2-(methylsulfanyl)ethyl and (3,3,3-trifluoropropyl)sulfanyl substituents at positions N6 and C2 respectively. Used (in the form of its tetrasodium salt) as an intravenous antiplatelet drug that prevents formation of harmful blood clots in the coronary arteries.		3.110adenosine 5'-phosphate;
aryl sulfide;
nucleoside triphosphate analogue;
organochlorine compound;
organofluorine compound;
secondary amino compound		P2Y12 receptor antagonist;
platelet aggregation inhibitor
5-bromouridine triphosphate
5-bromouridine 5'-triphosphate : A pyrimidine ribonucleoside 5'-triphosphate having 5-bromouracil as the pyrimidine component.		2.4520organobromine compound;
pyrimidine ribonucleoside 5'-triphosphate
denufosol tetrasodium
[no description available]		2.9540
denufosol tetrasodium
denufosol tetrasodium: for treatment of cystic fibrosis		5.0750
5-fluorouridine 5'-triphosphate
[no description available]		2.0510
sar 1118
lifitegrast: An LFA-1 (LYMPHOCYTE FUNCTION-ASSOCIATED ANTIGEN-1) antagonist that is used in the treatment of DRY EYE SYNDROMES.. lifitegrast : An N-acyl-L-alpha-amino acid obtained by formal condensation of the carboxy group of N-[2-(1-benzofuran-6-carbonyl)]-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxylic acid with the amino group of 3-(methanesulfonyl)-L-phenylalanine. Used for treatment of keratoconjunctivitis sicca (dry eye syndrome).		2.17101-benzofurans;
isoquinolines;
L-phenylalanine derivative;
N-acyl-L-alpha-amino acid;
sulfone		anti-inflammatory drug;
lymphocyte function-associated antigen-1 antagonist
scopolamine hydrobromide
[no description available]		2.1710
thymosin beta(4)
thymosin beta(4): biological active peptide present in thymosin fractions 5 & 5A; participates in the regulation, differentiation & function of thymus-derived lymphocytes & may also act directly or indirectly on macrophages & other cells involved in cell-mediated immunity		2.1710
thymosin
Thymosin: Thymosin. A family of heat-stable, polypeptide hormones secreted by the thymus gland. Their biological activities include lymphocytopoiesis, restoration of immunological competence and enhancement of expression of T-cell characteristics and function. They have therapeutic potential in patients having primary or secondary immunodeficiency diseases, cancer or diseases related to aging.		2.1710
epidermal growth factor
Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.		2.1310
cyclosporine
Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).		8.79136
lactoferrin
Lactoferrin: An iron-binding protein that was originally characterized as a milk protein. It is widely distributed in secretory fluids and is found in the neutrophilic granules of LEUKOCYTES. The N-terminal part of lactoferrin possesses a serine protease which functions to inactivate the TYPE III SECRETION SYSTEM used by bacteria to export virulence proteins for host cell invasion.		2.1110
muramidase
Muramidase: A basic enzyme that is present in saliva, tears, egg white, and many animal fluids. It functions as an antibacterial agent. The enzyme catalyzes the hydrolysis of 1,4-beta-linkages between N-acetylmuramic acid and N-acetyl-D-glucosamine residues in peptidoglycan and between N-acetyl-D-glucosamine residues in chitodextrin. EC 3.2.1.17.		2.1110
ConditionIndicatedRelationship StrengthStudiesTrials
Cystic Fibrosis of Pancreas
[description not available]		06.9371
Allergic Reaction
[description not available]		02.9410
Innate Inflammatory Response
[description not available]		03.7130
Obstructive Lung Diseases
[description not available]		02.9410
Benign Neoplasms
[description not available]		02.9410
Dry Eye
[description not available]		018.4512648
Cystic Fibrosis
An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION.		06.9371
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		02.9410
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		08.7130
Lung Diseases, Obstructive
Any disorder marked by obstruction of conducting airways of the lung. AIRWAY OBSTRUCTION may be acute, chronic, intermittent, or persistent.		02.9410
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.9410
Dry Eye Syndromes
Corneal and conjunctival dryness due to deficient tear production, predominantly in menopausal and post-menopausal women. Filamentary keratitis or erosion of the conjunctival and corneal epithelium may be caused by these disorders. Sensation of the presence of a foreign body in the eye and burning of the eyes may occur.		018.4512648
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.7590
Diabetes Mellitus, Adult-Onset
[description not available]		06.58101
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		06.58101
Cataract, Membranous
[description not available]		05.9922
Cataract
Partial or complete opacity on or in the lens or capsule of one or both eyes, impairing vision or causing blindness. The many kinds of cataract are classified by their morphology (size, shape, location) or etiology (cause and time of occurrence). (Dorland, 27th ed)		05.9922
Adverse Drug Event
[description not available]		03.811
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		03.811
Ache
[description not available]		02.610
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		02.610
Glaucoma
An ocular disease, occurring in many forms, having as its primary characteristics an unstable or a sustained increase in the intraocular pressure which the eye cannot withstand without damage to its structure or impairment of its function. The consequences of the increased pressure may be manifested in a variety of symptoms, depending upon type and severity, such as excavation of the optic disk, hardness of the eyeball, corneal anesthesia, reduced visual acuity, seeing of colored halos around lights, disturbed dark adaptation, visual field defects, and headaches. (Dictionary of Visual Science, 4th ed)		09.24100
Lacerations
Torn, ragged, mangled wounds.		03.9911
Nearsightedness
[description not available]		02.610
Myopia
A refractive error in which rays of light entering the EYE parallel to the optic axis are brought to a focus in front of the RETINA when accommodation (ACCOMMODATION, OCULAR) is relaxed. This results from an overly curved CORNEA or from the eyeball being too long from front to back. It is also called nearsightedness.		02.610
Eyelid Diseases
Diseases involving the EYELIDS.		03.9321
Diseases, Occupational
[description not available]		03.5311
Graft-Versus-Host Disease
[description not available]		07.5420
Graft vs Host Disease
The clinical entity characterized by anorexia, diarrhea, loss of hair, leukopenia, thrombocytopenia, growth retardation, and eventual death brought about by the GRAFT VS HOST REACTION.		02.5420
Keratitis
Inflammation of the cornea.		02.1710
Corneal Diseases
Diseases of the cornea.		02.5720
Foreign-Body Reaction
Chronic inflammation and granuloma formation around irritating foreign bodies.		02.2110
Meibomian Gland Dysfunction
A chronic dysfunction of MEIBOMIAN GLANDS characterized by altered tear film stability and function due to a decrease or alteration in lipid quality/content in meibum. It is often associated with evaporative-type DRY EYE SYNDROME.		08.5911
Sicca Syndrome
[description not available]		09.04131
Xerophthalmia
Dryness of the eye surfaces caused by deficiency of tears or conjunctival secretions. It may be associated with vitamin A deficiency, trauma, or any condition in which the eyelids do not close completely.		03.3620
Sjogren's Syndrome
Chronic inflammatory and autoimmune disease in which the salivary and lacrimal glands undergo progressive destruction by lymphocytes and plasma cells resulting in decreased production of saliva and tears. The primary form, often called sicca syndrome, involves both KERATOCONJUNCTIVITIS SICCA and XEROSTOMIA. The secondary form includes, in addition, the presence of a connective tissue disease, usually rheumatoid arthritis.		09.04131
Complication, Postoperative
[description not available]		04.8221
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		04.8221
Keratoconjunctivitis Sicca
Drying and inflammation of the conjunctiva as a result of insufficient lacrimal secretion. When found in association with XEROSTOMIA and polyarthritis, it is called SJOGREN'S SYNDROME.		08.7330
Corneal Wavefront Aberration
Asymmetries in the topography and refractive index of the corneal surface that affect visual acuity.		03.4420
Benign Mucosal Pemphigoid
[description not available]		02.1110
Pemphigoid, Benign Mucous Membrane
A chronic blistering disease with predilection for mucous membranes and less frequently the skin, and with a tendency to scarring. It is sometimes called ocular pemphigoid because of conjunctival mucous membrane involvement.		02.1110
Chronic Primary Open Angle Glaucoma
[description not available]		02.1310
Glaucoma, Open-Angle
Glaucoma in which the angle of the anterior chamber is open and the trabecular meshwork does not encroach on the base of the iris.		02.1310
Intraocular Pressure
The pressure of the fluids in the eye.		02.4720
Anaplastic Astrocytoma
[description not available]		02.0110
Benign Neoplasms, Brain
[description not available]		02.0110
Astrocytoma
Neoplasms of the brain and spinal cord derived from glial cells which vary from histologically benign forms to highly anaplastic and malignant tumors. Fibrillary astrocytomas are the most common type and may be classified in order of increasing malignancy (grades I through IV). In the first two decades of life, astrocytomas tend to originate in the cerebellar hemispheres; in adults, they most frequently arise in the cerebrum and frequently undergo malignant transformation. (From Devita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2013-7; Holland et al., Cancer Medicine, 3d ed, p1082)		02.0110
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		02.0110
Respiratory Tract Diseases
Diseases involving the RESPIRATORY SYSTEM.		02.9310
Breathing Sounds
[description not available]		03.3911
Cough
A sudden, audible expulsion of air from the lungs through a partially closed glottis, preceded by inhalation. It is a protective response that serves to clear the trachea, bronchi, and/or lungs of irritants and secretions, or to prevent aspiration of foreign materials into the lungs.		03.3911
Respiratory Sounds
Noises, normal and abnormal, heard on auscultation over any part of the RESPIRATORY TRACT.		03.3911
Arteriosclerosis
Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.		02.9210
Chronic Bronchitis
[description not available]		02.9210
Bronchitis, Chronic
A subcategory of CHRONIC OBSTRUCTIVE PULMONARY DISEASE. The disease is characterized by hypersecretion of mucus accompanied by a chronic (more than 3 months in 2 consecutive years) productive cough. Infectious agents are a major cause of chronic bronchitis.		02.9210