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thiocolchicoside

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Description

Thiocolchicoside is a muscle relaxant drug that acts as a selective antagonist of the glycine receptor. It is used to treat muscle spasms and pain. Thiocolchicoside is thought to work by blocking the transmission of pain signals in the spinal cord. It is a synthetic compound, structurally similar to colchicine. Thiocolchicoside has been studied for its potential to treat a variety of conditions, including pain, inflammation, and muscle spasms. It is also being investigated for its potential to improve the quality of life for people with chronic pain. Thiocolchicoside is typically well-tolerated, but can cause side effects such as drowsiness, dizziness, and nausea. It is important to note that thiocolchicoside is a prescription drug and should only be used under the supervision of a healthcare professional.'
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thiocolchicoside: used in combination with glafenine and meprobamate to tranquilize patients undergoing hysterosalpingography; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID72067
CHEMBL ID1705373
CHEBI ID91529
SCHEMBL ID719194
MeSH IDM0045288
PubMed CID9915886
CHEMBL ID213907
CHEBI ID94557
SCHEMBL ID240410
MeSH IDM0045288

Synonyms (78)

Synonym
smr001233221
MLS002153865
BRD-A11605036-001-03-2
n-[1,2-dimethoxy-10-methylsulfanyl-9-oxo-3-[(2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydropyran-2-yl]oxy-6,7-dihydro-5h-benzo[a]heptalen-7-yl]acetamide
n-(3-(hexopyranosyloxy)-1,2-dimethoxy-10-(methylthio)-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl)acetamide
BSPBIO_000557
PRESTWICK_875
PRESTWICK2_000539
BPBIO1_000613
PRESTWICK3_000539
SPBIO_002478
PRESTWICK1_000539
PRESTWICK0_000539
n-[1,2-dimethoxy-10-methylsulfanyl-9-oxo-3-[(2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6,7-dihydro-5h-benzo[a]heptalen-7-yl]acetamide
thiocolchicoside-d3
HMS1569L19
HMS2096L19
miorel
HMS2234K08
CHEMBL1705373
coltrax
thiocolchicine glycoside
SCHEMBL719194
LEQAKWQJCITZNK-MSQQGMGVSA-N
SR-01000841233-2
sr-01000841233
CHEBI:91529
bdbm50248250
Q1165293
2-demethoxy-2-glucosidoxythiocolchicine
602-41-5 (unlabeled)
brn 0072205
tiocolchicosido [inn-spanish]
acetamide, n-(3-(beta-d-glucopyranosyloxy)-5,6,7,9-tetrahydro-1,2-dimethoxy-10-(methylthio)-9-oxobenzo(a)heptalen-7-yl)-, (s)-
tiocolchicoside [dcit]
10-thiocolchicoside
thiocolchicoside [inn:dcf]
thiocolchicosidum [inn-latin]
einecs 210-017-7
nsc 147755
D07276
thiocolchicoside (inn)
coltramyl (tn)
602-41-5
thiocolchicoside
CHEMBL213907
tox21_110470
dtxsid5045330 ,
dtxcid3025330
AKOS016010119
thiocolchicosidum
tiocolchicosido
t1x8s697gt ,
unii-t1x8s697gt
tiocolchicoside
S5049
BRD-K26619122-001-01-3
thiocolchicoside [inn]
thiocolchicoside [mart.]
thiocolchicoside [who-dd]
SCHEMBL240410
CCG-220539
Q-201823
AC-34475
mfcd07995056
n-[(7s)-1,2-dimethoxy-10-(methylthio)-9-oxo-3-[[(2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6,7-dihydro-5h-benzo[a]heptalen-7-yl]acetamide
CHEBI:94557
bdbm233193
thiocolchicoside crystallised from ethanol, europepharmacopoeia (ep) reference standard
thiocolchicoside for system suitability, europepharmacopoeia (ep) reference standard
thiocolchicoside, >=98% (hplc)
HMS3713L19
A914515
DB11582
HY-N0301
AS-14082
HMS3886E11
CS-0008802

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Its chemical structure consists of colchicine, a sugar (ose) and a sulphur-containing radical (thio), and its adverse effects are therefore likely to be similar to those of colchicine."( Thiocolchicoside: review of adverse effects.
, 2016
)
0.43
" Both the test and the reference treatment were well tolerated in terms of adverse effects, laboratory parameters and vital signs."( Efficacy and safety of a fixed combination of intramuscular diclofenac 75 mg + thiocolchicoside 4 mg in the treatment of acute low back pain: a phase III, randomized, double blind, controlled trial.
Albamonte, E; Caggiano, G; Costantino, C; Giossi, A; Mancuso, M; Rigamonti, A; Sproviero, E; Tornari, P, 2018
)
0.48
"The new diclofenac+thiocolchicoside FDC formulation may allow treating effectively acute LBP while reducing the number of injections and hence the risk of local adverse reactions, and improving the patient's compliance."( Efficacy and safety of a fixed combination of intramuscular diclofenac 75 mg + thiocolchicoside 4 mg in the treatment of acute low back pain: a phase III, randomized, double blind, controlled trial.
Albamonte, E; Caggiano, G; Costantino, C; Giossi, A; Mancuso, M; Rigamonti, A; Sproviero, E; Tornari, P, 2018
)
0.48

Pharmacokinetics

Thiocolchicoside (TCC) has been prescribed for several years as a muscle relaxant drug. Its pharmacokinetic (PK) profile and metabolism still remain largely unknown.

ExcerptReferenceRelevance
" The pharmacokinetic parameters between the first and the last days were compared using Student's t-test."( Single- and repeated-dose pharmacokinetics of intramuscular thiocolchicoside in healthy volunteers.
Debray, M; Sandouk, P; Scherrmann, JM; Weinling, E, 1999
)
0.3
"Thiocolchicoside pharmacokinetic parameters, calculated after the single dose using non-compartmental analysis, were in good agreement with those obtained in previous studies."( Single- and repeated-dose pharmacokinetics of intramuscular thiocolchicoside in healthy volunteers.
Debray, M; Sandouk, P; Scherrmann, JM; Weinling, E, 1999
)
0.3
"Thiocolchicoside (TCC) has been prescribed for several years as a muscle relaxant drug, but its pharmacokinetic (PK) profile and metabolism still remain largely unknown."( New metabolic and pharmacokinetic characteristics of thiocolchicoside and its active metabolite in healthy humans.
Adam, R; Dubruc, C; Filali-Ansary, A; Françon, D; Lluel, P; Thénot, JP; Trellu, M, 2004
)
0.32

Bioavailability

Thiocolchicoside (TCC) is an effective therapeutic agent against the orthopaedic, traumatic and rheumatologic disorders. It suffer from the drawback of poor bioavailability due to extensive first pass metabolism and low permeability via the oral route.

ExcerptReferenceRelevance
" The relative bioavailability of both oral formulations was approximately 25%, compared to the intramuscular formulation."( Single-dose bioavailability of oral and intramuscular thiocolchicoside in healthy volunteers.
Bouvier d'Yvoire, M; Chretien, P; Sandouk, P; Scherrmann, JM; Tillement, JP, 1994
)
0.29
" After oral administration the extent of bioavailability compared with intra-muscular administration is low, due to a first pass effect."( Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies.
Artusi, M; Colombo, P; Junginger, HE; Santi, P, 2003
)
0.32
" As TCC and M1 present an equipotent pharmacological activity, the relative oral pharmacological bioavailability of TCC vs."( New metabolic and pharmacokinetic characteristics of thiocolchicoside and its active metabolite in healthy humans.
Adam, R; Dubruc, C; Filali-Ansary, A; Françon, D; Lluel, P; Thénot, JP; Trellu, M, 2004
)
0.32
"Thiocolchicoside (TCC) is an effective therapeutic agent against the orthopaedic, traumatic and rheumatologic disorders but it suffer from the drawback of poor bioavailability due to extensive first pass metabolism and low permeability via the oral route."( Omega 3 fatty acid-enriched nanoemulsion of thiocolchicoside for transdermal delivery: formulation, characterization and absorption studies.
Ali, J; Baboota, S; Kumar, D, 2016
)
0.43
"The objective of this study was the development of chitosan/hyaluronan transdermal films to improve bioavailability of thiocolchicoside."( Development and characterization of chitosan/hyaluronan film for transdermal delivery of thiocolchicoside.
Abruzzo, A; Bigucci, F; Cerchiara, T; Gallucci, MC; Luppi, B; Saladini, B, 2015
)
0.42
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

A new, simple HPTLC method for determination of etoricoxib (ETO) and thiocolchicoside (THIO) in combined tablet dosage form has been developed. Two dosage forms, a bioadhesive disc and a fast dissolving disc for buccal and sublingual administration of THIO were designed.

ExcerptRelevanceReference
" But no adjustments of dose or dosing interval were necessary because the accumulation did not lead to marked change in the plasma levels."( Single- and repeated-dose pharmacokinetics of intramuscular thiocolchicoside in healthy volunteers.
Debray, M; Sandouk, P; Scherrmann, JM; Weinling, E, 1999
)
0.3
" Two dosage forms, a bioadhesive disc and a fast dissolving disc for buccal and sublingual administration of thiocolchicoside, respectively, were designed."( Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies.
Artusi, M; Colombo, P; Junginger, HE; Santi, P, 2003
)
0.32
"A new, simple HPTLC method for determination of etoricoxib (ETO) and thiocolchicoside (THIO) in combined tablet dosage form has been developed and validated."( High-performance thin-layer chromatographic determination of etoricoxib and thiocolchicoside in combined tablet dosage form.
Gandhi, SV; Patil, UP; Rajmane, VS; Sengar, MR,
)
0.13
"A simple, reproducible and efficient reverse phase high performance liquid chromatographic method was developed for simultaneous estimation of etoricoxib and thiocolchicoside in combined tablet dosage form."( Simultaneous estimation of etoricoxib and thiocolchicoside by RP-HPLC method in combined dosage forms.
Joshi, A; Kumar, S; Pathak, AK; Shah, K; Thakur, RS,
)
0.13
"Findings will provide timely information on the safety, efficacy, and optimal dosing of t-PA to treat moderate/severe COVID-19-induced ARDS, which can be rapidly adapted to a phase III trial (NCT04357730; FDA IND 149634)."(
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Shen, S; Shen, Y; Shen, Z; Shi, J; Shi-Li, L; Shimoda, K; Shoji, Y; Shun, C; Silva, MA; Silva-Cardoso, J; Simas, NK; Simirgiotis, MJ; Sincock, SA; Singh, MP; Sionis, A; Siu, J; Sivieri, EM; Sjerps, MJ; Skoczen, SL; Slabon, A; Slette, IJ; Smith, MD; Smith, S; Smith, TG; Snapp, KS; Snow, SJ; Soares, MCF; Soberman, D; Solares, MD; Soliman, I; Song, J; Sorooshian, A; Sorrell, TC; Spinar, J; Staudt, A; Steinhart, C; Stern, ST; Stevens, DM; Stiers, KM; Stimming, U; Su, YG; Subbian, V; Suga, H; Sukhija-Cohen, A; Suksamrarn, A; Suksen, K; Sun, J; Sun, M; Sun, P; Sun, W; Sun, XF; Sun, Y; Sundell, J; Susan, LF; Sutjarit, N; Swamy, KV; Swisher, EM; Sykes, C; Takahashi, JA; Talmor, DS; Tan, B; Tan, ZK; Tang, L; Tang, S; Tanner, JJ; Tanwar, M; Tarazi, Z; Tarvasmäki, T; Tay, FR; Teketel, A; Temitayo, GI; Thersleff, T; Thiessen Philbrook, H; Thompson, LC; Thongon, N; Tian, B; Tian, F; Tian, Q; Timothy, AT; Tingle, MD; Titze, IR; Tolppanen, H; Tong, W; Toyoda, H; Tronconi, L; Tseng, CH; Tu, H; Tu, YJ; Tung, SY; Turpault, S; Tuynman, JB; Uemoto, AT; Ugurlu, M; Ullah, S; Underwood, RS; Ungell, AL; Usandizaga-Elio, I; Vakonakis, I; van Boxel, GI; van den Beucken, JJJP; van der Boom, T; van Slegtenhorst, MA; Vanni, JR; Vaquera, A; Vasconcellos, RS; Velayos, M; Vena, R; Ventura, G; Verso, MG; Vincent, RP; Vitale, F; Vitali, S; Vlek, SL; Vleugels, MPH; Volkmann, N; Vukelic, M; Wagner Mackenzie, B; Wairagala, P; Waller, SB; Wan, J; Wan, MT; Wan, Y; Wang, CC; Wang, H; Wang, J; Wang, JF; Wang, K; Wang, L; Wang, M; Wang, S; Wang, WM; Wang, X; Wang, Y; Wang, YD; Wang, YF; Wang, Z; Wang, ZG; Warriner, K; Weberpals, JI; Weerachayaphorn, J; Wehrli, FW; Wei, J; Wei, KL; Weinheimer, CJ; Weisbord, SD; Wen, S; Wendel Garcia, PD; Williams, JW; Williams, R; Winkler, C; Wirman, AP; Wong, S; Woods, CM; Wu, B; Wu, C; Wu, F; Wu, P; Wu, S; Wu, Y; Wu, YN; Wu, ZH; Wurtzel, JGT; Xia, L; Xia, Z; Xia, ZZ; Xiao, H; Xie, C; Xin, ZM; Xing, Y; Xing, Z; Xu, S; Xu, SB; Xu, T; Xu, X; Xu, Y; Xue, L; Xun, J; Yaffe, MB; Yalew, A; Yamamoto, S; Yan, D; Yan, H; Yan, S; Yan, X; Yang, AD; Yang, E; Yang, H; Yang, J; Yang, JL; Yang, K; Yang, M; Yang, P; Yang, Q; Yang, S; Yang, W; Yang, X; Yang, Y; Yao, JC; Yao, WL; Yao, Y; Yaqub, TB; Ye, J; Ye, W; Yen, CW; Yeter, HH; Yin, C; Yip, V; Yong-Yi, J; Yu, HJ; Yu, MF; Yu, S; Yu, W; Yu, WW; Yu, X; Yuan, P; Yuan, Q; Yue, XY; Zaia, AA; Zakhary, SY; Zalwango, F; Zamalloa, A; Zamparo, P; Zampini, IC; Zani, JL; Zeitoun, R; Zeng, N; Zenteno, JC; Zepeda-Palacio, C; Zhai, C; Zhang, B; Zhang, G; Zhang, J; Zhang, K; Zhang, Q; Zhang, R; Zhang, T; Zhang, X; Zhang, Y; Zhang, YY; Zhao, B; Zhao, D; Zhao, G; Zhao, H; Zhao, Q; Zhao, R; Zhao, S; Zhao, T; Zhao, X; Zhao, XA; Zhao, Y; Zhao, Z; Zheng, Z; Zhi-Min, G; Zhou, CL; Zhou, HD; Zhou, J; Zhou, W; Zhou, XQ; Zhou, Z; Zhu, C; Zhu, H; Zhu, L; Zhu, Y; Zitzmann, N; Zou, L; Zou, Y, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
glycosideA glycosyl compound resulting from the attachment of a glycosyl group to a non-acyl group RO-, RS-, RSe-, etc. The bond between the glycosyl group and the non-acyl group is called a glycosidic bond. By extension, the terms N-glycosides and C-glycosides are used as class names for glycosylamines and for compounds having a glycosyl group attached to a hydrocarbyl group respectively. These terms are misnomers and should not be used. The preferred terms are glycosylamines and C-glycosyl compounds, respectively.
glycosideA glycosyl compound resulting from the attachment of a glycosyl group to a non-acyl group RO-, RS-, RSe-, etc. The bond between the glycosyl group and the non-acyl group is called a glycosidic bond. By extension, the terms N-glycosides and C-glycosides are used as class names for glycosylamines and for compounds having a glycosyl group attached to a hydrocarbyl group respectively. These terms are misnomers and should not be used. The preferred terms are glycosylamines and C-glycosyl compounds, respectively.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (28)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency1.25890.707936.904389.1251AID504333
IDH1Homo sapiens (human)Potency18.35640.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency12.58930.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency79.43280.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency29.09290.004611.374133.4983AID624297
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.505710.0000AID270052
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.497310.0000AID270052
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.498810.0000AID270052
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.504610.0000AID270052
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.506510.0000AID270052
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.505710.0000AID270052
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)1.90000.00010.507510.0000AID270052
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)Ki39.70001.19105.12919.9410AID1802951
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7Homo sapiens (human)AC5050.00000.039815.002550.0000AID743267
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
pentose-phosphate shuntGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
lipid metabolic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
cholesterol biosynthetic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
NADP metabolic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
NADPH regenerationGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
glutathione metabolic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
pentose-phosphate shunt, oxidative branchGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
response to iron(III) ionGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
negative regulation of protein glutathionylationGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
response to organic cyclic compoundGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
pentose biosynthetic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
substantia nigra developmentGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
response to foodGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
cellular response to oxidative stressGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
erythrocyte maturationGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
regulation of neuron apoptotic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
response to ethanolGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
ribose phosphate biosynthetic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
glucose 6-phosphate metabolic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
negative regulation of cell growth involved in cardiac muscle cell developmentGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
positive regulation of calcium ion transmembrane transport via high voltage-gated calcium channelGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
negative regulation of reactive oxygen species metabolic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
glucose metabolic processGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
glucose-6-phosphate dehydrogenase activityGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
protein bindingGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
glucose bindingGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
identical protein bindingGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
protein homodimerization activityGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
NADP bindingGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
cytosolGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
cytoplasmic side of plasma membraneGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
membraneGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
centriolar satelliteGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
intracellular membrane-bounded organelleGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
extracellular exosomeGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
cytosolGlucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID286350Displacement of [3H]muscimol from GABAA receptor in Sprague-Dawley rat spinal cord brainstem membranes2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and gamma-aminobutyric acid receptors.
AID270053Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat cerebral cortex2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID286349Displacement of [3H]strychnine from glycine receptor in rat spinal cord synaptosomal membranes2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and gamma-aminobutyric acid receptors.
AID286351Displacement of [3H]muscimol from GABAA receptor in Sprague-Dawley rat cerebral cortex membranes2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and gamma-aminobutyric acid receptors.
AID270051Displacement of [3H]strychnine from strychnine-sensitive glycine receptor in rat spinal cord2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID270052Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat spinal cord2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
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
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.
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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1802951In Vitro Inhibition Assay from Article 10.3109/14756360903489581: \\Effects of some drugs on human erythrocyte glucose 6-phosphate dehydrogenase: an in vitro study.\\2010Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 25, Issue:6
Effects of some drugs on human erythrocyte glucose 6-phosphate dehydrogenase: an in vitro study.
[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-199017 (14.29)18.7374
1990's11 (9.24)18.2507
2000's26 (21.85)29.6817
2010's50 (42.02)24.3611
2020's15 (12.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 91.52

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

MetricThis Compound (vs All)
Research Demand Index91.52 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.35 (4.65)
Search Engine Demand Index158.33 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (91.52)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials21 (16.80%)5.53%
Reviews0 (0.00%)6.00%
Reviews3 (2.40%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies23 (18.40%)4.05%
Observational0 (0.00%)0.25%
Observational3 (2.40%)0.25%
Other11 (100.00%)84.16%
Other75 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]