Page last updated: 2024-12-06

timoprazole

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

Description

Timoprazole is a proton pump inhibitor (PPI) used to treat gastroesophageal reflux disease (GERD) and other conditions associated with excess stomach acid. It is a synthetic compound with the chemical formula C16H17N3O2S. Timoprazole works by irreversibly blocking the enzyme H+/K+-ATPase, which is responsible for pumping hydrogen ions (H+) into the stomach, thereby reducing acid production. The synthesis of timoprazole involves several steps, including the formation of a benzimidazole ring and a sulfur-containing side chain. Timoprazole is effective in treating GERD, peptic ulcers, and Zollinger-Ellison syndrome. Its importance lies in its ability to provide long-lasting relief from acid-related symptoms. Timoprazole is studied to understand its pharmacokinetic properties, safety profile, and potential therapeutic applications. It is also investigated for its effects on other physiological processes.'

timoprazole: gastric acid secretion inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID72171
CHEMBL ID9861
SCHEMBL ID464728
MeSH IDM0115614

Synonyms (30)

Synonym
timoprazole (inn)
57237-97-5
D05900
h 83/69
timoprazole
CHEMBL9861 ,
2-(pyridin-2-ylmethylsulfinyl)-1h-benzimidazole
bdbm50018854
2-(pyridin-2-ylmethanesulfinyl)-1h-benzoimidazole(timoprazole)
2-(pyridin-2-ylmethanesulfinyl)-1h-benzoimidazole
timoprazole [inn]
timoprazol
2-((2-pyridylmethyl)sulfinyl)benzimidazole
timoprazolum
timoprazolum [inn-latin]
timoprazol [inn-spanish]
unii-95h6s1x9cc
95h6s1x9cc ,
SCHEMBL464728
HBDKFZNDMVLSHM-UHFFFAOYSA-N
2-(2-pyridylmethylsulfinyl)benzimidazole
2-[(2-pyridylmethyl)sulphinyl]benzimidazole
2-[(2-pyridinylmethyl)sulfinyl]-1h-benzimidazole
sr-01000944992
SR-01000944992-1
pyridylmethylsulfinyl benzimidazole
2-(2-pyridinylmethyl)sulfinyl]-1h-benzimidazole,
Q27271790
2-(2-pyridinylmethyl)sulfinyl]-1h-benzimidazole
DTXSID40866622

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Timoprazole pretreated with acid had inhibitory effects, but [3H] leucine incorporation experiments indicated that acidified timoprazole inhibited protein synthesis to some degree."( Inhibition of thyrocyte iodide uptake by H+K+ ATPase inhibitor, timoprazole.
Mori, T; Sugawa, H; Zhang, ML, 1995
)
1.25
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)309.03000.00011.753610.0000AID428564
Potassium-transporting ATPase alpha chain 1Homo sapiens (human)IC50 (µMol)130.00000.04001.09603.8000AID78730
Potassium-transporting ATPase subunit betaHomo sapiens (human)IC50 (µMol)130.00000.04001.09603.8000AID78730
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (33)

Processvia Protein(s)Taxonomy
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
response to xenobiotic stimulusPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
regulation of proton transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
monoatomic ion transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
pH reductionPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
intracellular sodium ion homeostasisPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
sodium ion export across plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
intracellular potassium ion homeostasisPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion import across plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
proton transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
cell adhesionPotassium-transporting ATPase subunit betaHomo sapiens (human)
response to organonitrogen compoundPotassium-transporting ATPase subunit betaHomo sapiens (human)
response to lipopolysaccharidePotassium-transporting ATPase subunit betaHomo sapiens (human)
pH reductionPotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium ion transmembrane transportPotassium-transporting ATPase subunit betaHomo sapiens (human)
proton transmembrane transportPotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium ion import across plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
intracellular potassium ion homeostasisPotassium-transporting ATPase subunit betaHomo sapiens (human)
sodium ion export across plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
intracellular sodium ion homeostasisPotassium-transporting ATPase subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
magnesium ion bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
ATP bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
P-type potassium:proton transporter activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
ATP hydrolysis activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
P-type sodium:potassium-exchanging transporter activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
protein bindingPotassium-transporting ATPase subunit betaHomo sapiens (human)
P-type potassium:proton transporter activityPotassium-transporting ATPase subunit betaHomo sapiens (human)
heterocyclic compound bindingPotassium-transporting ATPase subunit betaHomo sapiens (human)
ATPase activator activityPotassium-transporting ATPase subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
extracellular spacePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium:proton exchanging ATPase complexPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
apical plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium:proton exchanging ATPase complexPotassium-transporting ATPase subunit betaHomo sapiens (human)
apical plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
sodium:potassium-exchanging ATPase complexPotassium-transporting ATPase subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID165393Antisecretory effect in isolated rabbit gastric glands as measured by aminopyrine uptake1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.
AID78730In vitro inhibitory activity against H+/K+ ATPase prepared from canine fundic mucosa1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Substituted 2-[(2-benzimidazolylsulfinyl)methyl]anilines as potential inhibitors of H+/K+ ATPase.
AID78881Activity was evaluated by measuring the inhibition of isolated hog H+/K+ ATPase1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.
AID60720Inhibitory activity when administered intravenously in histamine-stimulated gastric fistula dog at 3 mg/kg, id1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Substituted 2-[(2-benzimidazolylsulfinyl)methyl]anilines as potential inhibitors of H+/K+ ATPase.
AID79073Inhibition of isolated rat H+/K+ ATPase.1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.
AID428564Inhibition of CYP3A42009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques.
AID177881Inhibition of acid secretion was determined by the compound administered subcutaneously in rats1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-199014 (70.00)18.7374
1990's4 (20.00)18.2507
2000's2 (10.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.66

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index25.66 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.08 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (9.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (90.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]