Page last updated: 2024-11-11

sabiporide

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

Description

sabiporide: a NHE-1 inhibitor and a cardioprotective agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9868115
CHEMBL ID2105423
SCHEMBL ID1286662
MeSH IDM0452989

Synonyms (19)

Synonym
n-(diaminomethylidene)-4-[4-(1h-pyrrole-2-carbonyl)piperazin-1-yl]-3-(trifluoromethyl)benzamide
unii-u52apa00x7
biib 722
n-carbamimidoyl-4-(4-(1h-pyrrol-2-ylcarbonyl)piperazin-1-yl)-3-(trifluoromethyl)benzamide
sabiporide hcl
sabiporide [inn]
biib722
324758-66-9
biib 722cl
u52apa00x7 ,
biib-722
sabiporide
CHEMBL2105423
bdbm50396462
4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine
SCHEMBL1286662
261505-80-0
Q27290695
DTXSID00870321

Research Excerpts

Treatment

Treatment with sabiporide significantly attenuated the increase in PAP by 38% and PVR by 67%, as well as significantly improved cardiac output by 51%. SabipOride treatment also improved mixed venous blood oxygen saturation.

ExcerptReferenceRelevance
"Sabiporide treatment also improved mixed venous blood oxygen saturation (55% in sabiporide group vs."( Sabiporide improves cardiovascular function, decreases the inflammatory response and reduces mortality in acute metabolic acidosis in pigs.
Abraham, WM; Kraut, JA; Wu, D, 2013
)
2.55
"Treatment with sabiporide significantly attenuated the increase in PAP by 38% and PVR by 67%, as well as significantly improved cardiac output by 51%."( Sabiporide improves cardiovascular function, decreases the inflammatory response and reduces mortality in acute metabolic acidosis in pigs.
Abraham, WM; Kraut, JA; Wu, D, 2013
)
2.17

Pharmacokinetics

ExcerptReferenceRelevance
" In this study, we characterized the pharmacodynamic properties of new guanidine NHE1 inhibitors (cariporide, sabiporide, KR-32511, KR-32570, and KR-33028) to analyze their myocardial protective effects."( Pharmacodynamic characteristics and cardioprotective effects of new NHE1 inhibitors.
Han, W; Jung, YS; Kim, J; Kim, KH; Kim, MY; Lee, BH; Lee, MG; Namkung, W; Yi, KY; Yoo, SE, 2007
)
0.55
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium/hydrogen exchanger 1Homo sapiens (human)IC50 (µMol)0.02800.00500.56013.5000AID701661
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (40)

Processvia Protein(s)Taxonomy
monoatomic ion transportSodium/hydrogen exchanger 1Homo sapiens (human)
intracellular sodium ion homeostasisSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of pHSodium/hydrogen exchanger 1Homo sapiens (human)
response to acidic pHSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of cardiac muscle hypertrophySodium/hydrogen exchanger 1Homo sapiens (human)
regulation of cardiac muscle contraction by calcium ion signalingSodium/hydrogen exchanger 1Homo sapiens (human)
cell migrationSodium/hydrogen exchanger 1Homo sapiens (human)
maintenance of cell polaritySodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of cell growthSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to insulin stimulusSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilitySodium/hydrogen exchanger 1Homo sapiens (human)
response to muscle stretchSodium/hydrogen exchanger 1Homo sapiens (human)
sodium ion export across plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of apoptotic processSodium/hydrogen exchanger 1Homo sapiens (human)
negative regulation of apoptotic processSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of action potentialSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISodium/hydrogen exchanger 1Homo sapiens (human)
stem cell differentiationSodium/hydrogen exchanger 1Homo sapiens (human)
protein complex oligomerizationSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of intracellular pHSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of stress fiber assemblySodium/hydrogen exchanger 1Homo sapiens (human)
regulation of focal adhesion assemblySodium/hydrogen exchanger 1Homo sapiens (human)
cardiac muscle cell differentiationSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to coldSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of calcineurin-NFAT signaling cascadeSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to antibioticSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to electrical stimulusSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to mechanical stimulusSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to organic cyclic compoundSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to hypoxiaSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to acidic pHSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to epinephrine stimulusSodium/hydrogen exchanger 1Homo sapiens (human)
cardiac muscle cell contractionSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of cardiac muscle cell membrane potentialSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of the force of heart contraction by cardiac conductionSodium/hydrogen exchanger 1Homo sapiens (human)
sodium ion import across plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of the force of heart contractionSodium/hydrogen exchanger 1Homo sapiens (human)
proton transmembrane transportSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of calcium:sodium antiporter activitySodium/hydrogen exchanger 1Homo sapiens (human)
potassium ion transmembrane transportSodium/hydrogen exchanger 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
protein bindingSodium/hydrogen exchanger 1Homo sapiens (human)
calmodulin bindingSodium/hydrogen exchanger 1Homo sapiens (human)
phospholipid bindingSodium/hydrogen exchanger 1Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingSodium/hydrogen exchanger 1Homo sapiens (human)
sodium:proton antiporter activitySodium/hydrogen exchanger 1Homo sapiens (human)
protein phosphatase 2B bindingSodium/hydrogen exchanger 1Homo sapiens (human)
protein-macromolecule adaptor activitySodium/hydrogen exchanger 1Homo sapiens (human)
identical protein bindingSodium/hydrogen exchanger 1Homo sapiens (human)
calcium-dependent protein bindingSodium/hydrogen exchanger 1Homo sapiens (human)
molecular adaptor activitySodium/hydrogen exchanger 1Homo sapiens (human)
sodium:proton antiporter activity involved in regulation of cardiac muscle cell membrane potentialSodium/hydrogen exchanger 1Homo sapiens (human)
potassium:proton antiporter activitySodium/hydrogen exchanger 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
nucleoplasmSodium/hydrogen exchanger 1Homo sapiens (human)
cytoplasmSodium/hydrogen exchanger 1Homo sapiens (human)
mitochondrionSodium/hydrogen exchanger 1Homo sapiens (human)
plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
focal adhesionSodium/hydrogen exchanger 1Homo sapiens (human)
cell surfaceSodium/hydrogen exchanger 1Homo sapiens (human)
intercalated discSodium/hydrogen exchanger 1Homo sapiens (human)
membraneSodium/hydrogen exchanger 1Homo sapiens (human)
basolateral plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
apical plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
lamellipodiumSodium/hydrogen exchanger 1Homo sapiens (human)
T-tubuleSodium/hydrogen exchanger 1Homo sapiens (human)
membrane raftSodium/hydrogen exchanger 1Homo sapiens (human)
perinuclear region of cytoplasmSodium/hydrogen exchanger 1Homo sapiens (human)
extracellular exosomeSodium/hydrogen exchanger 1Homo sapiens (human)
cation-transporting ATPase complexSodium/hydrogen exchanger 1Homo sapiens (human)
plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID701655Inhibition of CYP3A4 in human liver microsomes using 7-benzyloxy-4-(trifluoromethyl)-coumarin as substrate after 30 mins by LC/MS/MS analysis2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
AID701661Inhibition of NHE1 in human HT-29 cells assessed as intracellular pH change after 30 mins2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
AID701665Clearance in jugular and femoral vein precannulated Sprague-Dawley rat at 1 mg/kg, iv by LC/MS/MS analysis relative to hepatic blood flow2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
AID701658Inhibition of CYP2C19 in human liver microsomes using 7-ethoxy-3-cyanocoumarin as substrate after 45 mins by LC/MS/MS analysis2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
AID701663Volume of distribution at steady state in jugular and femoral vein precannulated Sprague-Dawley rat at 1 mg/kg, iv by LC/MS/MS analysis2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
AID701664Mean resident time in jugular and femoral vein precannulated Sprague-Dawley rat at 1 mg/kg, iv by LC/MS/MS analysis2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
AID701660Inhibition of NHE1 in human platelet rich plasma assessed as reduction of propionate medium induced platelet swelling measured every 6 secs for 5 mins2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
AID701662Oral bioavailability in jugular and femoral vein precannulated Sprague-Dawley rat plasma at 5 mg/kg by LC/MS/MS analysis2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (46.67)29.6817
2010's8 (53.33)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]