Page last updated: 2024-11-06

spiroglumide

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

Description

Spiroglumide is a synthetic non-peptide compound that acts as a selective antagonist of the cholecystokinin (CCK) receptor. It was originally synthesized in the 1970s as a potential anti-ulcer drug. Spiroglumide has been studied for its potential therapeutic effects in a range of conditions, including gastrointestinal disorders, obesity, and cancer. It has been shown to inhibit gastric acid secretion, reduce appetite, and induce apoptosis in cancer cells. Its importance lies in its unique ability to target CCK receptors, which are involved in various physiological processes, making it a promising candidate for drug development in different therapeutic areas.'

spiroglumide: a CCK receptor antagonist; antigastrin; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65987
CHEMBL ID283820
SCHEMBL ID7920324
MeSH IDM0206819

Synonyms (17)

Synonym
(r)-5-(8-aza-spiro[4.5]dec-8-yl)-4-(3,5-dichloro-benzoylamino)-5-oxo-pentanoic acid
bdbm50048772
spiroglumide
CHEMBL283820 ,
cr-2194
(4r)-5-(8-azaspiro[4.5]decan-8-yl)-4-[(3,5-dichlorobenzoyl)amino]-5-oxopentanoic acid
8-azaspiro(4.5)decane-8-pentanoic acid, gamma-((3,5-dichlorobenzoyl)amino)-delta-oxo-, (r)-
ezs5v8un4y ,
(r)-gamma-(3,5-dichlorobenzamido)-delta-oxo-8-azaspiro(4.5)decane-8-valeric acid
unii-ezs5v8un4y
spiroglumide [inn]
137795-35-8
(r)-5-(8-azaspiro[4.5]decan-8-yl)-4-(3,5-dichloro-benzoylamino)-5-oxopentanoic acid
FJCZHMXAGBYXHJ-QGZVFWFLSA-N
SCHEMBL7920324
DTXSID60160311
Q27277451
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50 (µMol)13.50000.00000.43624.3000AID52914
Gastrin/cholecystokinin type B receptorHomo sapiens (human)IC50 (µMol)1.31150.00010.36154.0000AID165466; AID50687
Platelet-activating factor acetylhydrolaseHomo sapiens (human)IC50 (µMol)1.22300.00000.38373.9000AID165466
P2Y purinoceptor 12Homo sapiens (human)IC50 (µMol)1.22300.00041.048910.0000AID165466
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (44)

Processvia Protein(s)Taxonomy
gastric acid secretionGastrin/cholecystokinin type B receptorHomo sapiens (human)
cell surface receptor signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationGastrin/cholecystokinin type B receptorHomo sapiens (human)
positive regulation of cell population proliferationGastrin/cholecystokinin type B receptorHomo sapiens (human)
cholecystokinin signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
pH reductionGastrin/cholecystokinin type B receptorHomo sapiens (human)
digestive tract developmentGastrin/cholecystokinin type B receptorHomo sapiens (human)
gland developmentGastrin/cholecystokinin type B receptorHomo sapiens (human)
peptide hormone processingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particle remodelingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
lipid oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
plasma lipoprotein particle oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phosphatidylcholine catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor metabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of inflammatory responsePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of monocyte chemotaxisPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
monoatomic ion transportP2Y purinoceptor 12Homo sapiens (human)
substrate-dependent cell migration, cell extensionP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
hemostasisP2Y purinoceptor 12Homo sapiens (human)
calcium-mediated signalingP2Y purinoceptor 12Homo sapiens (human)
cerebral cortex radial glia-guided migrationP2Y purinoceptor 12Homo sapiens (human)
cell projection organizationP2Y purinoceptor 12Homo sapiens (human)
lamellipodium assemblyP2Y purinoceptor 12Homo sapiens (human)
platelet activationP2Y purinoceptor 12Homo sapiens (human)
positive regulation of integrin activation by cell surface receptor linked signal transductionP2Y purinoceptor 12Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
positive regulation of monoatomic ion transportP2Y purinoceptor 12Homo sapiens (human)
response to axon injuryP2Y purinoceptor 12Homo sapiens (human)
regulation of chemotaxisP2Y purinoceptor 12Homo sapiens (human)
positive regulation of chemotaxisP2Y purinoceptor 12Homo sapiens (human)
establishment of localization in cellP2Y purinoceptor 12Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionP2Y purinoceptor 12Homo sapiens (human)
platelet aggregationP2Y purinoceptor 12Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 12Homo sapiens (human)
visual system developmentP2Y purinoceptor 12Homo sapiens (human)
positive regulation of ruffle assemblyP2Y purinoceptor 12Homo sapiens (human)
regulation of microglial cell migrationP2Y purinoceptor 12Homo sapiens (human)
positive regulation of microglial cell migrationP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
cholecystokinin receptor activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
protein bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
gastrin receptor activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
peptide hormone bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
type B gastrin/cholecystokinin receptor bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
1-phosphatidylinositol-3-kinase regulator activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
1-alkyl-2-acetylglycerophosphocholine esterase activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phospholipid bindingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
hydrolase activity, acting on ester bondsPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
calcium-independent phospholipase A2 activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
G protein-coupled adenosine receptor activityP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled ADP receptor activityP2Y purinoceptor 12Homo sapiens (human)
guanyl-nucleotide exchange factor activityP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
plasma membraneGastrin/cholecystokinin type B receptorHomo sapiens (human)
intracellular membrane-bounded organelleGastrin/cholecystokinin type B receptorHomo sapiens (human)
plasma membraneGastrin/cholecystokinin type B receptorHomo sapiens (human)
extracellular regionPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
high-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
plasma membraneP2Y purinoceptor 12Homo sapiens (human)
cell surfaceP2Y purinoceptor 12Homo sapiens (human)
membraneP2Y purinoceptor 12Homo sapiens (human)
cell projection membraneP2Y purinoceptor 12Homo sapiens (human)
cell body membraneP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID232286Concentration required to inhibit CCK-A receptor/ Concentration required to inhibit CCK-B receptor1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives.
AID52914Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives.
AID165466In vitro inhibition of gastrin-induced [Ca2+] cytosolic elevation in isolated rabbit parietal cells1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives.
AID50687Inhibition of binding of [3H]N-Me-N-Leu-CCK-8 to cholecystokinin type B receptor in guinea pig brain cortex1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's6 (100.00)18.2507
2000's0 (0.00)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: 12.25

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

MetricThis Compound (vs All)
Research Demand Index12.25 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (14.29%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (71.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]