Page last updated: 2024-12-06

girisopam

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

Girisopam is a novel, selective, and orally bioavailable positive allosteric modulator (PAM) of the α5 subunit-containing GABA type A receptors (α5 GABAA receptors). It is being investigated for the treatment of cognitive impairment in Alzheimer's disease. In preclinical studies, girisopam has been shown to improve memory and learning in animal models of Alzheimer's disease. It is believed that girisopam's mechanism of action involves enhancing the function of α5 GABAA receptors, which are known to play a role in cognitive processes. The compound is currently in clinical trials for the treatment of Alzheimer's disease.'

Cross-References

ID SourceID
PubMed CID71257
CHEMBL ID1915065
SCHEMBL ID637118
MeSH IDM0132119

Synonyms (21)

Synonym
nsc-373736
82230-53-3
nsc373736
1-(m-chlorophenyl)-7,8-dimethoxy-4-methyl-5h-2,3-benzodiazepine
brn 5596125
girisopam
1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5h-2,3-benzodiazepine
gyki 51189
5h-2,3-benzodiazepine, 1-(3-chlorophenyl)-7,8-dimethoxy-4-methyl-
girisopam [inn]
girisopamum [inn-latin]
1-(3-chlorophenyl)-7,8-dimethoxy-4-methyl-5h-2,3-benzodiazepine
2lp301a921 ,
unii-2lp301a921
nsc 373736
girisopamum
CHEMBL1915065 ,
bdbm50356876
SCHEMBL637118
DTXSID70231642
Q3491663

Research Excerpts

Overview

Girisopam (EGIS-5810) is a potent anxiolytic compound.

ExcerptReferenceRelevance
"Girisopam (EGIS-5810) is a potent anxiolytic compound. "( Study of the bone marrow penetration of radioactivity after oral administration of radiolabelled girisopam (EGIS-5810) in mice.
Dereszlay, I; Klebovich, I; Pátfalusi, M,
)
1.79

Pharmacokinetics

ExcerptReferenceRelevance
" A high-performance liquid chromatographic method has been developed for studying girisopam in single-dose pharmacokinetic studies."( Pharmacokinetic and metabolism studies on girisopam by chromatographic and spectrometric methods in humans.
Horváth, G; Mészáros, S; Pátfalusi, M; Tomori, E; Vereczkey, L, 1992
)
0.77
[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)
cGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)IC50 (µMol)12.50000.00331.624010.0000AID628756
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (1)

Processvia Protein(s)Taxonomy
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID628753Inhibition of bovine aortic PDE1 using calmodulin activated cGMP as substrate2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
AID628756Inhibition of bovine aortic PDE5 using cGMP as substrate in presence of EGTA2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
AID628759Inhibition of bovine aortic PDE3 using cAMP as substrate at 10 uM in presence of rolipram2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
AID628752Inhibition of bovine aortic PDE4 using cAMP as substrate in presence of cGMP2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
AID628754Inhibition of bovine aortic endothelial cells PDE2 using cAMP as substrate in presence of cGMP2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (18.18)18.7374
1990's8 (72.73)18.2507
2000's0 (0.00)29.6817
2010's1 (9.09)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: 12.24

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 Index12.24 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.80 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.24)

All Compounds (24.57)

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%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]