Page last updated: 2024-12-08

sk&f 100330-a

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

Description

SK&F 100330-A: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID134985
CHEMBL ID103623
SCHEMBL ID5162505
MeSH IDM0132507

Synonyms (14)

Synonym
skf-100330a
CHEMBL103623 ,
3-pyridinecarboxylic acid, 1-(4,4-diphenyl-3-butenyl)-1,2,5,6-tetrahydro-
85375-88-8
bdbm50020882
1-(4,4-diphenylbut-3-enyl)-1,2,5,6-tetrahydropyridine-3-carboxylic acid
1-(4,4-diphenyl-but-3-enyl)-1,2,5,6-tetrahydro-pyridine-3-carboxylic acid
sk&f 100330-a
n-(4,4-diphenyl-3-butenyl)guvacine
SCHEMBL5162505
n-[4,4-diphenyl-3-butenyl]-guvacine
1-(4,4-diphenylbut-3-en-1-yl)-1,2,5,6-tetrahydropyridine-3-carboxylic acid
DTXSID801005837
3-pyridinecarboxylic acid,1-(4,4-diphenyl-3-butenyl)-1,2,5,6-tetrahyd ro-

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Observation of behaviour indicated that the novel GABA uptake blockers exerted no side-effects in anticonvulsant doses, whereas diazepam produced sedative effects at all active dosage levels."( Comparison of the anticonvulsant effects of two novel GABA uptake inhibitors and diazepam in amygdaloid kindled rats.
Löscher, W; Schwark, WS, 1985
)
0.27
[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- and chloride-dependent GABA transporter 1Homo sapiens (human)IC50 (µMol)0.20000.01013.090310.0000AID487219
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
memorySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
associative learningSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
synapse organizationSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
chemical synaptic transmissionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to toxic substanceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to sucroseSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to inorganic substanceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to lead ionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to purine-containing compoundSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to estradiolSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to cocaineSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to calcium ionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid importSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
inorganic anion import across plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium ion import across plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
transport across blood-brain barrierSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
chloride transmembrane transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
amino acid transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
protein bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
identical protein bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
metal ion bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
axonSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
presynaptic membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
neuronal cell bodySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
postsynaptic membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
GABA-ergic synapseSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
axonSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
cell surfaceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID73508Percent inhibition of Gamma-amino-N-butyrate transaminase from rat was evaluated1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID40836Percent inhibition of [3H]- Diazepam binding to GABA-A Benzodiazepine receptor of rat frontal cortex membranes1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID487219Binding affinity to GAT12010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.
AID74548Percent inhibition of Glutamate decarboxylase from rat was evaluated1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID179937Inhibition of GABA uptake from rat diencephalon-midbrain,1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID179941Inhibition of Norepinephrine uptake from rat diencephalon-midbrain1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID71450Displacement of [3H]- muscimol from GABA-A receptor from rat cerebellum membrane at 100 uM1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-199010 (52.63)18.7374
1990's7 (36.84)18.2507
2000's1 (5.26)29.6817
2010's1 (5.26)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: 11.09

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 Index11.09 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index4.13 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.09)

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%
Other20 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]