Page last updated: 2024-11-10

awd 131-138

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

Description

AWD 131-138: a GABA-A receptor partial agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3083511
CHEMBL ID204240
SCHEMBL ID1645360
MeSH IDM0299072

Synonyms (49)

Synonym
imepitoin [inn]
1-(4-chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2h-imidazol-2-one
2h-imidazol-2-one, 1-(4-chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-
imepition
1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one
19v39682li ,
unii-19v39682li
188116-07-6
awd-131-138
elb-138
add-233089
imepitoin
CHEMBL204240
awd131-138
pexion
awd 131-138
3-(4-chlorophenyl)-5-morpholin-4-yl-4h-imidazol-2-one
1-(4-chlorophenyl)-4-(morpholin-4-yl)-1,5-dihydro-2h-imidazol-2-one
imepitoin [mi]
imepitoin [ema epar veterinary]
1-(4-chlorophenyl)-4-morpholin-4-yl-5h-imidazol-2-one
S5319
HY-14953
CS-1733
SCHEMBL1645360
AKOS024258133
1-(4-chlorophenyl)-4-morpholino-1h-imidazol-2(5h)-one
1-(4-chlorophenyl)-4-morpholino-1,5-dihydro-2h-imidazol-2-one
DTXSID50172160 ,
J-690252
EX-A261
1-(4-chlorophenyl)-4-(morpholin-4-yl)-2,5-dihydro-1h-imidazol-2-one
AS-72354
NCGC00371144-03
awd 131-138(imepitoin)
FT-0700248
BCP08396
A13726
HMS3886O19
CCG-267239
NCGC00371144-02
Q27252133
3-(4-chlorophenyl)-5-morpholino-4h-imidazol-2-one
imepitoin (ema epar veterinary)
imepitoine
imepitoinum
imepitoina
dtxcid0094651
AC-36287

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The frequency of adverse events including somnolence/sedation, polydipsia and increased appetite was significantly higher in the phenobarbital group."( Clinical efficacy and safety of imepitoin in comparison with phenobarbital for the control of idiopathic epilepsy in dogs.
de Vries, F; Keefe, TJ; Löscher, W; Rundfeldt, C; Tipold, A, 2015
)
0.42
" The frequency of dogs with any adverse drug reactions was higher in the 30 mg/kg BID dose (59 % vs."( Efficacy, safety, and tolerability of imepitoin in dogs with newly diagnosed epilepsy in a randomized controlled clinical study with long-term follow up.
Löscher, W; Rundfeldt, C; Tipold, A, 2015
)
0.42
" Most CNS related adverse drug reactions were transient."( Efficacy, safety, and tolerability of imepitoin in dogs with newly diagnosed epilepsy in a randomized controlled clinical study with long-term follow up.
Löscher, W; Rundfeldt, C; Tipold, A, 2015
)
0.42

Pharmacokinetics

ExcerptReferenceRelevance
" In a crossover study, co-administration of imepitoin tablets with food reduced the total AUC by 30%, but it did not result in significant changes in Tmax and Cmax , indicating lack of clinical relevance."( Imepitoin as novel treatment option for canine idiopathic epilepsy: pharmacokinetics, distribution, and metabolism in dogs.
Gasparic, A; Rundfeldt, C; Wlaź, P, 2014
)
0.4

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model."( Anticonvulsant efficacy of the low-affinity partial benzodiazepine receptor agonist ELB 138 in a dog seizure model and in epileptic dogs with spontaneously recurrent seizures.
Löscher, W; Potschka, H; Rieck, S; Rundfeldt, C; Tipold, A, 2004
)
0.32
" Based on these data, imepitoin can be dosed twice daily, but the timing of tablet administration in relation to feeding should be kept consistent."( Imepitoin as novel treatment option for canine idiopathic epilepsy: pharmacokinetics, distribution, and metabolism in dogs.
Gasparic, A; Rundfeldt, C; Wlaź, P, 2014
)
0.4
" The dosage of imepitoin was increased from 20 mg/kg twice daily to 30 mg/kg twice daily, 3 days before the onset of skin lesions, due to uncontrolled seizures."( Cutaneous adverse drug reaction in a dog associated with imepitoin.
Bhatti, S; De Cock, H; Kitshoff, A; Royaux, E; Van Ham, L; Vandenabeele, S, 2016
)
0.43
" Future work may evaluate optimal dosage regimens."( Evaluation of Pexion
Dixit, V; Emke, C; Griffith, EH; Gruen, ME; Johnson, B; Perdew, I; Song, Y; Watson, P, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (17)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency31.62280.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki4.35000.00020.656110.0000AID261133
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki4.35000.00020.656110.0000AID261133
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki4.35000.00020.656110.0000AID261133
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki4.35000.00020.561410.0000AID261133
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki4.35000.00020.635210.0000AID261133
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki4.35000.00020.621710.0000AID261133
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki4.35000.00020.675810.0000AID261133
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki4.35000.00020.646910.0000AID261133
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki4.35000.00020.656110.0000AID261133
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki4.35000.00020.656110.0000AID261133
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki4.35000.00020.671210.0000AID261133
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki4.35000.00020.557710.0000AID261133
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki4.35000.00020.640310.0000AID261133
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki4.35000.00020.570810.0000AID261133
GABA theta subunitRattus norvegicus (Norway rat)Ki4.35000.00020.656110.0000AID261133
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki4.35000.00020.656110.0000AID261133
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID261132Partition coefficient of the compound, log P2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
AID261143Plasma concentration in cynomolgus monkey at 30 mg/kg, po2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
AID261145Anxiolytic activity in CF1 mice after ip administration by PTZ test2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
AID261136Neurotoxicological activity in NMRI BR mice after ip administration by rotarod test2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
AID261133Binding affinity to Wistar rat benzodiazepine receptor2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
AID261140Protective index (PI=TD50/ED50) in rat after oral administration2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
AID261139Neurotoxicological activity in rat after oral administration by rotarod test2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
AID261146Neurotoxicological activity in CF1 mice after ip administration by rotarod test2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
AID261138Anxiolytic activity in rat after oral administration by vogel conflict test2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (33)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (3.03)18.2507
2000's5 (15.15)29.6817
2010's21 (63.64)24.3611
2020's6 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.69

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 Index11.69 (24.57)
Research Supply Index3.83 (2.92)
Research Growth Index5.52 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (32.35%)5.53%
Reviews2 (5.88%)6.00%
Case Studies1 (2.94%)4.05%
Observational0 (0.00%)0.25%
Other20 (58.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]