Page last updated: 2024-12-06

bepafant

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

Description

bepafant: RN given from Toxlit 6/90; PAF antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65923
CHEMBL ID325439
SCHEMBL ID94512
MeSH IDM0176382

Synonyms (25)

Synonym
6-(2-chlorophenyl)-1-methyl-8,9-dihydro-4h,7h-cyclopenta[4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-9-yl-1,4-oxazinan-4-ylmethanone (web 2170)
bdbm50038755
4-((6-(o-chlorophenyl)-8,9-dihydro-1-methyl-4h,7h-cyclopenta(4,5)thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepin-8-yl)carbonyl)morpholine
bepafant
bepafant [inn]
web-2170
bepafanto [inn-spanish]
web 2170
web2170
114776-28-2
CHEMBL325439
unii-cks724b66o
bepafanto
cks724b66o ,
gtpl6078
SCHEMBL94512
bepafant [mart.]
bepafant o
Q27075103
[9-(2-chlorophenyl)-3-methyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaen-13-yl]-morpholin-4-ylmethanone
(6-(2-chlorophenyl)-1-methyl-8,9-dihydro-4h,7h-cyclopenta[4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-8-yl)(morpholino)methanone
sty 2108
DTXSID10869589
[6-(2-chlorophenyl)-1-methyl-8,9-dihydro-4h,7h-cyclopenta[4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-8-yl](morpholin-4-yl)methanone
AKOS040747948

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The toxic effect was observed only in mice with a cryptococcal infection and was reduced or absent in the early and late stages of disease."( Acute lethal toxicity following passive immunization for treatment of murine cryptococcosis.
Kozel, TR; Lupan, DM; Manalo, PB; Roberts, JS; Savoy, AC; Schlageter, AM; Weinhold, LC, 1997
)
0.3

Dosage Studied

ExcerptRelevanceReference
"Dissolution testing of solid oral dosage forms plays a very important part both in the development of new products and in quality control."( The automation of dissolution testing of solid oral dosage forms.
Lamparter, E; Lunkenheimer, CH,
)
0.13
" Although lower WEB 2170 doses prevented NEC, neither fourfold higher dosing with WEB 2170 nor similar dosing with WEB 2086 affected the incidence of disease in this study."( The platelet-activating factor receptor antagonist WEB 2170 prevents neonatal necrotizing enterocolitis in rats.
Adler, L; Caplan, MS; Hedlund, E; Hsueh, W; Lickerman, M, 1997
)
0.3
[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)
Platelet-activating factor receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.07300.00430.75777.8000AID157890; AID165616
Platelet-activating factor receptorCavia porcellus (domestic guinea pig)Ki0.02920.00040.33863.2500AID154449
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID157890In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel antagonists of platelet-activating factor. 2. Synthesis and structure-activity relationships of potent and long-acting heterofused [1,5]benzodiazepine and [1,4]diazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.
AID165616Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel antagonists of platelet-activating factor. 1. Synthesis and structure-activity relationships of benzodiazepine and benzazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.
AID176972In vivo antagonist activity for PAF-Induced cutaneous vascular permeability in the rat1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.
AID132753In vivo antagonist activity against PAF-Induced paw edema in the mouse1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.
AID112370The compound was tested for their ability to protect mice from lethal effects after administration of PAF (Platelet-Activating Factor)1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel antagonists of platelet-activating factor. 1. Synthesis and structure-activity relationships of benzodiazepine and benzazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.
AID19918Duration of action in Conscious Dog at 0.1 mg/kg po1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel antagonists of platelet-activating factor. 2. Synthesis and structure-activity relationships of potent and long-acting heterofused [1,5]benzodiazepine and [1,4]diazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.
AID112368Ability to protect mice from lethal effects after administration of PAF (Platelet-Activating Factor)1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel antagonists of platelet-activating factor. 2. Synthesis and structure-activity relationships of potent and long-acting heterofused [1,5]benzodiazepine and [1,4]diazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.
AID154449Antagonist activity against platelet activating factor (PAF) receptor in rabbit platelet membranes using [3H]C18-PAF as radioligand1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.
AID1346403Human PAF receptor (Platelet-activating factor receptor)1990The Journal of pharmacology and experimental therapeutics, Oct, Volume: 255, Issue:1
Pharmacological actions of PCA 4248, a new platelet-activating factor receptor antagonist: in vivo studies.
AID1346403Human PAF receptor (Platelet-activating factor receptor)1990The Journal of pharmacology and experimental therapeutics, Dec, Volume: 255, Issue:3
Pharmacologic activity of bepafant (WEB 2170), a new and selective hetrazepinoic antagonist of platelet activating factor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (161)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's118 (73.29)18.2507
2000's37 (22.98)29.6817
2010's6 (3.73)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%
Reviews4 (2.30%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other170 (97.70%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]