Page last updated: 2024-12-07

modipafant

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

Description

modipafant: structure given in first source ; PAF antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID129796
SCHEMBL ID6995473
MeSH IDM0197583
PubMed CID3047770
CHEMBL ID2105829
SCHEMBL ID93821
MeSH IDM0197583

Synonyms (44)

Synonym
uk-74505
modipafant racemate
3-pyridinecarboxylic acid, 4-(2-chlorophenyl)-1,4-dihydro-6-methyl-2-(4-(2-methyl-1h-imidazo(4,5-c)pyridin-1-yl)phenyl)-5-((2-pyridinylamino)carbonyl)-, ethyl ester
rac-modipafant
ethyl 4-(2-chlorophenyl)-6-methyl-2-[4-(2-methylimidazo[4,5-c]pyridin-1-yl)phenyl]-5-(pyridin-2-ylcarbamoyl)-1,4-dihydropyridine-3-carboxylate
FT-0672447
3qk4u86953 ,
unii-3qk4u86953
122956-68-7
SCHEMBL6995473
modipafant, (+/-)-
4-(2-chlorophenyl)-5-(ethoxycarbonyl)-2-methyl-6-[4-(2-methyl-1h-imidazo[4,5-c]pyridin-1-yl)phenyl]-n-(pyridin-2-yl)-1,4-dihydropyridine-3-carboximidic acid
DTXSID10924329
Q27888306
(+/-)-modipafant
ethyl 4-(2-chlorophenyl)-6-methyl-2-(4-(2-methyl-1h-imidazo[4,5-c]pyridin-1-yl)phenyl)-5-(pyridin-2-ylcarbamoyl)-1,4-dihydropyridine-3-carboxylate
modipafant racemate; uk-74505; uk 74505; uk74505
BCP31819
MS-30665
CS-0031421
(rac)-modipafant
HY-108908
3-pyridinecarboxylic acid,4-(2-chlorophenyl)-1,4-dihydro-6-methyl-2-[4-(2-methyl-1h-imidazo[4,5-c]pyridin-1-yl)phenyl]-5-[(2-pyridinylamino)carbonyl]-, ethyl ester, (4r)-
modipafantracemate
AKOS040748952
ethyl 4-(2-chlorophenyl)-6-methyl-2-(4-{2-methylimidazo[4,5-c]pyridin-1-yl}phenyl)-5-[(pyridin-2-yl)carbamoyl]-1,4-dihydropyridine-3-carboxylate
modipafant
uk 80067
uk-80067
ethyl (4r)-4-(2-chlorophenyl)-6-methyl-2-[4-(2-methylimidazo[4,5-c]pyridin-1-yl)phenyl]-5-(pyridin-2-ylcarbamoyl)-1,4-dihydropyridine-3-carboxylate
CHEMBL2105829
1dmi0e5023 ,
ethyl (+)-(r)-4-(o-chlorophenyl)-1,4-dihydro-6-methyl-2-(p-(2-methyl-1h-imidazo(4,5-c)pyridin-1-yl)phenyl)-5-(2-pyridylcarbamoyl)nicotinate
122957-06-6
modipafant [inn:ban]
unii-1dmi0e5023
modipafant [inn]
SCHEMBL93821
DTXSID30153811
(r)-ethyl 4-(2-chlorophenyl)-6-methyl-2-(4-(2-methyl-1h-imidazo[4,5-c]pyridin-1-yl)phenyl)-5-(pyridin-2-ylcarbamoyl)-1,4-dihydropyridine-3-carboxylate
Q27252294
CS-0031431
HY-108908A
AKOS040753121

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Following oral administration to man, absorption was rapid with a mean value for Tmax of 1 h, and Cmax's ranging non-linearly from 90 to 2100 ng/ml following dosing at 12."( Modipafant, a new PAF antagonist: pharmacokinetics and disposition in rat, dog and man.
Jezequel, SG; Uden, S; Wastall, P, 1996
)
0.29

Dosage Studied

ExcerptRelevanceReference
" Following oral administration to man, absorption was rapid with a mean value for Tmax of 1 h, and Cmax's ranging non-linearly from 90 to 2100 ng/ml following dosing at 12."( Modipafant, a new PAF antagonist: pharmacokinetics and disposition in rat, dog and man.
Jezequel, SG; Uden, S; Wastall, P, 1996
)
0.29
[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)0.00430.00430.75777.8000AID157890; AID165614; AID165616
Platelet-activating factor receptorCavia porcellus (domestic guinea pig)Ki0.00710.00040.33863.2500AID154449
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID19906Duration of action in Conscious Dog at a dose of 0.075 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.
AID212971In vitro inhibition of thromboxane synthase (TXA2) in human platelet microsomes [reduced formation of TXB2 from prostaglandin H2(PGH2)]2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
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.
AID113143Ability to protect mice from lethal effects of an injection of PAF in vivo.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.
AID165614In vitro inhibition of PAF-induced aggregation of rabbit washed platelets.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.
AID114742Antagonism of Platelet activating factor (PAF)in mice after Intravenous administration, assayed by PAF-induced death2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
AID160937In vitro inhibition of platelet activating factor induced platelet aggregation in rabbit platelet rich plasma.2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Approach to dual-acting platelet activating factor (PAF) receptor antagonist/thromboxane synthase inhibitor (TxSI) based on the link of PAF antagonists and TxSIs.
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.
AID157733Displacement of [3H]nitrendipine from L-type calcium channel of bovine frontal cortex membranes.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.
AID212977Thromboxane synthase inhibitor (TxSI) activity was assessed by ex vivo inhibition of serum TXB2 production in rat after Intravenous administration; NT means not tested2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
AID113511Antagonism of Platelet activating factor (PAF) activity in mice after oral administration, assayed by PAF-induced death2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
AID59344Compound was tested ex vivo for its potency to inhibit PAF-induced whole blood aggregation in dog at 75 mg/kg (p.o.)1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.
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.
AID157731Displacement of [3H]desmethoxy-verapamil from L-type calcium channel of bovine frontal cortex membranes1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.
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.
AID212614In vitro inhibition of Thromboxane A2 synthase determined by inhibiting TXB2 production by incubating prostaglandin H2 (PGH-2) with human platelet microsomes; Not tested2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Approach to dual-acting platelet activating factor (PAF) receptor antagonist/thromboxane synthase inhibitor (TxSI) based on the link of PAF antagonists and TxSIs.
AID160940Tested in vitro for the inhibition of Platelet activating factor (PAF) induced platelet aggregation in rabbit platelet rich plasma (PRP); NT=Not tested2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
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.
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.
AID157732Displacement of [3H]-diltiazem from L-type calcium channel of bovine frontal cortex membranes.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.
AID213111Thromboxane synthase inhibitor (TxSI) activity was assessed by ex vivo inhibition of serum TXB2 production in rat after peroral administration; NT means not tested2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's18 (52.94)18.2507
2000's12 (35.29)29.6817
2010's4 (11.76)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: 17.49

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

MetricThis Compound (vs All)
Research Demand Index17.49 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials3 (10.34%)5.53%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
Other26 (89.66%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]