Page last updated: 2024-12-05

pca 4248

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

Description

PCA 4248: structure given in first source; platelet activating factor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4698
CHEMBL ID1395565
CHEBI ID91615
SCHEMBL ID10587428
MeSH IDM0181320

Synonyms (58)

Synonym
HMS3266M12
BRD-A29289453-001-02-1
BIO1_000954
BIO1_000465
BIO1_001443
BIO2_000817
BIO2_000337
BSPBIO_000994
IDI1_002092
ptemc
STK368865
methyl 2-(phenylsulfanyl)ethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate
NCGC00024658-02
NCGC00024658-03
KBIOGR_000334
KBIO2_000334
KBIO3_000667
KBIO2_005470
KBIOSS_000334
KBIO2_002902
KBIO3_000668
NCGC00024658-04
HMS1990B15
AKOS001610477
123875-01-4
pca-4248
HMS1362B15
HMS1792B15
3-o-methyl 5-o-(2-phenylsulfanylethyl) 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate
2-(phenylthio)ethyl-5-methoxycarbonyl-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
pca 4248
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,4,6-trimethyl-, methyl 2-(phenylthio)ethyl ester
3-(2-(phenylthio)ethyl)-5-methoxycarbonyl-4-methyl-2,6-dimethyl-1,4-dihydropyridine-3-carboxylate
gtpl6080
o5-methyl o3-(2-phenylsulfanylethyl) 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate
AKOS022067894
SCHEMBL10587428
1,4-dihydro-2,4,6-trimethyl-3,5-pyridinedicarboxylic acid methyl 2-(phenylthio)ethyl ester
CHEMBL1395565
DHCNAWNKZMNTIS-UHFFFAOYSA-N
pyridine-3, 5-dicarboxylic acid, 1,4-dihydro-2,4,6-trimethyl-, methyl 2-phenylthioethyl ester
3-methyl 5-[2-(phenylsulfanyl)ethyl] 2,4,6-trimethyl-1,4-dihydro-3,5-pyridinedicarboxylate #
HMS3403B15
HMS3428G07
J-004992
SR-01000597713-1
sr-01000597713
CHEBI:91615
DTXSID60924617
3-methyl 5-(2-(phenylthio)ethyl) 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate
HMS3675G04
Q27088253
pca4248
pca-4248;pca 4248
HMS3411G04
2-phenylsulfanylethyl methyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-d icarboxylate
BRD-A29289453-001-03-9
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,4,6-trimethyl-, 3-methyl 5-[2-(phenylthio)ethyl] ester

Research Excerpts

Actions

ExcerptReferenceRelevance
"PCA 4248 blocked the increase in the number of neutrophils, eosinophils and mononuclear cells observed 6 h after the i.t."( Interference of the PAF receptor antagonist, PCA 4248, with the rat pleurisy evoked by inflammatory mediators or allergen.
Bozza, PT; Cordeiro, RS; Faria Neto, HC; Lima, MC; Martins, MA; Silva, PM; Sunkel, CE, 1993
)
1.27

Dosage Studied

ExcerptRelevanceReference
" PCA 4248 behaved as a competitive and selective antagonist in [3H]serotonin secretion studies on rabbit platelets, since it displaced rightwards log dose-response curves and lacked any effect on thrombin- and ionophore A23187-induced platelet secretion."( 1,4-Dihydropyridines, a new class of platelet-activating factor receptor antagonists: in vitro pharmacologic studies.
de Casa-Juana, MF; García, MC; Gijón, MA; Ortega, MP; Priego, JG; Sanchez Crespo, M; Sunkel, C, 1990
)
1.19
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
dihydropyridine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency8.91250.125919.1169125.8920AID2549
Chain A, Ferritin light chainEquus caballus (horse)Potency50.11875.623417.292931.6228AID485281
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency35.48130.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency37.68580.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency25.11890.035520.977089.1251AID504332
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency23.75300.00798.23321,122.0200AID2546; AID2551
survival motor neuron protein isoform dHomo sapiens (human)Potency28.18380.125912.234435.4813AID1458
[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)
Platelet-activating factor receptorCavia porcellus (domestic guinea pig)Ki0.01510.00040.33863.2500AID157899
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID157899Tested for inhibition of [3H]PAF binding to rabbit Platelet activating factor receptor 1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-Alkyl-1,4-dihydropyridines derivatives as specific PAF-acether antagonists.
AID186691Tested in vivo for ability to inhibit PAF-induced hypotension in rats by measuring the drop in mean arterial blood pressure(mmHg) after 3 minutes activity1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-Alkyl-1,4-dihydropyridines derivatives as specific PAF-acether antagonists.
AID166772Tested in vitro for platelet activating factor (PAF) receptor antagonist activity by inhibiting PAF-induced ATP release in rabbit platelets1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-Alkyl-1,4-dihydropyridines derivatives as specific PAF-acether antagonists.
AID166773Tested in vitro for platelet activating factor (PAF) receptor antagonist activity by inhibiting PAF-induced platelet aggregation from rabbit1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-Alkyl-1,4-dihydropyridines derivatives as specific PAF-acether antagonists.
AID186690Tested in vivo for ability to inhibit PAF-induced hypotension in rats by measuring the drop in mean arterial blood pressure(mmHg) after 20 minutes activity1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-Alkyl-1,4-dihydropyridines derivatives as specific PAF-acether 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's16 (57.14)18.2507
2000's5 (17.86)29.6817
2010's7 (25.00)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: 10.96

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 Index10.96 (24.57)
Research Supply Index3.37 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (96.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]