Page last updated: 2024-11-07

sdz 64-412

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

Description

SDZ 64-412: structure given in first source; PAF antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID159547
CHEMBL ID449395
SCHEMBL ID9118339
MeSH IDM0161381

Synonyms (15)

Synonym
bdbm50041921
5-{4-[2-(3,4,5-trimethoxy-phenyl)-ethyl]-phenyl}-2,3-dihydro-imidazo[2,1-a]isoquinoline
gtpl1855
sdz 64-412
L024111
CHEMBL449395 ,
sdz-64-412
SCHEMBL9118339
5-[4-[2-(3,4,5-trimethoxyphenyl)ethyl]phenyl]-2,3-dihydroimidazo[2,1-a]isoquinoline
HY-U00040
paf-an-1
CS-7323
115621-84-6
Q27088770
AKOS040740987

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The bioavailability of the parent drug, calculated by dose-normalized AUC and deconvolution methods, was only 10-15% from the low dose, but increased to approximately 40% following the high dose."( Pharmacokinetics of SDZ 64-412, a novel antiasthmatic agent, following intravenous, oral, and inhalation dosing in the rat.
Athill, LV; Charnick, SB; Karara, AH; Lau, DT; Tse, FL; Yu, Z, 1994
)
0.29

Dosage Studied

ExcerptRelevanceReference
"The pharmacokinetics of SDZ 64-412, an antiasthmatic agent, were investigated following intravenous, oral, and inhalation dosing in rats."( Pharmacokinetics of SDZ 64-412, a novel antiasthmatic agent, following intravenous, oral, and inhalation dosing in the rat.
Athill, LV; Charnick, SB; Karara, AH; Lau, DT; Tse, FL; Yu, Z, 1994
)
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 receptorHomo sapiens (human)IC50 (µMol)0.06000.00030.63183.7000AID154467
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
positive regulation of cellular extravasationPlatelet-activating factor receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIPlatelet-activating factor receptorHomo sapiens (human)
chemotaxisPlatelet-activating factor receptorHomo sapiens (human)
inflammatory responsePlatelet-activating factor receptorHomo sapiens (human)
immune responsePlatelet-activating factor receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
parturitionPlatelet-activating factor receptorHomo sapiens (human)
response to symbiotic bacteriumPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of interleukin-6 productionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of tumor necrosis factor productionPlatelet-activating factor receptorHomo sapiens (human)
inositol trisphosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of neutrophil degranulationPlatelet-activating factor receptorHomo sapiens (human)
transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of translationPlatelet-activating factor receptorHomo sapiens (human)
negative regulation of blood pressurePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
cellular response to gravityPlatelet-activating factor receptorHomo sapiens (human)
cellular response to cAMPPlatelet-activating factor receptorHomo sapiens (human)
cellular response to fatty acidPlatelet-activating factor receptorHomo sapiens (human)
response to dexamethasonePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of leukocyte tethering or rollingPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of maternal process involved in parturitionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of gastro-intestinal system smooth muscle contractionPlatelet-activating factor receptorHomo sapiens (human)
cellular response to 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholinePlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide immune receptor activityPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor activityPlatelet-activating factor receptorHomo sapiens (human)
platelet activating factor receptor activityPlatelet-activating factor receptorHomo sapiens (human)
protein bindingPlatelet-activating factor receptorHomo sapiens (human)
phospholipid bindingPlatelet-activating factor receptorHomo sapiens (human)
mitogen-activated protein kinase bindingPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityPlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membranePlatelet-activating factor receptorHomo sapiens (human)
membranePlatelet-activating factor receptorHomo sapiens (human)
secretory granule membranePlatelet-activating factor receptorHomo sapiens (human)
tertiary granule membranePlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID77109In vivo PAF induced hemoconcentration tested in guinea pig1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists.
AID77108In vivo PAF induced bronchoconstriction tested in guinea pig1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists.
AID154467In vitro PAF antagonistic activity by determining [3H]PAF binding to the PAF-receptor of human platelets1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists.
AID1346403Human PAF receptor (Platelet-activating factor receptor)1988The Journal of pharmacology and experimental therapeutics, Nov, Volume: 247, Issue:2
Biological effects of the orally active platelet activating factor receptor antagonist SDZ 64-412.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (16.67)18.7374
1990's5 (83.33)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]