Page last updated: 2024-12-05

prenylamine

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

Description

Prenylamine: A drug formerly used in the treatment of angina pectoris but superseded by less hazardous drugs. Prenylamine depletes myocardial catecholamine stores and has some calcium channel blocking activity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1406) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9801
CHEMBL ID24072
CHEBI ID8397
SCHEMBL ID182253
MeSH IDM0017547

Synonyms (74)

Synonym
benzenepropanamine, n-(1-methyl-2-phenylethyl)-.gamma.-phenyl-
prenylamine
PDSP1_001083
b-436
falliocor
bismethin
n-(3,3-diphenylpropyl)-alpha-methylphenaethylamin [german]
hostaginan
elecor
sandoz 13-194
n-(3'-phenylo-2-propylo)-1,1-diphenylo-3-propyloamine [polish]
corpax
synadrin
prenilamina [inn-spanish]
brn 2060323
valecor
phenethylamine, n-(3,3-diphenylpropyl)-alpha-methyl-
prenylamine (vasodilator)
segontin
san 13-194
prenylamine [usan:inn:ban]
benzenepropanamine, n-(1-methyl-2-phenylethyl)-gamma-phenyl-
einecs 206-869-4
prenylaminum [inn-latin]
PDSP2_001067
n-(1-methyl-2-phenylethyl)-gamma-phenylbenzenepropanamine
dl-prenylamine
1-phenyl-2-(1',1'-diphenylpropyl-3'-amino)propane
DB04825
n-(3,3-diphenylpropyl)-alpha-methylphenethylamine
390-64-7
prenylamine (usan/inn)
D02383
SPBIO_002560
PRESTWICK0_000560
PRESTWICK1_000560
OPREA1_229505
PRESTWICK2_000560
CHEMBL24072 ,
3,3-diphenyl-n-(1-phenylpropan-2-yl)propan-1-amine
(3,3-diphenyl-propyl)-(1-methyl-2-phenyl-ethyl)-amine
bdbm50017723
prenylamine(3,3-diphenyl-propyl)-(1-methyl-2-phenyl-ethyl)-amine
carditin
n-(3'-phenyl-2-propyl)-1,1-diphenyl-3-propyloamine
n-(3'-phenylo-2-propylo)-1,1-diphenylo-3-propyloamine
n-(3,3-diphenylpropyl)-alpha-methylphenaethylamin
prenilamina
prenylaminum
unii-k2oh82z000
k2oh82z000 ,
prenylamine [mart.]
prenylamine [inn]
prenylamine [mi]
prenylamine [who-dd]
prenylamine [usan]
SCHEMBL182253
n-(3,3-diphenylpropyl)-.alpha.-methylphenaethylamin
phenethylamine, n-(3,3-diphenylpropyl)-.alpha.-methyl-
IFFPICMESYHZPQ-UHFFFAOYSA-N
n-(1-methyl-2-phenylethyl)-.gamma.-phenylbenzenepropanamine
n-(3,3-diphenylpropyl)-.alpha.-methylphenethylamine
corontin (salt/mix)
n-(1-methyl-2-phenylethyl)-3,3-diphenyl-1-propanamine #
DTXSID0048555
Q-201618
AKOS025150812
HMS3604C22
CHEBI:8397
Q7240579
EN300-18552722
(3,3-diphenylpropyl)(1-phenylpropan-2-yl)amine
CS-0017601
HY-A0257

Research Excerpts

Overview

Prenylamine is a vasodilator of phenylalkylamine structure. It was used for the treatment of angina pectoris, until reports of undesirable effects including ventricular tachycardia led to a decreasing use of the drug in the 1980s.

ExcerptReferenceRelevance
"Prenylamine is a vasodilator of phenylalkylamine structure and was used for the treatment of angina pectoris, until reports of undesirable effects including ventricular tachycardia led to a decreasing use of the drug in the 1980s. "( Identification and characterization of urinary prenylamine metabolites by means of liquid chromatography-tandem mass spectrometry.
Beuck, S; Koch, A; Kwiatkowska, D; Pokrywka, A; Schänzer, W; Sigmund, G; Thevis, M, 2012
)
2.08
"Prenylamine is a known calcium channel blocker, but its local anesthetic blocking effects on voltage-gated sodium channels have not been studied thus far."( Local anesthetic properties of prenylamine.
Gerner, P; Mujtaba, MG; Wang, GK, 2001
)
1.32
"Prenylamine is a weak Ca-antagonist compared to nifedipine, verapamil and diltiazem."( In vitro analysis of Ca-antagonistic effects of prenylamine as mechanisms for its cardiac actions.
Hashimoto, K; Imai, S; Nabata, H; Nakagawa, Y, 1978
)
1.24

Toxicity

ExcerptReferenceRelevance
" In a double-blind clinical trial with 26 oncological patients, no cardiomyopathy, arrhythmia or adverse reactions were observed in the group given adriamycin plus prenylamine."( The role of prenylamine in the prevention of adriamycin-induced cardiotoxicity. A review of experimental and clinical findings.
Boveris, A; Llesuy, S; Marantz, A; Milei, J; Molina, HA; Storino, R; Vazquez, A,
)
0.71

Pharmacokinetics

ExcerptReferenceRelevance
"A sensitive assay for prenylamine and dideuteroprenylamine (racemic or pseudo-racemate) has been developed and used in human pharmacokinetic studies."( A gas chromatographic/mass spectrometric assay for prenylamine suitable for pharmacokinetic studies of the racemate and the enantiomers.
Dengler, HJ; Paar, WD; Schmidt, EK; von Unruh, GE, 1992
)
0.85
" Distinct differences in various pharmacokinetic parameters were found between the S- and R-enantiomer."( Single- and multiple-dose pharmacokinetics of R-(-)-and S-(+)-prenylamine in man.
Gietl, Y; Knauf, H; Mutschler, E; Spahn, H, 1990
)
0.52
" Concentration-time profiles were analyzed both by compartment-dependent and compartment-independent pharmacokinetic models."( Pharmacokinetics of prenylamine racemate and enantiomers in man.
Brockmeier, D; Dengler, HJ; Hirzebruch, M; Paar, WD; Schmidt, EK; von Unruh, GE, 1990
)
0.6

Compound-Compound Interactions

ExcerptReferenceRelevance
" Brief information on the following reports of drug-drug interactions is given in this article with the intention of giving these reports wider publicity and, possibly, encouraging further observation and research to establish or disprove their validity in a larger and wider range of patients or volunteer subjects."( Early reports on drug interactions.
D'Arcy, PF, 1983
)
0.27

Bioavailability

ExcerptReferenceRelevance
" The relative bioavailability of prenylamine (Segontin 100) was 82."( Pharmacokinetics of prenylamine racemate and enantiomers in man.
Brockmeier, D; Dengler, HJ; Hirzebruch, M; Paar, WD; Schmidt, EK; von Unruh, GE, 1990
)
0.88

Dosage Studied

amil, D600, nifedipine, terodiline, diltiazem, fendiline and prenylamine.

ExcerptRelevanceReference
" dosage of 2 mg/kg racemic prenylamine."( Enantioselective disposition of R-(-)- and S-(+)-prenylamine in the rat.
Gietl, Y; Mutschler, E; Spahn, H, 1989
)
0.83
" In fact, the latter dosage has an opposite effect on endothelium and increases the number of circulating endothelial cells."( Experimental prevention of venous thrombosis.
Hladovec, J; Prerovský, I, 1980
)
0.26
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C atom.
[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 (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.06500.00091.901410.0000AID1207225
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)2.52000.00033.64849.2000AID1207166
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Calmodulin Bos taurus (cattle)Kd1.80001.80002.93333.5000AID1297606
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (57)

Processvia Protein(s)Taxonomy
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumCalmodulin Bos taurus (cattle)
negative regulation of ryanodine-sensitive calcium-release channel activityCalmodulin Bos taurus (cattle)
positive regulation of ryanodine-sensitive calcium-release channel activityCalmodulin Bos taurus (cattle)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
calcium ion bindingCalmodulin Bos taurus (cattle)
protein bindingCalmodulin Bos taurus (cattle)
protein domain specific bindingCalmodulin Bos taurus (cattle)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
cytosolCalmodulin Bos taurus (cattle)
spindle poleCalmodulin Bos taurus (cattle)
cytoplasmCalmodulin Bos taurus (cattle)
protein-containing complexCalmodulin Bos taurus (cattle)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID1061889Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1297602Displacement of [3H]bepridil from porcine brain CaM by Dixon analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID227699Virtual screen for compounds with anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1207688Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1207166Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1207195Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1297607Binding affinity to dansylated bovine testes CaM by fluorescence analysis in presence of calcium2+2016European journal of medicinal chemistry, Jun-30, Volume: 116The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1207225Inhibition of potassium current (Ikr) measured using whole-cell patch clamp experiments in HEK-293 cells stable transfected with hERG cDNA2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1207256Effective free therapeutic plasma concentration (EFTPC): the concentration of unbound compund in the blood plasma at therapeutic dose (mean of range)2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1297606Binding affinity to bovine brain CaM by FTPFACE analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1297603Binding affinity to dansylated bovine brain CaM assessed as half maximal increase in fluorescence by fluorescence analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II.
AID1297597Association constant, pKa of the compound by capillary electrophoresis analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (587)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990551 (93.87)18.7374
1990's17 (2.90)18.2507
2000's10 (1.70)29.6817
2010's8 (1.36)24.3611
2020's1 (0.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.49

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 Index23.49 (24.57)
Research Supply Index6.50 (2.92)
Research Growth Index4.21 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials43 (6.90%)5.53%
Reviews34 (5.46%)6.00%
Case Studies24 (3.85%)4.05%
Observational0 (0.00%)0.25%
Other522 (83.79%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]