Page last updated: 2024-12-06

tocainide

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Description

Tocainide: An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tocainide : A monocarboxylic acid amide in which 2,6-dimethylphenylaniline and isobutyric acid have combined to form the amide bond; used as a local anaesthetic. [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]

Cross-References

ID SourceID
PubMed CID38945
CHEMBL ID1762
CHEBI ID9611
SCHEMBL ID15761
MeSH IDM0025410

Synonyms (79)

Synonym
tocainida
tocainidum
AC-16017
CHEBI:9611 ,
w 36095
HMS3393G06
BRD-A92670106-003-03-9
CHEMBL1762
PRESTWICK3_001027
2',6'-propionoxylidide, 2-amino-
tocainida [inn-spanish]
tocainidum [inn-latin]
einecs 255-505-0
2-amino-n-(2,6-dimethylphenyl)propionamid
w-36095
astra w 36095
brn 2416564
propanamide, 2-amino-n-(2,6-dimethylphenyl)-
PRESTWICK2_001027
tocainide (usan/inn)
D06172
BPBIO1_001335
BSPBIO_001213
MLS001423966
AB00514717
C07142
41708-72-9
tocainide
smr000466388
MLS000759525
DB01056
2-amino-n-(2,6-dimethylphenyl)propanamide
alanyl-2,6-xylidide
2-amino-2',6'-propionoxylidide
NCGC00162129-01
PRESTWICK0_001027
PRESTWICK1_001027
SPBIO_003074
NCGC00162129-02
n-(2,6-dimethylphenyl)alaninamide
HMS2051G06
NCGC00162129-03
(-)-2-amino-n-(2,6-dimethylphenyl)propanamide
propanamide, 2-amino-n-(2,6-dimethylphenyl)-, (-)-
53984-26-2
76213-25-7
HMS2232D16
CCG-100842
27dxo59san ,
unii-27dxo59san
tocainide [usan:inn:ban]
AKOS009044713
2-amino-n-(2,6-dimethylphenyl)propanimidic acid
gtpl7309
AB00514717-06
NC00092
SCHEMBL15761
tocainide [mart.]
tocainide [mi]
tocainide [vandf]
tocainide [usan]
tocainide [inn]
tocainide [who-dd]
2-amino-n-(2,6-dimethylphenyl)propanamide #
BUJAGSGYPOAWEI-UHFFFAOYSA-N
AB00514717_08
DTXSID9040766
mfcd00072010
FT-0754302
41708-72-9 (free base)
AS-47668
Q757058
SDCCGSBI-0633699.P001
NCGC00162129-09
NCGC00162129-04
F15117
EN300-6499518
CS-0013837
HY-B1798

Research Excerpts

Overview

Tocainide is an antiarrhythmic drug structurally related to lignocaine with similar electrophysiological, haemodynamic and antiarr hythmic effects. It was primarily used for suppression of symptomatic ventricular arrhythmias.

ExcerptReferenceRelevance
"Tocainide is an antiarrhythmic agent belonging to class IB that was primarily used for suppression of symptomatic ventricular arrhythmias. "( A Focus on the Synthesis and Pharmacokinetics of Tocainide and its Analogues.
Carocci, A; Catalano, A; Cavalluzzi, MM; Corbo, F; Franchini, C; Lentini, G, 2018
)
2.18
"Tocainide is a new antiarrhythmic agent which seems to reduce effectively sodium conductance."( Successuful treatment of paramyotonia congenita (Eulenburg): muscle stiffness and weakness prevented by tocainide.
Böhlen, R; Haass, A; Mertens, HG; Ricker, K; Rüdel, R, 1980
)
1.2
"Tocainide appeared to be an effective and safe agent for the control of these refractory symptomatic ventricular arrhythmias in 14 of the 21 patients (66%)."( Chronic tocainide therapy for refractory high-grade ventricular arrhythmias.
Alpert, JS; Dalen, JE; Haffajee, CI; Howe, JP; Ockene, IS; Paraskos, JA; Sacks, GM, 1983
)
1.42
"Tocainide is a new antiarrhythmic agent that is used clinically as the racemic mixture. "( Gas--liquid chromatographic resolution and assay of tocainide enantiomers using a chiral capillary column and study of their selective disposition in man.
McErlane, KM; Pillai, GK, 1983
)
1.96
"Tocainide is an antiarrhythmic drug structurally related to lignocaine with similar electrophysiological, haemodynamic and antiarrhythmic effects. "( Tocainide. A review of its pharmacological properties and therapeutic efficacy.
Avery, GS; Brogden, RN; Heel, RC; Holmes, B; Speight, TM, 1983
)
3.15
"Tocainide is an orally effective antiarrhythmic agent, structurally and pharmacologically similar to lidocaine. "( Chemistry, pharmacology, antiarrhythmic efficacy and adverse effects of tocainide hydrochloride, an orally active structural analog of lidocaine.
Alpert, JS; Haffajee, CI; Young, MD,
)
1.81
"Tocainide is a new experimental antiarrhythmic agent used clinically as the racemic mixture of two enantiomers. "( Simultaneous determination of the enantiomers of tocainide in blood plasma using gas-liquid chromatography with electron-capture detection.
Gal, J; Sedman, AJ, 1984
)
1.96
"Tocainide is a primary amine with antiarrhythmic properties derived from lidocaine. "( Determination of tocainide in human plasma by gas chromatography with nitrogen-selective detection after Schiff base formation.
Johansson, L; Vessman, J, 1982
)
2.05
"Tocainide is a primary analog of lidocaine with antiarrhythmic properties used to treat ventricular rhythm disorders. "( Tocainide: a severe adverse reaction.
DeSimone, A; Dunn, JM; Groth, PE, 1988
)
3.16
"Tocainide is a derivative of lidocaine with anti-arrhythmic action and, unlike lidocaine, can be used for oral treatment. "( The analgesic effect of tocainide in trigeminal neuralgia.
Lindblom, U; Lindström, P, 1987
)
2.02
"Tocainide is an effective oral antiarrhythmic agent. "( Tocainide-induced reversible agranulocytosis and anemia.
Kadin, ME; Soff, GA, 1987
)
3.16
"Tocainide is an orally active lidocaine analog indicated for the suppression of ventricular arrhythmias. "( Tocainide: a new oral antiarrhythmic.
Hasegawa, GR,
)
3.02

Effects

Tocainide has been known to cause minor, transient and treatable side effects in the form of gastrointestinal and central nervous symptoms. The drug has not been shown to be more effective than quinidine or procainamide.

ExcerptReferenceRelevance
"Tocainide therapy has been evaluated in 38 patients with ventricular arrhythmias. "( Tocainide for drug-resistant ventricular arrhythmias: efficacy, side effects, and lidocaine responsiveness for predicting tocainide success.
Harrison, DC; Mason, JW; Winkle, RA, 1980
)
3.15
"Tocainide has been known to cause minor, transient and treatable side effects in the form of gastrointestinal and central nervous symptoms--mainly nausea, tremor and dizziness."( Mental changes associated with tocainide, a new antiarrhythmic.
Bikadoroff, S, 1987
)
1.28
"Tocainide has minimal negative inotropic effects and a tendency to shorten effective refractory periods."( Tocainide: a new oral antiarrhythmic agent.
Horowitz, LN; Kutalek, SP; Morganroth, J, 1985
)
2.43
"Tocainide has not been shown to be more effective than quinidine or procainamide."( Tocainide: a new oral antiarrhythmic.
Hasegawa, GR,
)
2.3

Actions

ExcerptReferenceRelevance
"Tocainide was found to inhibit the IK,ATP by 74% at 200 mumol.L-1 but not at 50 mumol.L-1."( [Inhibitory effect of tocainide on calcium current and potassium current in guinea pig ventricular myocytes].
Sheng, BT; Wang, WZ; Wu, BW; Zhao, RR, 1995
)
1.33

Treatment

Tocainide HCl treatment of tinnitus is promising. Treatment with tocainide decreased the plasma clearance of theophylline.

ExcerptReferenceRelevance
"Tocainide HCl treatment of tinnitus is promising."( Treatment of tinnitus with tocainide hydrochloride.
Emmett, JR; Shea, JJ,
)
1.15
"Treatment with tocainide decreased the plasma clearance of theophylline from 37.5 +/- 6.9 (mean +/- s.d.) to 33.7 +/- 5.0 ml kg-1 h-1 (difference -3.8, 95% CI, -1.7 to -5.9; P = 0.004) and increased its terminal elimination half-life from 9.7 +/- 2.5 to 10.4 +/- 2.1 h (difference 0.7, 95% CI, 0.2 to 1.2; P = 0.011)."( The effect of tocainide on theophylline metabolism.
Korrapati, MR; Loi, CM; Parker, BM; Vestal, RE; Wei, X, 1993
)
0.99

Toxicity

Tocainide appears to be as safe as quinidine but less effective in suppressing ventricular arrhythmias. Serious adverse effects occurred in 7 of 12 dogs (58%) receiving tocainide for longer than 4 consecutive months.

ExcerptReferenceRelevance
" Minor central nervous system side effects were seen in 2 patients and dermatologic adverse reaction was seen in one patient only."( Efficacy and safety of oral tocainide in refractory ventricular arrhythmia: a preliminary report on an open label study.
Mahapatra, D; Mahapatra, RK, 1986
)
0.57
" A common cause of drug trial failure for both drugs was the occurrence of adverse effects that frequently appeared well after hospital discharge."( Mexiletine and tocainide: a comparison of antiarrhythmic efficacy, adverse effects, and predictive value of lidocaine testing.
Barbey, JT; Echt, DS; Kopelman, HA; Murray, KT; Roden, DM; Siddoway, LA; Woosley, RL, 1989
)
0.63
" Thus, tocainide, the new oral analog of lidocaine, appears to be as safe as quinidine but is slightly less effective in suppressing ventricular arrhythmias."( Comparative efficacy and safety of oral tocainide and quinidine for benign and potentially lethal ventricular arrhythmias.
Morganroth, J; Oshrain, C; Steele, PP, 1985
)
0.99
" TAhe most frequent adverse experiences reported were neurologic and gastrointestinal in nature and included dizziness, lightheadedness, tremors, nausea, vomiting, and anorexia."( Safety evaluation of tocainide in the American Emergency Use Program.
Hadidian, Z; Horn, HR; Johnson, JL; Vassallo, HG; Williams, JH; Young, MD, 1980
)
0.58
" Serious adverse effects occurred in 7 of 12 dogs (58%) receiving tocainide for longer than 4 consecutive months."( Efficacy and toxicity of tocainide for the treatment of ventricular tachyarrhythmias in Doberman pinschers with occult cardiomyopathy.
Calvert, CA; Jacobs, GJ; Pickus, CW,
)
0.67
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Pharmacokinetics

ExcerptReferenceRelevance
" The present experiments examined these substances for pharmacodynamic differences."( Stereoselectivity of tocainide pharmacodynamics in vivo and in vitro.
Block, AJ; Merrill, D; Smith, ER, 1988
)
0.59
"0748 hr-1), elimination half-life (average reduction, 13."( Influence of rifampin on tocainide pharmacokinetics in humans.
Celestin, C; Foster, JR; Patterson, JH; Powell, JR; Rice, TL, 1989
)
0.58
" The terminal half-life and renal clearance of tocainide were not altered by either H2-receptor antagonists, compared with placebo."( The effect of histamine-2 receptor antagonists on tocainide pharmacokinetics.
Kapil, RP; Lalonde, RL; Mattern, AL; North, DS, 1988
)
0.78
" On the other hand, the elimination half-life of antiarrhythmic agents that have a large volume of distribution and are highly cleared by the liver may be twice as long in patients with CHF compared with normal subjects."( Effects of congestive heart failure on the pharmacokinetics and pharmacodynamics of antiarrhythmic agents.
Echt, DS; Roden, DM; Woosley, RL, 1986
)
0.27
" The mean plasma half-life was 15."( Pharmacokinetics and haemodynamic effects of tocainide in patients with acute myocardial infarction complicated by left ventricular failure.
Bakshi, M; Branagan, P; Kelly, JG; MacMahon, B; Walsh, MJ, 1985
)
0.53
" In 9 with total renal failure, the plasma half-life ranged from 16."( Pharmacokinetics of tocainide in patients with renal dysfunction and during haemodialysis.
Augustin, J; Graffner, C; Hanrath, P; Kuck, KH; Pottage, A; Runge, M; Wiegers, U, 1983
)
0.59
" In one patient with active hepatic necrosis the terminal plasma half-life was 57."( Pharmacokinetics of tocainide in patients with combined hepatic and renal dysfunction.
Endell, W; Oltmanns, D; Pottage, A, 1983
)
0.59
"This article reviews clinical pharmacokinetic data on 8 new antiarrhythmic agents."( Clinical pharmacokinetics of the newer antiarrhythmic agents.
Gillis, AM; Kates, RE,
)
0.13
"Quantitative structure-pharmacokinetic relationships (QSPkR) have increasingly been used for the prediction of the pharmacokinetic properties of drug leads."( Quantitative structure-pharmacokinetic relationships for drug clearance by using statistical learning methods.
Chen, YZ; Li, ZR; Yap, CW, 2006
)
0.33
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
" We examined the efficacy and electrophysiology of 110 antiarrhythmic drug combination trials at electrophysiologic study in 74 patients with recurrent ventricular tachycardia."( Antiarrhythmic drug combinations in the treatment of ventricular tachycardia.
Echt, DS; Griffin, JC; Keefe, DL; Mason, JW; Ross, DL; Swerdlow, CD; Sze, DY; Winkle, RA, 1982
)
0.26

Bioavailability

Tocainide's long plasma half-life and high oral bioavailability permit an 8-h regime. Cimetidine causes a decrease in the bioavailability of tocainide.

ExcerptReferenceRelevance
" These data indicate that cimetidine, but not ranitidine, causes a decrease in the bioavailability of tocainide and that neither agent alters the apparent elimination rate of tocainide."( The effect of histamine-2 receptor antagonists on tocainide pharmacokinetics.
Kapil, RP; Lalonde, RL; Mattern, AL; North, DS, 1988
)
0.74
" The drug has nearly 100% bioavailability after oral administration and an effective half-life of 9 to 37 hours (mean, 15 hours)."( Tocainide: a new oral antiarrhythmic agent.
Horowitz, LN; Kutalek, SP; Morganroth, J, 1985
)
1.71
" Oral bioavailability is virtually complete, elimination half-life is 11-15 hours, and 40 percent of a dose is excreted unchanged in urine."( Tocainide: a new oral antiarrhythmic.
Hasegawa, GR,
)
1.57
" Tocainide's long plasma half-life and high oral bioavailability permit an 8-h regime."( Chronic tocainide therapy for refractory high-grade ventricular arrhythmias.
Alpert, JS; Dalen, JE; Haffajee, CI; Howe, JP; Ockene, IS; Paraskos, JA; Sacks, GM, 1983
)
1.61
" In contrast to lignocaine (lidocaine) it is well absorbed after oral administration and has a plasma half-life of about 15 hours."( Tocainide. A review of its pharmacological properties and therapeutic efficacy.
Avery, GS; Brogden, RN; Heel, RC; Holmes, B; Speight, TM, 1983
)
1.71
" Flecainide pharmacokinetics are suitable for oral use but encainide disposition is complex with variable bioavailability and active metabolites that contribute substantially to activity."( Clinical profiles of newer class I antiarrhythmic agents--tocainide, mexiletine, encainide, flecainide and lorcainide.
Pottage, A, 1983
)
0.51
" Lorcainide is also a class Ic antiarrhythmic drug, the bioavailability of which is nonlinear."( Clinical pharmacokinetics of the newer antiarrhythmic agents.
Gillis, AM; Kates, RE,
)
0.13
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36

Dosage Studied

Tocainide does not exert an antifibrillatory action in the early phase of acute myocardial infarction. In the elderly, tocainide should be used in a lower dosage than normally recommended.

ExcerptRelevanceReference
" Serious adverse reactions necessitate a change in antiarrhythmic therapy, as opposed to lowering drug dosage to an ineffective level."( Antiarrhythmic drug therapy. Recent advances and current status.
Somberg, J, 1985
)
0.27
"Two middle aged female patients developed hallucinations and severe confusion with paranoid features during oral tocainide administration at recommended dosage levels."( Confusion and paranoia associated with oral tocainide.
Clarke, CW; el-Mahdi, EO, 1985
)
0.74
" The dosage of tocainide hydrochloride ranged from 200-600 mg daily."( A sequential double blind cross-over trial of tocainide hydrochloride in tinnitus.
Blayney, AW; Colman, BH; Guy, AM; Phillips, MS, 1985
)
0.88
" Its side effect profile appears to be similar in percentage to the adverse effects of quinidine, but often these side effects are milder, better tolerated, and respond to dosage alteration."( A review of the uses and limitations of tocainide--a class IB antiarrhythmic agent.
Horowitz, LN; Morganroth, J; Nestico, PF, 1985
)
0.54
" The findings are used to suggest a safe dosage regimen."( Pharmacokinetics of tocainide in patients with severe renal failure.
Braun, J; Engelmaier, F; Gessler, U; Gluth, WP; Sörgel, F, 1985
)
0.59
" If side effects intervene that may cause continued therapy to be intolerable, changing the antiarrhythmic agent, as opposed to decreasing the dosage to an ineffective range, may be appropriate."( New directions in antiarrhythmic drug therapy.
Somberg, JC, 1984
)
0.27
"Measurement of drug levels is becoming increasingly popular to optimise the dosage of various drugs."( Reliability of antiarrhythmic drug plasma concentration monitoring.
Follath, F; Ganzinger, U; Schuetz, E,
)
0.13
" These results suggest that in the dosage used in this study tocainide does not exert an antifibrillatory action in the early phase of acute myocardial infarction."( Prophylaxis of primary ventricular fibrillation with tocainide in acute myocardial infarction.
Campbell, RW; Elton, RA; Goodfellow, RM; Hutton, I; Taylor, E, 1983
)
0.76
" It is suggested that in the elderly, tocainide should be used in a lower dosage than normally recommended."( Nodal bradycardia induced by tocainide.
Datta, SK; Mandal, SK, 1983
)
0.83
" After evaluation of arrhythmias and treatment with intravenous lidocaine, oral tocainide dosage regimens were based on age, weight, and clinical status."( Tocainide kinetics in congestive heart failure.
Aronow, WS; Esterbrooks, D; Hee, TT; Hilleman, DE; Mohiuddin, SM; Mooss, AN; Patterson, AJ; Reich, JW; Sketch, MH, 1983
)
1.94
" Each patient then received a tocainide dosage schedule."( The appropriate dosage regime for the transition from intravenous lignocaine to oral tocainide after acute myocardial infarction.
Akhras, F; Emery, P; Holt, D; Jackson, G; Upward, JW, 1983
)
0.78
" In isolated right atria IQB-M-81 did not block the positive chronotropic and inotropic responses to isoprenaline but shifted the dose-response curve to the right."( Comparison of three beta-amino anilides: IQB-M-81, lidocaine and tocainide, on isolated rat atria.
Barrigón, S; Tamargo, J; Tejerina, T, 1983
)
0.5
" Tocainide dosage was 17."( Antiarrhythmic efficacy, pharmacokinetics and clinical safety of tocainide in convalescent myocardial infarction patients.
Klein, MD; Levine, PA; Ryan, TJ, 1980
)
1.41
" Survival, frequency of symptomatic tachycardia, frequency of asymptomatic ventricular tachycardia, and tolerance of the therapeutically effective dosage were the criteria used to assess therapeutic effectiveness."( Open clinical studies at a referral center: chronic maintenance tocainide therapy in patients with recurrent sustained ventricular tachycardia refractory to conventional antiarrhythmic agents.
Maloney, JD; McColgan, JM; Nissen, RG, 1980
)
0.5
"-mass spectrometric analysis of urine extracts from rats dosed with tocainide (I) revealed the presence of cyclic compound identified as 3-(2,6-xylyl)-5-methylhydantoin (IV) derived from tocainide."( 3-(2,6-Xylyl)-5-methylhydantoin--a metabolite or a metabonate of tocainide in rats.
Axelson, JE; Venkataramanan, R, 1981
)
0.74
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
local anaestheticAny member of a group of drugs that reversibly inhibit the propagation of signals along nerves. Wide variations in potency, stability, toxicity, water-solubility and duration of action determine the route used for administration, e.g. topical, intravenous, epidural or spinal block.
anti-arrhythmia drugA drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres.
sodium channel blockerAn agent that inhibits sodium influx through cell membranes.
[role 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]

Drug Classes (1)

ClassDescription
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
[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]

Pathways (1)

PathwayProteinsCompounds
Tocainide Action Pathway478

Protein Targets (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.00600.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (149)

Assay IDTitleYearJournalArticle
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID25320Dissociation constant (pKa)1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
New antiarrhythmic agents. 6. Quantitative structure-activity relationships of aminoxylidides.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID128839Antiarrhythmic activity against arrhythmogenic effects of chloroform in mice after sc administration1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 5. alpha-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID114025Effective dose of compound that evoked CNS toxicity in mice in the form of ataxia1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
New antiarrhythmic agents. 7. 2,3-Diaminopropionanilides.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1128790Inhibition of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle at -140 mV of holding potential by Hille-Campbell vaseline gap voltage-clamp recording2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1128779Inhibition of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle assessed as tonic block by measuring reduction of maximal peak sodium transient at holding potential -100 mV by Hille-Campbell vaseline gap voltage-clamp 2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID396080Blockade of Nav1.4 sodium channel in frog semitendinosus muscle fibres assessed as phasic block at 10 Hz stimulation frequency by vaseline-gap voltage clamp method2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents.
AID114458Ataxia was measured in mice after sc administration at given dose.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1130809Antiarrhythmic activity in Swiss albino mouse assessed as protection against chloroform-induced fibrillation at 100 mg/kg, sc treated 20 mins before chloroform challenge1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID1128800Binding affinity to rat serum albumin at 30 uM by HPLC analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID63262Ventricular rate was measured in anesthetized dog at 0.32+/-0.11 dose1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID1130837Ratio of lidocaine ED50 to compound ED50 for antiarrhythmic activity sc dosed mouse assessed as protection against chloroform-induced fibrillation1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
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
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1128782Inhibition of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle assessed as use-dependent block at 10 Hz frequency by Hille-Campbell vaseline gap voltage-clamp recording2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID1128804Ratio of binding affinity to rat serum albumin assessed as fraction unbound to binding affinity to human serum albumin assessed as fraction unbound2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID396079Blockade of Nav1.4 sodium channel in frog semitendinosus muscle fibres assessed as tonic block elicited by infrequent depolarizing pulses at a frequency of 0.3 Hz by vaseline-gap voltage clamp method2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1128780Inhibition of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle assessed as use-dependent block at at 2 Hz stimulation frequency by Hille-Campbell vaseline gap voltage-clamp recording2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
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]
AID1128781Ratio of IC50 for tonic block of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle to IC50 for use-dependent block of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle at 2 Hz frequ2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID60099Nature of toxicity was expressed; convulsion1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1130815Ratio of lidocaine ED50 to compound ED50 for antiarrhythmic activity sc dosed Swiss albino mouse assessed as protection against chloroform-induced ventricular fibrillation1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID174599Anesthetic activity of compound (1.0%) was evaluated by duration of sciatic nerve block1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
New antiarrhythmic agents. 7. 2,3-Diaminopropionanilides.
AID1130818Antiarrhythmic activity in left anterior descending coronary artery ligated myocardial infarction dog model assessed as mean arterial blood pressure at infusion rate 0.5 mg/kg/min, iv1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID74899Amount of ouabain needed for production of ventricular extra-systoles at a dose of 4 mg/kg (iv given 5 min prior) in guinea pig1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
New antiarrhythmic agents. 2,2,5,5-Tetramethyl-3-pyrroline-3-carboxamides and 2,2,5,5-tetramethylpyrrolidine-3-carboxamindes.
AID1130841Antiarrhythmic activity in iv dosed left anterior descending coronary artery ligated myocardial infarction model of dog assessed as dose required for reduction of ectopic beats to <= 5%1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID1130811Toxicity in Swiss albino mouse assessed as convulsion at 100 mg/kg, sc measured up to 20 mins1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1130836Antiarrhythmic activity in sc dosed mouse assessed as protection against chloroform-induced fibrillation1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID58891MABP value was measured in anesthetized dog at 0.32+/-0.11 dose.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID110241Percentage toxicity measured as ataxia.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
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.
AID114027Effective dose of compound that protects mice against chloroform induced tachycardia1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
New antiarrhythmic agents. 7. 2,3-Diaminopropionanilides.
AID1128802Binding affinity to human serum albumin assessed as fraction unbound at 30 uM by HPLC analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID174598Anesthetic activity of compound (0.5%) was evaluated by duration of sciatic nerve block1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
New antiarrhythmic agents. 7. 2,3-Diaminopropionanilides.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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]
AID1128791Inhibition of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle at -70 mV of holding potential by Hille-Campbell vaseline gap voltage-clamp recording2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1128783Ratio of IC50 for tonic block of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle to IC50 for use-dependent block of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle at 10 Hz freq2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1128777Inhibition of voltage-gated sodium channel in Rana esculenta ventral branch of semitendinosus muscle assessed as tonic block by measuring reduction of maximal peak sodium transient at 500 uM at 10 Hz stimulation frequency by Hille-Campbell vaseline gap vo2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID60698% ectopic beats was measured in anesthetized dog at 0.32+/-0.11 dose; 2+/-21981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID128299Acute CNS toxicity against arrhythmogenic effects of chloroform in mice after sc administration1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 5. alpha-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID235211Therapeutic index is the ratio of ED50 (ataxia) to ED50 (protection) in mice1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
New antiarrhythmic agents. 6. Quantitative structure-activity relationships of aminoxylidides.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID114662Compound was evaluated for protection against tachycardia in mice1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
New antiarrhythmic agents. 6. Quantitative structure-activity relationships of aminoxylidides.
AID27368Lethal dose of compound evaluated by administering intravenously to female CRCD mice1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
New antiarrhythmic agents. 7. 2,3-Diaminopropionanilides.
AID1128799Binding affinity to human serum albumin at 30 uM by HPLC analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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]
AID1130832Toxicity in mouse assessed as loss of righting reflex at 100 mg/kg, sc measured up to 20 mins1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1130838Antiarrhythmic activity in left anterior descending coronary artery ligated myocardial infarction model of dog assessed as clearing value of ventricular ectopic beats at 0.5 mg/kg/min, iv1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID74896Amount of ouabain needed for production of ventricular arrhythmias that causes death in guinea pig by cardiac arrest at a dose of 4 mg/kg iv given 5 min prior1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
New antiarrhythmic agents. 2,2,5,5-Tetramethyl-3-pyrroline-3-carboxamides and 2,2,5,5-tetramethylpyrrolidine-3-carboxamindes.
AID60465The dose at which toxicity was measured.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID23097Compound was evaluated for -Log [fraction ionized x ED50 (protection)]1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
New antiarrhythmic agents. 6. Quantitative structure-activity relationships of aminoxylidides.
AID74902Amount of ouabain needed for production of ventricular fibrillation at a dose of 4 mg/kg (iv given 5 min prior) in guinea pig1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
New antiarrhythmic agents. 2,2,5,5-Tetramethyl-3-pyrroline-3-carboxamides and 2,2,5,5-tetramethylpyrrolidine-3-carboxamindes.
AID119034Protection against chloroform induced arrhythmias in mice after subcutaneous administration at 100 mg/kg dose.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID1130843Toxicity in iv dosed left anterior descending coronary artery ligated myocardial infarction model of dog assessed as dose required to cause toxic effect1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1130817Antiarrhythmic activity in left anterior descending coronary artery ligated myocardial infarction dog model assessed as clearing value as reduction in ventricular ectopic beat rate per min at infusion rate 0.5 mg/kg/min, iv treated until arrhythmia cleare1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID1130833Toxicity in mouse assessed as mortality at 100 mg/kg, sc measured up to 20 mins1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID1130821Toxicity in left anterior descending coronary artery ligated myocardial infarction dog model assessed as dose required to cause convulsion at infusion rate at 0.5 mg/kg/min1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1130840Antiarrhythmic activity in left anterior descending coronary artery ligated myocardial infarction model of dog assessed as mean arterial blood pressure at 0.5 mg/kg/min, iv1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID1130810Toxicity in Swiss albino mouse assessed as ataxia at 100 mg/kg, sc measured up to 20 mins1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID115266Percentage toxicity measured as loss of righting reflex.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID235615Therapeutic index is defined as the ratio of ED50(ataxia)/ED50(protection)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 5. alpha-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID114213Protection against chloroform induced arrhythmias was measured in mice after sc administration at given dose.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID1130820Antiarrhythmic activity in iv dosed left anterior descending coronary artery ligated myocardial infarction dog model assessed as dose required to reduction in ventricular ectopic beats to <= 5% at infusion rate 0.5 mg/kg/min1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
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]
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]
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID111310Percentage toxicity measured as death of mice.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID1130814Antiarrhythmic activity in sc dosed Swiss albino mouse assessed as protection against chloroform-induced ventricular fibrillation1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID114641Compound was evaluated for ataxia in mice1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
New antiarrhythmic agents. 6. Quantitative structure-activity relationships of aminoxylidides.
AID1130831Toxicity in mouse assessed as convulsion at 100 mg/kg, sc measured up to 20 mins1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID110154Percentage toxicity measured as convulsions.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 4. 1'-(Aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1130812Toxicity in Swiss albino mouse assessed as loss of righting reflex at 100 mg/kg, sc measured up to 20 mins1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID23494Partition coefficient (logP)1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
New antiarrhythmic agents. 6. Quantitative structure-activity relationships of aminoxylidides.
AID1130839Antiarrhythmic activity in left anterior descending coronary artery ligated myocardial infarction model of dog assessed as clearing value of ventricular rate at 0.5 mg/kg/min, iv1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 3. Primary beta-amino anilides.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1130816Antiarrhythmic activity in left anterior descending coronary artery ligated myocardial infarction dog model assessed as clearing value as reduction in ventricular ectopic beats to <= 5% for 5 mins at infusion rate 0.5 mg/kg/min, iv treated until arrhythmi1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID1130813Toxicity in Swiss albino mouse assessed as death at 100 mg/kg, sc measured up to 20 mins1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
New antiarrhythmic agents. 2. Amide alkyl alpha-amino xylidides.
AID1128803Binding affinity to rat serum albumin assessed as fraction unbound at 30 uM by HPLC analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
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 (373)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990271 (72.65)18.7374
1990's54 (14.48)18.2507
2000's25 (6.70)29.6817
2010's18 (4.83)24.3611
2020's5 (1.34)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.03

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

MetricThis Compound (vs All)
Research Demand Index42.03 (24.57)
Research Supply Index6.12 (2.92)
Research Growth Index4.15 (4.65)
Search Engine Demand Index66.05 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials47 (11.60%)5.53%
Reviews59 (14.57%)6.00%
Case Studies50 (12.35%)4.05%
Observational0 (0.00%)0.25%
Other249 (61.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]