Page last updated: 2024-11-05

terodiline

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

Terodiline is a synthetic anticholinergic drug that was initially marketed for the treatment of urinary incontinence and overactive bladder. It acts by blocking the action of acetylcholine, a neurotransmitter that stimulates bladder contractions. However, terodiline was withdrawn from the market in several countries due to the risk of severe adverse effects, including cardiac arrhythmias and liver toxicity. Its synthesis involves multiple steps and starts with the reaction of a substituted phenoxyacetic acid with a cyclic amine. Despite its withdrawal, terodiline remains an interesting compound for researchers studying its pharmacological properties and the mechanisms underlying its adverse effects. The study of terodiline's effects on the cardiovascular system and the liver provides valuable insights into the potential risks of anticholinergic drugs.'

Cross-References

ID SourceID
PubMed CID23480
CHEMBL ID363295
CHEBI ID135168
SCHEMBL ID78908
MeSH IDM0056258

Synonyms (32)

Synonym
tert-butyl-(1-methyl-3,3-diphenyl-propyl)-amine
bdbm50151868
15793-40-5
terodiline
terodilina [inn-spanish]
terodiline [inn:ban:jan]
benzenepropanamine, n-(1,1-dimethylethyl)-alpha-methyl-gamma-phenyl-
terodilinum [inn-latin]
n-tert-butyl-1-methyl-3,3-diphenylpropylamine
benzenepropanamine, n-(1,1-dimethylethyl)-.alpha.-methyl-.gamma.-phenyl-
propylamine, n-tert-butyl-1-methyl-3,3-diphenyl-
CHEBI:135168
n-tert-butyl-4,4-diphenylbutan-2-amine
CHEMBL363295
terodilina
70kg06964w ,
terodilinum
unii-70kg06964w
terodiline [who-dd]
terodiline [inn]
terodiline [mi]
(+/-)-n-tert-butyl-1-methyl-3,3-diphenylpropylamine
SCHEMBL78908
n-(tert-butyl)-4,4-diphenyl-2-butanamine #
UISARWKNNNHPGI-UHFFFAOYSA-N
DTXSID60860001
DB13725
Q7702989
NCGC00183030-02
n-(tert-butyl)-4,4-diphenylbutan-2-amine
CS-0006361
HY-16489

Research Excerpts

Overview

Terodiline is a secondary amine with anticholinergic and calcium antagonistic properties. It is an alternative drug in the treatment of detrusor hyperreflexia.

ExcerptReferenceRelevance
"Terodiline is a secondary amine with antimuscarinic and calcium antagonistic properties. "( Terodiline in the treatment of urinary frequency and motor urge incontinence. A controlled multicentre trial.
Peters, D, 1984
)
3.15
"Terodiline is a secondary amine with anticholinergic and calcium antagonistic properties. "( Evaluation of long-term safety and clinical benefit of terodiline in women with urgency/urge incontinence. A multicentre study.
Fischer-Rasmussen, W, 1984
)
1.96
"Terodiline is a new drug combining anticholinergic and calcium-blocking effects."( Functional daytime incontinence: pharmacological treatment.
Chiozza, ML; Hjälmås, K; Passerini-Glazel, G, 1992
)
1
"Terodiline is an alternative drug in the treatment of detrusor hyperreflexia."( Terodiline treatment of detrusor hyperreflexia in sclerosis multiplex.
Jensen, D,
)
2.3
"Terodiline seems to be a promising alternative for treatment of motor urge incontinence in women."( The effect of terodiline treatment in women with motor urge incontinence. Results from a double-blind study and long-term treatment.
Andersson, KE; Ekman, G; Ulmsten, U, 1985
)
1.35

Effects

Terodiline has the theoretical advantage of being a drug with anticholinergic and calcium channel blocking effects. It has been compared with emepronium in the treatment of 20 women suffering with frequency, urgency and incontinence.

ExcerptReferenceRelevance
"Terodiline has been compared with emepronium in the treatment of 20 women suffering with frequency, urgency and incontinence in a double-blind, two-way cross-over study with fixed placebo as wash-out. "( A symptomatic and cystometric comparison of terodiline with emepronium in the treatment of women with frequency, urgency and incontinence.
Arkell, DG; Sole, GM, 1984
)
1.97
"Terodiline has non-selective anticholinergic and calcium blocking effects within the same concentration range, the anticholinergic effect predominating at low and the calcium entry blocking action at high concentrations."( Clinical pharmacology of terodiline.
Andersson, KE, 1984
)
1.29
"Terodiline has concentration dependent QT prolonging effects and thus the potential for cardiotoxicity. "( CYP2D6 and CYP2C19 genotypes of patients with terodiline cardiotoxicity identified through the yellow card system.
Daly, AK; Ford, GA; Wood, SM, 2000
)
2.01
"Terodiline has both anticholinergic and calcium antagonist properties and, as a result, effectively reduces abnormal bladder contractions caused by detrusor instability. "( Terodiline. A review of its pharmacological properties, and therapeutic use in the treatment of urinary incontinence.
Langtry, HD; McTavish, D, 1990
)
3.16
"Terodiline has the theoretical advantage of being a drug with anticholinergic and calcium channel blocking effects."( Terodiline: a dose titrated, multicenter study of the treatment of idiopathic detrusor instability in women.
Abrams, P; Carr, T; Choa, R; Fall, M; Korhonen, M; Massey, A; Norgaard, J; Tapp, A, 1989
)
2.44

Toxicity

ExcerptReferenceRelevance
" The safety was evaluated by recording of adverse reactions and measurements of haematology (B-Hb, B-erythrocytes, B-leukocytes, B-thrombocytes), liver function (S-ALAT, S-ASAT, S-ALP), kidney function (S-creatinine), ESR, heart rate and blood pressure."( Evaluation of long-term safety and clinical benefit of terodiline in women with urgency/urge incontinence. A multicentre study.
Fischer-Rasmussen, W, 1984
)
0.51
" However, possession of the CYP2C19*2 allele appears to contribute to adverse cardiac reactions to terodiline."( CYP2D6 and CYP2C19 genotypes of patients with terodiline cardiotoxicity identified through the yellow card system.
Daly, AK; Ford, GA; Wood, SM, 2000
)
0.78

Pharmacokinetics

terodiline (Mictrol) is an anticholinergic and calcium antagonist drug effective in the treatment of urinary incontinence. The mean terminal half-life was 131 h and the clearance after oral administration (clearance/systemic availability) was 39 ml.

ExcerptReferenceRelevance
"5 mg/kg), the terminal half-life 3 hr, the systemic clearance 40 ml/min."( Pharmacokinetics of terodiline and a major metabolite in dogs with a correlation to a pharmacodynamic effect.
Brötell, H; Grälls, M; Hallén, B; Strömberg, S, 1990
)
0.6
" The mean terminal half-life of terodiline was 131 h and the clearance after oral administration (clearance/systemic availability) was 39 ml."( Tolerability and steady-state pharmacokinetics of terodiline and its main metabolites in elderly patients with urinary incontinence.
Bogentoft, S; Hallén, B; Ryd-Kjellén, E; Sandquist, S; Setterberg, G; Strömberg, S, 1989
)
0.81
" Moreover, their pharmacokinetic profiles were the same as for the water solution."( Single-dose pharmacokinetics of terodiline, including a stable isotope technique for improvement of statistical evaluations.
Guilbaud, O; Hallén, B; Lindeke, B; Strömberg, S,
)
0.41
"As a target group, geriataric patients were selected for pharmacokinetic studies with terodiline (Mictrol), an anticholinergic and calcium antagonist drug effective in the treatment of urinary incontinence."( Single- and multiple-dose pharmacokinetics of terodiline in geriatric patients.
Bogentoft, S; Ekelund, P; Hallén, B; Magnusson, A, 1988
)
0.76
"4 hr, terminal half-life 61 hr, oral clearance 77 ml/min."( Concomitant single-dose and multiple-dose pharmacokinetics of terodiline in man, with a note on its enantiomers and major metabolites.
Gabrielsson, J; Guilbaud, O; Hallén, B; Johansson, A; Larsson, E; Nyambati, S, 1995
)
0.53
" 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

Bioavailability

Terodiline is well absorbed from the gastrointestinal tract, and has a bioavailability of 90%.

ExcerptReferenceRelevance
" The bioavailability was about 25% (0."( Pharmacokinetics of terodiline and a major metabolite in dogs with a correlation to a pharmacodynamic effect.
Brötell, H; Grälls, M; Hallén, B; Strömberg, S, 1990
)
0.6
" It has complete bioavailability from the gastro-intestinal tract and a mean elimination half-life of 60 hours."( Terodiline in the treatment of urinary frequency and motor urge incontinence. A controlled multicentre trial.
Peters, D, 1984
)
1.71
" Terodiline is well absorbed from the gastrointestinal tract, and has a bioavailability of 90%."( Clinical pharmacology of terodiline.
Andersson, KE, 1984
)
1.48
" The absolute bioavailability varied between 64% and 105% with a mean of 92%."( Pharmacokinetics of terodiline in human volunteers.
Andersson, KE; Ekman, G; Karlén, B; Strömberg, S; Ulmsten, U, 1982
)
0.59
" The bioavailability of (+)-terodiline was 93 +/- 19%."( Pharmacokinetics of R(+)-terodiline given intravenously and orally to healthy volunteers.
Ekström, B; Gabrielsson, J; Hallén, B; Palmér, L, 1993
)
0.88
"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

Terodiline (10(-6) M) parallelly shifted the dose-response curve for carbachol in rabbit detrusor to the right. Peak effects occurred 8 hours after dosing when increases in QTc from baseline (95% confidence intervals) were -3 (-20, 13) for placebo, 23 (8, 37) for racemic terodilines.

ExcerptRelevanceReference
" At a daily dosage of 25 mg, terodiline was well tolerated and, as compared with placebo, resulted in a statistically significant reduction in the daily frequency of wetting."( [Diurnal enuresis in childhood is effectively treated with terodiline].
Adolfsson, T; Djurhuus, JC; Elmér, M; Nørgaard, JP, 1991
)
0.82
" A follow-up investigation indicates that an increase in terodiline dosage may improve the results."( Terodiline treatment of detrusor hyperreflexia in sclerosis multiplex.
Jensen, D,
)
1.82
" Theoretically, by using a drug with dual action the beneficial effect of reduced detrusor overactivity might occur at a dosage below that likely to lead to the troublesome side effects experienced by patients who take pure anticholinergic agents."( Terodiline: a dose titrated, multicenter study of the treatment of idiopathic detrusor instability in women.
Abrams, P; Carr, T; Choa, R; Fall, M; Korhonen, M; Massey, A; Norgaard, J; Tapp, A, 1989
)
1.72
"A bioequivalence study with terodiline (Mictrol) was performed in 8 healthy volunteers given a 25 mg oral dose of either of two solid dosage forms together with a water solution of the deuterated drug."( Single-dose pharmacokinetics of terodiline, including a stable isotope technique for improvement of statistical evaluations.
Guilbaud, O; Hallén, B; Lindeke, B; Strömberg, S,
)
0.71
" The dosing period extended from 2 through 53 weeks (21 weeks on the average)."( [Clinical evaluation of long-term administration with terodiline hydrochloride for the treatment of patients with neurogenic bladder].
Ishido, T; Miyazaki, K, 1988
)
0.52
" The results of this study indicate that TD-758 is useful for these patients and its optimal dosage is 24 mg once a day."( [Clinical effect of terodiline hydrochloride on nervous pollakisuria or irritative bladder].
Aida, Y; Fukui, J; Igawa, Y; Ogawa, A; Tomita, Y; Uchiyama, S; Wajiki, M; Watanabe, K; Yanagisawa, A; Yoneyama, T, 1987
)
0.6
" Terodiline (10(-6) M) parallelly shifted the dose-response curve for carbachol in rabbit detrusor to the right, and high doses of terodiline (3 X 10(-6)-3 X 10(-5) M) inhibited the maximal contraction."( [Effect of terodiline hydrochloride in isolated rabbit detrusor].
Abe, M; Ikeda, S; Ono, Y; Ujiie, A; Yamazaki, Y, 1987
)
1.57
" The optimum dosage was assessed by comparing 37."( The effect of terodiline on patients with detrusor instability.
Macfarlane, JR; Tolley, DA, 1984
)
0.63
" The degree of fluctuation during a dosage interval was 19% and the time to steady-state was about 9 days."( Concomitant single-dose and multiple-dose pharmacokinetics of terodiline in man, with a note on its enantiomers and major metabolites.
Gabrielsson, J; Guilbaud, O; Hallén, B; Johansson, A; Larsson, E; Nyambati, S, 1995
)
0.53
" The lessons learned from the experiences with these drugs hold implications for the future development of agents that prolong the QT interval and suggest the need for dose-response relation data and metabolic evaluations to define the subpopulations at particular risk."( Is QT interval prolongation harmful? A regulatory perspective.
Botstein, P, 1993
)
0.29
" Peak effects occurred 8 hours after dosing when increases in QTc from baseline (95% confidence intervals) were -3 (-20, 13) for placebo, 23 (8, 37) for racemic terodiline, 19 (6, 33) for R(+)-terodiline, and 0 (-10, 9) ms1/2 for S(-)-terodiline."( Stereoselective cardiotoxic effects of terodiline.
Bateman, DN; Daly, AK; Hartigan-Go, K; Thomas, SH, 1996
)
0.76
" At doses of 10(-6)-3 x 10(-5) M, propiverine caused both a rightward shift and inhibition of the maximum response in the acetylcholine (ACh) dose-response curve."( [Effects of propiverine hydrochloride (propiverine) on isolated rat and dog urinary bladder].
Kaneko, S; Nakano, D; Nishimori, T; Ohara, M, 1999
)
0.3
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency8.91250.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50 (µMol)4.80000.00032.63119.0000AID1207777
Catechol O-methyltransferaseRattus norvegicus (Norway rat)IC50 (µMol)4.80000.00222.81277.0795AID1207777
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)4.80000.00032.59559.0000AID1207777
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)3.12720.00091.901410.0000AID240820; AID576612
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)4.80000.00032.63119.0000AID1207777
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)4.80000.00032.25459.6000AID1207777
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (62)

Processvia Protein(s)Taxonomy
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
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)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
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 calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
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)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID1220559Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
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.
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
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.
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.
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.
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.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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.
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.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1220557Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1220554Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1220558Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1207777Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits2013Scientific reports, , Volume: 3MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID1220556Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
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.
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.
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.
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.
AID1220555Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1220560Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (130)

TimeframeStudies, This Drug (%)All Drugs %
pre-199052 (40.00)18.7374
1990's62 (47.69)18.2507
2000's12 (9.23)29.6817
2010's4 (3.08)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.40

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 Index22.40 (24.57)
Research Supply Index5.12 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials28 (20.29%)5.53%
Reviews3 (2.17%)6.00%
Case Studies9 (6.52%)4.05%
Observational0 (0.00%)0.25%
Other98 (71.01%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]