Page last updated: 2024-12-04

gallopamil

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Description

Gallopamil: Coronary vasodilator that is an analog of iproveratril (VERAPAMIL) with one more methoxy group on the benzene ring. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1234
CHEMBL ID51149
CHEBI ID34772
SCHEMBL ID49428
MeSH IDM0008964

Synonyms (80)

Synonym
BRD-A52922642-003-01-7
BRD-A52922642-001-02-9
galopamilo [inn-spanish]
gallopamillum [inn-latin]
gallopamil [inn:ban]
methoxyverapamil
c28h40n2o5
5-((3,4-dimethoxyphenethyl)methylamino)-2-isopropyl-2-(3,4,5-trimethoxyphenyl)valeronitrile
d 600
benzeneacetonitrile, alpha-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-3,4,5-trimethoxy-alpha-(1-methylethyl)-
gallopamil
5-[(3,4-dimethoxyphenethyl)methylamino]-2-isopropyl-2-(3,4,5-trimethoxyphenyl)valeronitrile
BIO1_000389
BIO2_000103
BIO1_001367
BIO2_000583
BIO1_000878
PDSP2_001069
IDI1_033853
LOPAC0_000778
BSPBIO_001383
PDSP1_001085
NCGC00089760-03
NCGC00089760-04
d600
16662-47-8
KBIOSS_000103
KBIO3_000206
KBIO2_002671
KBIO2_000103
KBIO3_000205
KBIOGR_000103
KBIO2_005239
HSCI1_000351
NCGC00089760-02
methoxyverapamil hydrochloride
NCGC00089760-05
HMS1989F05
NCGC00015686-09
chebi:34772 ,
CHEMBL51149
gallopamil (inn)
D08009
HMS1791F05
5-[2-(3,4-dimethoxyphenyl)ethyl-methylamino]-2-propan-2-yl-2-(3,4,5-trimethoxyphenyl)pentanenitrile
NCGC00015686-05
cas_119442
nsc_119442
bdbm82061
39wpc8jhr8 ,
galopamilo
unii-39wpc8jhr8
gallopamillum
CCG-204863
5-((3,4-dimethoxyphenethyl)(methyl)amino)-2-isopropyl-2-(3,4,5-trimethoxyphenyl)pentanenitrile
NCGC00015686-10
NCGC00015686-03
NCGC00015686-06
NCGC00015686-04
NCGC00015686-07
AKOS015914091
.alpha.-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-3,4,5-trimethoxy-.alpha.-(1-methylethyl)benzeneacetonitrile
gallopamil [mi]
gallopamil [who-dd]
gallopamil [inn]
56949-78-1
.alpha.-isopropyl-.alpha.-((n-methyl-n-homoveratryl)-.gamma.-aminopropyl)-3,4,5-trimethoxyphenylacetonitrile
SCHEMBL49428
DTXSID5045172
5-[[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino]-2-isopropyl-2-(3,4,5-trimethoxyphenyl)pentanenitrile #
XQLWNAFCTODIRK-UHFFFAOYSA-N
5-[2-(3,4-dimethoxyphenyl)ethyl-methyl-amino]-2-isopropyl-2-(3,4,5-trimethoxyphenyl)pentanenitrile
DB12923
Q412127
SDCCGSBI-0050756.P002
NCGC00015686-13
CS-0002968
HY-14276
methoxyverapamilhydrochloride
benzeneacetonitrile, alpha-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4,5-trimethoxy-alpha-(1-methylethyl)-

Research Excerpts

Overview

Gallopamil (GAL) is a new calcium-antagonist that, although structurally similar to verapamil, has more potency. It is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verAPamil.

ExcerptReferenceRelevance
"Gallopamil is a methoxy derivative of verapamil. "( Gallopamil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in ischaemic heart disease.
Benfield, P; Brogden, RN, 1994
)
3.17
"Gallopamil (GSR) is a new calcium-channel blocker. "( Slow-release gallopamil in patients with stable effort angina.
Cherchi, A; Lai, C; Onnis, E; Solinas, R, 1992
)
2.1
"Gallopamil (GAL) is a new calcium-antagonist that, although structurally similar to verapamil, has more potency."( Calcium antagonists and hormone release. VII. Effects of gallopamil infusion on insulin and C peptide release in normal subjects.
Camaioni, M; Conte, G; De Marinis, L; Fiumara, C; Folli, G; Mancini, A; Zuppi, P, 1991
)
1.25
"Gallopamil is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verapamil. "( High-performance liquid chromatographic (HPLC) assay using fluorescence detection for the simultaneous determination of gallopamil and norgallopamil in human plasma.
Babcock-Atkinson, E; Gonzalez, MA; McLean, AM; Noonan, PK; Rein, K; Ruggirello, DA, 1987
)
1.92

Effects

ExcerptReferenceRelevance
"Gallopamil has complex actions: it inhibits ryanodine binding to its low affinity site(s), and probably modulates the cooperativity of ryanodine binding and/or the transition to a receptor state characterized by slow ryanodine dissociation."( Interaction between gallopamil and cardiac ryanodine receptors.
Galbani, P; Mariani, M; Ronca, G; Ronca-Testoni, S; Yu, G; Zucchi, R, 1995
)
1.34

Treatment

Gallopamil pretreatment had no significant effect on methacholine-induced bronchoconstriction. Pretreatment with gallopAmil increased histamine PD50 to 19.8 +/- 7.5 breath units, which was significantly greater than on control and placebo days.

ExcerptReferenceRelevance
"Gallopamil treatment for 12 months reduces BSM remodeling and prevents the occurrence of asthma exacerbations. "( Calcium channel blocker reduces airway remodeling in severe asthma. A proof-of-concept study.
Begueret, H; Berger, P; Dos Santos, P; Dournes, G; Dupin, I; Girodet, PO; Laurent, F; Marthan, R; Montaudon, M; Ozier, A; Thumerel, M; Trian, T, 2015
)
1.86
"Gallopamil pretreatment had no significant effect on methacholine-induced bronchoconstriction; methacholine PD50 increased to 13.4 +/- 5.5 breath units (p = NS)."( Modification of histamine- and methacholine-induced bronchoconstriction by calcium antagonist gallopamil in asthmatics.
Ahmed, T; Danta, I, 1992
)
1.22
"In Gallopamil-treated cats, higher levels of lactate were necessary to cause a similar decrease in pHi when compared to controls."( 31P and 1H NMR spectroscopy to study the effects of gallopamil on brain ischemia.
Chance, B; Kovach, AG; Leigh, JS; Ligeti, L; Osbakken, MD; Subramanian, HV, 1987
)
1.04
"Treatment with gallopamil and a VVI-pacemaker led to complete relief of all symptoms."( Vasospasm in smooth coronary arteries as a cause of asystole and syncope.
Fuerste, T; Haag, M; Unverdorben, M; Vallbracht, C; Weber, H, 1997
)
0.64
"Pretreatment with gallopamil increased histamine PD50 to 19.8 +/- 7.5 breath units, which was significantly greater than on control and placebo days (p < 0.01)."( Modification of histamine- and methacholine-induced bronchoconstriction by calcium antagonist gallopamil in asthmatics.
Ahmed, T; Danta, I, 1992
)
0.83
"Pretreatment with gallopamil protected the mitochondria against the ischemically induced changes in RCI, state 3 respiration."( Protective effects of gallopamil against ischemia and reperfusion damage.
Agnoletti, G; Boraso, A; Cargnoni, A; Condorelli, E; De Giuli, F; Ferrari, R; Ghielmi, S; Pasini, E, 1989
)
0.92

Toxicity

ExcerptReferenceRelevance
" Twenty-four-hour Holter monitoring, exercise testing, and adverse effects were controlled at days 7, 14, and 21."( Exercise-induced symptomatic and asymptomatic myocardial ischemia in patients with severe coronary artery disease: focus on the efficacy and safety of gallopamil.
Hohnloser, S; Just, H; Kosscheck, U; Meinertz, T; Weiss, C; Zehender, M, 1992
)
0.48
"Severe adverse effects associated with the use of calcium channel blockers do not occur very often."( [The spectrum of side effects of gallopamil in comparison with other calcium antagonists].
Hopf, R; Kaltenbach, M; Klepzig, H; Mildenberger, D, 1989
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
"We prospectively studied 10 patients with stable exertional ischaemia, selected from a larger group of patients referred for suspected coronary artery disease or to detect residual ischaemia after myocardial infarction, to evaluate pharmacokinetic changes during chronic treatment with gallopamil and its correlation with clinical efficacy in patients with coronary artery disease."( Efficacy and pharmacokinetics of gallopamil in patients with coronary artery disease.
Acanfora, D; Ferrara, N; Furgi, G; Guerra, N; Longobardi, G; Nicolino, A; Odierna, L; Rengo, F; Rosiello, R,
)
0.59

Compound-Compound Interactions

ExcerptReferenceRelevance
"In 18 patients (17 male and 1 female, 40 to 63 years old) with coronary heart disease, a randomized double-blind study was carried out to investigate in comparison to placebo, the antiischemic effects of 5, 10 and 20 mg isosorbide dinitrate (ISDN) alone and in combination with gallopamil (G: 25 and 50 mg) or 80 mg propranolol (P: 80 mg) on the ischemic ST-segment-depression in standardized exercise ECGs."( [The anti-ischemic effect of isosorbide dinitrate alone and in combination with gallopamil and propranolol].
Hopf, R; Kaltenbach, M; Sthler-Klich, HM, 1989
)
0.68

Bioavailability

Gallopamil has an absolute bioavailability of only 15% due to an extensive hepatic first-pass metabolism. The pharmacokinetics and bioavailability are not stereoselective at steady-state.

ExcerptReferenceRelevance
"A three cross-study was conducted in 12 healthy male volunteers to evaluate the relative bioavailability of three different gallopamil tablets: Product A-Galcan 25 mg, Product B-Galcan 50 mg and Product C-Procorum 50 mg."( Bioequivalency of three tableted gallopamil products.
Daneri, A; Legnazzi, P; Molinaro, M; Regazzi, MB; Tizzoni, M, 1989
)
0.76
"Despite its almost complete absorption following oral administration, gallopamil has an absolute bioavailability of only 15% due to an extensive hepatic first-pass metabolism."( [Pharmacokinetics and metabolism of gallopamil].
Eichelbaum, M, 1989
)
0.79
"The pharmacokinetics and bioavailability of the racemic drug gallopamil are not stereoselective at steady-state and are therefore not substantially altered compared with the single dose administration of gallopamil."( Pharmacokinetics and pharmacodynamics of R- and S-gallopamil during multiple dosing.
Eichelbaum, M; Gross, AS; Mikus, G; Mörike, K, 2000
)
0.8
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43

Dosage Studied

The dose-response relationship for the effect of gallopamil on excitation-contraction coupling has not been definitely established. The most frequently applied dosage was 1 film-coated tablet of gallopedamil 50 mg 2-3 times daily.

ExcerptRelevanceReference
"The effect of diazoxide, verapamil and compound D600 on calcium and isoproterenol dose-response relationships was investigated in isolated rabbit atrial preparations."( Effect of diazoxide, verapamil and compound D600 on isoproterenol and calcium-mediated dose-response relationships in isolated rabbit atrium.
Bristow, MR; Green, RD, 1977
)
0.26
"The effect of inhibiting isoprenaline-induced intracellular calcium accumulation on the degree of damage produced in the rat myocardium by this amine has been investigated by simultaneously dosing rats with the calcium antagonistic drug D600."( The effect of a calcium antagonist (D600) on isoprenaline-induced myocardial necrosis in the rat.
Powell, T; Rowles, PM; Steen, E; Woolf, N, 1979
)
0.26
" The dose-response relation with regard to the maximum rate of rise of the Ca spike showed no noticeable difference in effect between D600 and verapamil."( The effects of D600 and verapamil on action potential in the X-organ neuron of the crayfish.
Kuroda, T, 1976
)
0.26
" The dose-response curve for isoprenaline was shifted to the left by papaverine (3 times 10- minus 6 to 3 times 10- minus 5 M), in a dose-dependent manner, while that for calcium was not affected by the same concentration."( Effects of papaverine on isolated rabbit papillary muscle.
Endoh, M; Schümann, HJ, 1975
)
0.25
" The dose-response curve is bell shaped, and the maximum effect, which corresponds to 65% of the maximum effect of ryanodine, is achieved at therapeutic concentrations."( Effect of gallopamil on cardiac sarcoplasmic reticulum.
Galbani, P; Limbruno, U; Mariani, M; Ronca, G; Ronca-Testoni, S; Yu, G; Zucchi, R, 1992
)
0.69
" In isolated myocytes, a change in the holding potential from -90 to -70 mV displaces the gallopamil dose-response curve to block Ca2+ currents leftward by only 6-fold."( Marked dependence of the cardiac effects of gallopamil on the extracellular K(+)-concentration.
Herzig, S, 1992
)
0.77
" Dose-response curves to aerosolized methacholine or histamine were performed, without and following pretreatment with inhaled gallopamil (10 mg), on 6 different experiment days to determine the cumulative provocative dose (PD50) of each agonist in breath units which caused a 50% decrease in specific airway conductance (SGaw)."( Modification of histamine- and methacholine-induced bronchoconstriction by calcium antagonist gallopamil in asthmatics.
Ahmed, T; Danta, I, 1992
)
0.71
" The VST method is especially useful to quantify drug plasma levels in pharmacokinetic evaluation of sustained-release dosage forms, where the precise quantification of low levels of drug is critical."( Application of a variance-stabilizing transformation approach to linear regression of calibration lines.
Banfield, C; Bialer, M; Gonzalez, MA; McLean, AM; Ruggirello, DA, 1990
)
0.28
" For each period of treatment the gallopamil plasma concentrations were dosed during the ergometric test."( [Efficacy and duration of effect of two delayed-action preparations of gallopamil in patients with exercise angina].
Dovellini, EV; Fantoccoli, D; Fazzini, PF; Leoncini, M; Pucci, P; Sarro, F, 1990
)
0.79
" dosing of rats with gallopamil or verapamil, 13 and 2% of the dose, respectively, appeared in the bile as the N-glucuronide of the secondary amine metabolite over an 8-hr period."( Synthesis and identification of the N-glucuronides of norgallopamil and norverapamil, unusual metabolites of gallopamil and verapamil.
Mutlib, AE; Nelson, WL, 1990
)
0.84
" Relaxation dose-response curves for D600 or nifedipine were generated, and IC50 values were calculated."( Factors affecting rabbit mesenteric artery smooth muscle sensitivity to calcium antagonists.
Cipkus-Dubray, LA; Meisheri, KD; Sage, GP, 1990
)
0.28
" Propranolol also inhibited contractions to Ca in high K-containing solution and shifted the dose-response curve to the right."( Inhibitory action of propranolol on the contractions induced by nerve stimulations or calcium in the smooth muscle of rat vas deferens.
Inagaki, O; Kasuya, Y; Suzuki, N, 1986
)
0.27
" Higher concentrations of these antagonists shifted the Ca2+ dose-response curve to the right."( Adrenergic-cholinergic interactions in left atria. II. Comparison of the antagonism of inotropic responses to alpha- and beta-adrenoceptor stimulation and BAY K 8644 by carbachol, D-600, and nifedipine.
MacLeod, KM, 1987
)
0.27
" NE- and KCI-induced dose-response relationships were differentially depressed by SG-75 (NE much greater than KCI) and NIF (KCI much greater than NE)."( Effects of 2-nicotinamidoethyl nitrate on agonist-sensitive Ca++ release and Ca++ entry in rabbit aorta.
Hester, RK, 1985
)
0.27
" Dose-response curves were hyperbolic; Lineweaver-Burk plots revealed straight lines with different slopes intersecting near 1/Fmax, and indicating the following order of efficiency: Ni2+ greater than Ca2+ greater than Mn2+ much greater than Mg2+."( Competitive action of divalent cations and D600 in frog slow muscle fibers.
Krippeit-Drews, P; Schmidt, H, 1989
)
0.28
" During multiple oral dosing bioavailability increases to approximately 25% indicating a partial saturation of first-pass metabolism."( [Pharmacokinetics and metabolism of gallopamil].
Eichelbaum, M, 1989
)
0.55
"For effective treatment of coronary heart disease with calcium antagonists, knowledge of both the dose-response relationship of a remedy and equipotent dosage for comparison of different drugs is necessary."( [Dose-response relation of gallopamil in comparison with nifedipine, diltiazem and tiapamil in patients with coronary heart disease].
Fleischer, K; Forster, A; Hopf, R; Kaltenbach, M; Mohler, C; Schulz, PC, 1989
)
0.57
" The dose-response curves for CCK8 were shifted in parallel to the right by 10(-6) to 10(-5) M of the three benzodiazepines, although the maximum response to CCK8 was depressed by higher concentrations."( Cholecystokinin antagonism by benzodiazepines in the contractile response of the isolated guinea-pig gallbladder.
Kubota, K; Matsuda, I; Sugaya, K; Sunagane, N; Uruno, T, 1985
)
0.27
"To determine if there is a dose-response relationship for calcium channel blockers in preventing experimentally induced bronchoconstriction, we evaluated the effects of inhaled gallopamil (D600), a potent methoxy derivative of verapamil, on airway reactivity to methacholine and exercise in volunteers with mild asthma."( Dose response of inhaled gallopamil (D600), a calcium channel blocker, in attenuating airway reactivity to methacholine and exercise.
Ahrens, R; Harman, E; Hendeles, L; Hill, M; Massey, KL; Rutledge, DR, 1988
)
0.77
" CaCl2 dose-response (in the presence of 10(-5) mol."( Mechanism of hydralazine-induced relaxation of arterial smooth muscle.
Aloamaka, CP; Ebeigbe, AB, 1985
)
0.27
" The dose-response curve for isoprenaline was shifted to the right and downward in the presence of YC-93 in a concentration-dependent manner, and the positive inotropic action of calcium was also inhibited markedly by YC-93."( Dissociation of cyclic AMP and contractile responses to isoprenaline: effects of a dihydropyridine derivative, nicardipine (YC-93), on canine ventricular muscle.
Endoh, M; Taira, N; Yanagisawa, T, 1980
)
0.26
" Papaverine and theophylline caused a decrease both in the maximum height and the slope of dose-response curves induced by the three stimulants, and an increase in the cyclic AMP levels."( Smooth muscle relaxing drugs and guinea pig ileum.
Goto, J; Mukai, T; Takagi, K; Yamaguchi, E, 1981
)
0.26
" The most frequently applied dosage was 1 film-coated tablet of gallopamil 50 mg 2-3 times daily."( [Multicenter long-term study of gallopamil in patients with coronary heart disease].
Schiemann, J; Sućić, M, 1984
)
0.79
" Protoveratrine A increased the uptake of 22Na+ into the slices with a similar dose-response curve to that found for gamma-aminobutyrate release."( The role of Ca2+ in the protoveratrine-induced release of gamma-aminobutyrate from rat brain slices.
Minchin, MC, 1980
)
0.26
" After 2 weeks, aortic and portal vein strips were prepared from each rat for studies of cumulative dose-response curves to norepinephrine (NE) in Krebs' solution containing normal (2."( Effect of chronic treatment of spontaneously hypertensive rats with D 600.
Pang, CC; Sutter, MC,
)
0.13
" All three drugs inhibited norepinephrine (NE) and KCl dose-response curves in a concentration-dependent manner."( Spasmolytic action of verapamil, D600 and cinchocaine on the rat vas deferens.
Lin, CS; Swamy, VC, 1980
)
0.26
" Both gallopamil and verapamil inhibited the Ach-induced contractions of ovine tracheal smooth muscle, by shifting the dose-response curves to Ach to the right."( Ovine tracheal muscle contraction in vitro: inhibition by calcium channel blockers gallopamil and verapamil.
Abraham, WM; Ahmed, T; Chapman, GA; Jackowski, J, 1993
)
0.99
" The dose-response relationship for the effect of gallopamil on excitation-contraction coupling has not been definitely established."( Effect of gallopamil on excitation-contraction coupling.
Zucchi, R, 1996
)
0.95
" Dose-response curves revealed IC(50) values of 199+/-19 microM for verapamil, 466+/-151 microM for gallopamil and 326+/-67 microM for diltiazem."( Effects of phenylalkylamines and benzothiazepines on Ca(v)1.3-mediated Ca2+ currents in neonatal mouse inner hair cells.
Engel, J; Lacinova, L; Tarabova, B, 2007
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
benzenesAny benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives.
organic amino compoundA compound formally derived from ammonia by replacing one, two or three hydrogen atoms by organyl groups.
[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 (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency1.00000.100020.879379.4328AID588453
TDP1 proteinHomo sapiens (human)Potency20.45940.000811.382244.6684AID686978; AID686979
regulator of G-protein signaling 4Homo sapiens (human)Potency37.68580.531815.435837.6858AID504845
ParkinHomo sapiens (human)Potency20.59620.819914.830644.6684AID720573
arylsulfatase AHomo sapiens (human)Potency4.25621.069113.955137.9330AID720538
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency11.22020.01789.637444.6684AID588834
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.01610.005612.367736.1254AID624032
lamin isoform A-delta10Homo sapiens (human)Potency0.56230.891312.067628.1838AID1487
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency20.26771.000010.475628.1838AID1457
Ataxin-2Homo sapiens (human)Potency35.48130.011912.222168.7989AID588378
[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)0.01100.00032.63119.0000AID751841
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)Ki0.00540.00540.01160.0150AID751841
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)3.20000.00022.318510.0000AID681153
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)IC50 (µMol)0.02300.00132.24956.9000AID566280
Voltage-dependent L-type calcium channel subunit alpha-1DRattus norvegicus (Norway rat)IC50 (µMol)0.02300.00131.991510.0000AID566280
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)0.01100.00032.59559.0000AID751841
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)Ki0.00540.00540.02880.1030AID751841
Voltage-dependent L-type calcium channel subunit alpha-1SRattus norvegicus (Norway rat)IC50 (µMol)0.02300.00131.60206.9000AID566280
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)0.01100.00032.63119.0000AID751841
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)Ki0.00540.00540.01160.0150AID751841
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)0.01400.00032.25459.6000AID1207652; AID751841
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)Ki0.00540.00030.00720.0150AID751841
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (65)

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)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo 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)
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)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

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)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo 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)
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)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

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)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
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)
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)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (59)

Assay IDTitleYearJournalArticle
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID48972Antagonistic activity against K+ induced responses in canine coronary.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID346465Displacement of radiolabeled D 600 from verapamil site of L-type calcium channel2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID165537Inhibition of [Ca2+] uptake in rabbit aorta, K+.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
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.
AID752205Binding affinity to L-type calcium channel verapamil binding site (unknown origin) by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
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]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID48974Antagonistic activity against norepinephrine induced contraction in canine coronary1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID751841Binding affinity to L-Ca2+ channel verapamil site (unknown origin) by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID76669[Ca2+] antagonistic activity on contraction in guinea pig atria.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' 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]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1207652Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID48347[Ca2+] antagonistic activity on [Ca2+] current in cat papillary.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID681153TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells2001Chemical research in toxicology, Dec, Volume: 14, Issue:12
Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4.
AID566280Inhibition of rat L-type Ca2+ channel verapamil site2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID143602Binding affinity to displace 0.4 nM of [3H]- gallopamil in rat myocardial membranes1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Studies on Ca2+ channel antagonists. A 2-diazo-3,3,3-trifluoropropionamide derivative related to verapamil as a potential photoaffinity probe.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID195589Compound was evaluated for the displacement of [3H]gallopamil from specific binding sites on rat myocardial membrane particulates1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Studies on Ca2+ channel antagonists. 5-[(3,4-Dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2- isopropylpentyl isothiocyanate, a chemoaffinity ligand derived from verapamil.
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]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID175665Effective concentration for negative inotropic effect in rat myocardial ventricular strips1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Studies on Ca2+ channel antagonists. A 2-diazo-3,3,3-trifluoropropionamide derivative related to verapamil as a potential photoaffinity probe.
AID165539Inhibition of contraction in rabbit aorta, K+.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID340271Inhibition of L-type calcium channel2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
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]
AID681353TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in F4-6RADR cells1992Biochemical pharmacology, Jun-23, Volume: 43, Issue:12
Stereoisomers of calcium antagonists which differ markedly in their potencies as calcium blockers are equally effective in modulating drug transport by P-glycoprotein.
AID1336368Displacement of [3H]D888 from rat cerebral cortex calcium channel L type verapamil binding site measured after 120 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID1285669Displacement of [3H]D888 from rat cerebral cortex L-type calcium channel verapamil binding site2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID175483Compound was evaluated for the concentration dependent negative ionotropic effect in rat right myocardial ventricular strips1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Studies on Ca2+ channel antagonists. 5-[(3,4-Dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2- isopropylpentyl isothiocyanate, a chemoaffinity ligand derived from verapamil.
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
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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 (1,105)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990733 (66.33)18.7374
1990's295 (26.70)18.2507
2000's51 (4.62)29.6817
2010's20 (1.81)24.3611
2020's6 (0.54)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.02

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 Index28.02 (24.57)
Research Supply Index7.12 (2.92)
Research Growth Index4.10 (4.65)
Search Engine Demand Index42.09 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.02)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials88 (7.67%)5.53%
Reviews22 (1.92%)6.00%
Case Studies4 (0.35%)4.05%
Observational0 (0.00%)0.25%
Other1,034 (90.07%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Effects of Gallopamil on Bronchial Smooth Muscle Remodelling in Severe Asthma: a Double Blind Study. [NCT00896428]Phase 231 participants (Actual)Interventional2009-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]