DGIdb - VERAPAMIL Drug Record

VERAPAMIL chembl:CHEMBL6966 ApprovedAntineoplastic

Alternate Names:

VERAPAMIL
VERELAN
CP-165331
NSC-272306NA
CP-16533-1
TARKA
ISOPTIN
D-365
COVERA-HS
IPROVERATRIL
CALAN
VERAPAMILO
SECURON®
CP-165331 / CP-16533-1
ANSYR®
VERAPAMILUM
VÉRAPAMIL
pubchem.compound:2520
rxcui:11170
drugbank:00661
chemidplus:52-53-9
chembl:CHEMBL6966

Drug Info:

Drug Class	anti-arrhythmia agents
Year of Approval	1981
Drug Categories	selective calcium channel blockers with direct cardiac effects
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antihypertensive agent
Drug Categories	ace inhibitors and calcium channel blockers
Drug Categories	adrenergic alpha-1 receptor antagonists
Drug Categories	adrenergic alpha-antagonists
Drug Categories	adrenergic antagonists
Drug Categories	antiarrhythmic agents
Drug Categories	antihypertensive agents
Drug Categories	antihypertensive agents indicated for hypertension
Drug Categories	cytochrome p-450 cyp2c18 substrates
Drug Categories	cytochrome p-450 cyp2c8 inhibitors
Drug Categories	cytochrome p-450 cyp2c8 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c9 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2e1 substrates
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a5 inhibitors
Drug Categories	cytochrome p-450 cyp3a5 inhibitors (moderate)
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs that are mainly renally excreted
Drug Categories	mate 1 inhibitors
Drug Categories	mate 2 inhibitors
Drug Categories	mate inhibitors
Drug Categories	miscellaneous calcium-channel blocking agents
Drug Categories	oatp1b1/slco1b1 inhibitors
Drug Categories	oct1 inhibitors
Drug Categories	oct1 substrates
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	vasodilating agents
Drug Categories	verapamil and analogues

(6 More Sources)

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache
Morel et al., 1998, The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits., Br. J. Pharmacol.
Dilmac et al., 2004, Molecular determinants of frequency dependence and Ca2+ potentiation of verapamil block in the pore region of Cav1.2., Mol. Pharmacol.
Patel et al., 2005, Effect of serum withdrawal on the contribution of L-type calcium channels (CaV1.2) to intracellular Ca2+ responses and chemotaxis in cultured human vascular smooth muscle cells., Br. J. Pharmacol.
Beitelshees AL et al., 2009, CACNA1C gene polymorphisms, cardiovascular disease outcomes, and treatment response., Circ Cardiovasc Genet
Bacon et al., 1989, Potent and specific inhibition of IL-8-, IL-1 alpha- and IL-1 beta-induced in vitro human lymphocyte migration by calcium channel antagonists., Biochem. Biophys. Res. Commun.
Xu et al., 2008, Effect of amiodarone on Kv1.4 channel C-type inactivation: comparison of its effects with those induced by propafenone and verapamil., Pharmazie
van Noord C et al., 2009, Calcium channel blockers, NOS1AP, and heart-rate-corrected QT prolongation., Pharmacogenet Genomics
Brown et al., 1986, The effects of some slow channel blocking drugs on high affinity serotonin uptake by rat brain synaptosomes., Eur. J. Pharmacol.
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Dahllöf et al., Characterization of multidrug resistance in SEWA mouse tumor cells: increased glutathione transferase activity and reversal of resistance with verapamil., Anticancer Res.
Shigeto et al., 2007, Nateglinide and mitiglinide, but not sulfonylureas, induce insulin secretion through a mechanism mediated by calcium release from endoplasmic reticulum., J. Pharmacol. Exp. Ther.
Yamada et al., 2006, Protection conferred by myocardial ATP-sensitive K+ channels in pressure overload-induced congestive heart failure revealed in KCNJ11 Kir6.2-null mutant., J. Physiol. (Lond.)
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Ninomiya T et al., 2003, Verapamil, a Ca2+ entry blocker, targets the pore-forming subunit of cardiac type KATP channel (Kir6.2)., J Cardiovasc Pharmacol
Aguirre Ghiso et al., 1998, Secretion of urokinase and metalloproteinase-9 induced by staurosporine is dependent on a tyrosine kinase pathway in mammary tumor cells., Int. J. Cancer
Freeze et al., 2006, State-dependent verapamil block of the cloned human Ca(v)3.1 T-type Ca(2+) channel., Mol. Pharmacol.
Bergson P et al., 2011, Verapamil block of T-type calcium channels., Mol Pharmacol
Shchepotin et al., Apoptosis induced by hyperthermia and verapamil in vitro in a human colon cancer cell line., Int J Hyperthermia
Gong Y et al., 2015, PTPRD gene associated with blood pressure response to atenolol and resistant hypertension., J Hypertens
Jacob et al., 1996, Effects of trandolapril and verapamil on glucose transport in insulin-resistant rat skeletal muscle., Metab. Clin. Exp.
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
Li P et al., 2011, A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors., Drug Metab Dispos
Ridley et al., 2004, Lidoflazine is a high affinity blocker of the HERG K(+)channel., J. Mol. Cell. Cardiol.
Cheng et al., Isolated perfused and paced guinea pig heart to test for drug-induced changes of the QT interval., J Pharmacol Toxicol Methods
Schneider et al., 2005, Differential effects of human ether-a-go-go-related gene (HERG) blocking agents on QT duration variability in conscious dogs., Eur. J. Pharmacol.
Duan et al., 2007, Verapamil blocks HERG channel by the helix residue Y652 and F656 in the S6 transmembrane domain., Acta Pharmacol. Sin.
Shimizu et al., 2005, Specific therapy based on the genotype and cellular mechanism in inherited cardiac arrhythmias. Long QT syndrome and Brugada syndrome., Curr. Pharm. Des.
Collett et al., 1999, Modulation of the permeability of H2 receptor antagonists cimetidine and ranitidine by P-glycoprotein in rat intestine and the human colonic cell line Caco-2., J. Pharmacol. Exp. Ther.
Mickisch et al., 1991, Transgenic mice that express the human multidrug-resistance gene in bone marrow enable a rapid identification of agents that reverse drug resistance., Proc. Natl. Acad. Sci. U.S.A.
Colabufo NA et al., 2008, Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents., J Med Chem
Nesi G et al., 2014, SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity., Eur J Med Chem
Perestelo NR et al., 2011, Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes., Eur J Med Chem
Chae SW et al., 2015, Xanthone analogues as potent modulators of intestinal P-glycoprotein., Eur J Med Chem
Marks KM et al., 2011, The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes., J Nat Prod
Tang X et al., 2012, Synthesis and evaluation of nitric oxide-releasing DDB derivatives as potential Pgp-mediated MDR reversal agents in MCF-7/Adr cells., Bioorg Med Chem Lett
Gu X et al., 2012, Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors., Eur J Med Chem
Gu X et al., 2012, Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors., Bioorg Med Chem
Liu XL et al., 2008, Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein., Bioorg Med Chem
Nievergelt A et al., 2010, Identification of serotonin 5-HT1A receptor partial agonists in ginger., Bioorg Med Chem
Lou K et al., 2014, Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies., J Med Chem
Liu J et al., 2013, 20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs., Bioorg Med Chem
Silva GL et al., 2001, Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei., J Nat Prod
Walz et al., 1989, Similar effects of cyclosporine and verapamil on lymphokine, interleukin 2 receptor, and proto-oncogene expression., Transplantation
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Liu et al., 2003, Calmodulin is involved in heat shock signal transduction in wheat., Plant Physiol.
Chang SW et al., 2018, Genome-wide association study identifies pharmacogenomic loci linked with specific antihypertensive drug treatment and new-onset diabetes., Pharmacogenomics J
Vandell AG et al., 2012, G protein receptor kinase 4 polymorphisms: β-blocker pharmacogenetics and treatment-related outcomes in hypertension., Hypertension
Nielsen T et al., 2008, The KCNMB1 Glu65Lys polymorphism associates with reduced systolic and diastolic blood pressure in the Inter99 study of 5729 Danes., J Hypertens
Zhao Q et al., 2008, Interactions among genetic variants from contractile pathway of vascular smooth muscle cell in essential hypertension susceptibility of Chinese Han population., Pharmacogenet Genomics
Beitelshees AL et al., 2007, KCNMB1 genotype influences response to verapamil SR and adverse outcomes in the INternational VErapamil SR/Trandolapril STudy (INVEST)., Pharmacogenet Genomics
Dobrev D et al., 1999, The effects of verapamil and diltiazem on N-, P- and Q-type calcium channels mediating dopamine release in rat striatum., Br J Pharmacol
Wong IL et al., 2009, Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives., J Med Chem
Perrotton T et al., 2007, (R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1., J Biol Chem
Price ET et al., 2011, Liver X receptor α gene polymorphisms and variable cardiovascular outcomes in patients treated with antihypertensive therapy: results from the INVEST-GENES study., Pharmacogenet Genomics
Block et al., 1993, Transcriptional activation of low density lipoprotein receptor gene by angiotensin-converting enzyme inhibitors and Ca(2+)-channel blockers involves protein kinase C isoforms., Proc. Natl. Acad. Sci. U.S.A.
Takemura et al., 1992, Effect of verapamil on the class I major histocompatibility complex antigen expression in K562 chronic myelogenous leukemia cells treated with recombinant human interferon-gamma., Cancer Lett.
Tsukamoto et al., 1987, Effect of calcium channel blockers and trifluoperazine on rat liver regeneration., Eur. J. Pharmacol.
Perez-Reyes et al., 2009, Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs., J. Pharmacol. Exp. Ther.
Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation

VERAPAMIL CACNA1D

Interaction Types & Directionality:

inhibitor (inhibitory)

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache
VERAPAMIL CACNA1S

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

VERAPAMIL CYP3A4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of testosterone 6β-hydroxylation.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

Li P et al., 2011, A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors., Drug Metab Dispos

VERAPAMIL TPCN2

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
VERAPAMIL KCNA7

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand None

Publications:
VERAPAMIL KCNA10

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Publications:
VERAPAMIL NALCN

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Publications:
VERAPAMIL TPCN1

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Direct Interaction? False

Publications:
VERAPAMIL SLC29A4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

VERAPAMIL CACNA1C

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Morel et al., 1998, The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits., Br. J. Pharmacol.

Dilmac et al., 2004, Molecular determinants of frequency dependence and Ca2+ potentiation of verapamil block in the pore region of Cav1.2., Mol. Pharmacol.

VERAPAMIL CACNB4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Verapamil,Calan, Covera-HS

Novel drug target Established target

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache
VERAPAMIL CACNB3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Verapamil,Calan, Covera-HS

Novel drug target Established target

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache
VERAPAMIL CACNB1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Verapamil,Calan, Covera-HS

Novel drug target Established target

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

VERAPAMIL SLC6A4

Interaction Types & Directionality:

other/unknown

Interaction Info:

Publications:

Brown et al., 1986, The effects of some slow channel blocking drugs on high affinity serotonin uptake by rat brain synaptosomes., Eur. J. Pharmacol.

Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.

VERAPAMIL CACNA1F

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Verapamil,Calan, Covera-HS

Novel drug target Established target

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

VERAPAMIL KCNJ11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Shigeto et al., 2007, Nateglinide and mitiglinide, but not sulfonylureas, induce insulin secretion through a mechanism mediated by calcium release from endoplasmic reticulum., J. Pharmacol. Exp. Ther.

Yamada et al., 2006, Protection conferred by myocardial ATP-sensitive K+ channels in pressure overload-induced congestive heart failure revealed in KCNJ11 Kir6.2-null mutant., J. Physiol. (Lond.)

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

VERAPAMIL CACNA1G

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Freeze et al., 2006, State-dependent verapamil block of the cloned human Ca(v)3.1 T-type Ca(2+) channel., Mol. Pharmacol.

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

VERAPAMIL CACNB2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Verapamil,Calan, Covera-HS

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

VERAPAMIL KCNH2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Ridley et al., 2004, Lidoflazine is a high affinity blocker of the HERG K(+)channel., J. Mol. Cell. Cardiol.

Cheng et al., Isolated perfused and paced guinea pig heart to test for drug-induced changes of the QT interval., J Pharmacol Toxicol Methods

Schneider et al., 2005, Differential effects of human ether-a-go-go-related gene (HERG) blocking agents on QT duration variability in conscious dogs., Eur. J. Pharmacol.

VERAPAMIL CACNA1I

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

VERAPAMIL CACNA1B

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Dobrev D et al., 1999, The effects of verapamil and diltiazem on N-, P- and Q-type calcium channels mediating dopamine release in rat striatum., Br J Pharmacol

VERAPAMIL CACNA1A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Dobrev D et al., 1999, The effects of verapamil and diltiazem on N-, P- and Q-type calcium channels mediating dopamine release in rat striatum., Br J Pharmacol

VERAPAMIL CACNA1H

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Perez-Reyes et al., 2009, Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs., J. Pharmacol. Exp. Ther.
VERAPAMIL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation
VERAPAMIL ADRA1D

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation
VERAPAMIL ADRA1B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation
VERAPAMIL KCNJ5

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Na-Ca chanel blocker

Alteration KCNJ5:L168R

Publications:

VERAPAMIL IL1B

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Bacon et al., 1989, Potent and specific inhibition of IL-8-, IL-1 alpha- and IL-1 beta-induced in vitro human lymphocyte migration by calcium channel antagonists., Biochem. Biophys. Res. Commun.

VERAPAMIL KCNA4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Xu et al., 2008, Effect of amiodarone on Kv1.4 channel C-type inactivation: comparison of its effects with those induced by propafenone and verapamil., Pharmazie
VERAPAMIL NOS1AP

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

van Noord C et al., 2009, Calcium channel blockers, NOS1AP, and heart-rate-corrected QT prolongation., Pharmacogenet Genomics
VERAPAMIL GSTP1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Dahllöf et al., Characterization of multidrug resistance in SEWA mouse tumor cells: increased glutathione transferase activity and reversal of resistance with verapamil., Anticancer Res.
VERAPAMIL PLAU

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Aguirre Ghiso et al., 1998, Secretion of urokinase and metalloproteinase-9 induced by staurosporine is dependent on a tyrosine kinase pathway in mammary tumor cells., Int. J. Cancer
VERAPAMIL BAX

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Shchepotin et al., Apoptosis induced by hyperthermia and verapamil in vitro in a human colon cancer cell line., Int J Hyperthermia
VERAPAMIL PTPRD

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Gong Y et al., 2015, PTPRD gene associated with blood pressure response to atenolol and resistant hypertension., J Hypertens
VERAPAMIL SLC2A4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Jacob et al., 1996, Effects of trandolapril and verapamil on glucose transport in insulin-resistant rat skeletal muscle., Metab. Clin. Exp.

VERAPAMIL ABCB1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Collett et al., 1999, Modulation of the permeability of H2 receptor antagonists cimetidine and ranitidine by P-glycoprotein in rat intestine and the human colonic cell line Caco-2., J. Pharmacol. Exp. Ther.

Mickisch et al., 1991, Transgenic mice that express the human multidrug-resistance gene in bone marrow enable a rapid identification of agents that reverse drug resistance., Proc. Natl. Acad. Sci. U.S.A.

Colabufo NA et al., 2008, Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents., J Med Chem

VERAPAMIL IL2RA

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Walz et al., 1989, Similar effects of cyclosporine and verapamil on lymphokine, interleukin 2 receptor, and proto-oncogene expression., Transplantation
VERAPAMIL HSPA4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Liu et al., 2003, Calmodulin is involved in heat shock signal transduction in wheat., Plant Physiol.
VERAPAMIL PLEKHH2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Chang SW et al., 2018, Genome-wide association study identifies pharmacogenomic loci linked with specific antihypertensive drug treatment and new-onset diabetes., Pharmacogenomics J
VERAPAMIL GRK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Vandell AG et al., 2012, G protein receptor kinase 4 polymorphisms: β-blocker pharmacogenetics and treatment-related outcomes in hypertension., Hypertension

VERAPAMIL KCNIP1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Nielsen T et al., 2008, The KCNMB1 Glu65Lys polymorphism associates with reduced systolic and diastolic blood pressure in the Inter99 study of 5729 Danes., J Hypertens

Zhao Q et al., 2008, Interactions among genetic variants from contractile pathway of vascular smooth muscle cell in essential hypertension susceptibility of Chinese Han population., Pharmacogenet Genomics

Beitelshees AL et al., 2007, KCNMB1 genotype influences response to verapamil SR and adverse outcomes in the INternational VErapamil SR/Trandolapril STudy (INVEST)., Pharmacogenet Genomics

VERAPAMIL ABCC1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Wong IL et al., 2009, Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives., J Med Chem

Perrotton T et al., 2007, (R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1., J Biol Chem

VERAPAMIL NR1H3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Price ET et al., 2011, Liver X receptor α gene polymorphisms and variable cardiovascular outcomes in patients treated with antihypertensive therapy: results from the INVEST-GENES study., Pharmacogenet Genomics

VERAPAMIL LDLR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Block et al., 1993, Transcriptional activation of low density lipoprotein receptor gene by angiotensin-converting enzyme inhibitors and Ca(2+)-channel blockers involves protein kinase C isoforms., Proc. Natl. Acad. Sci. U.S.A.

VERAPAMIL KCNMB1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Nielsen T et al., 2008, The KCNMB1 Glu65Lys polymorphism associates with reduced systolic and diastolic blood pressure in the Inter99 study of 5729 Danes., J Hypertens

Zhao Q et al., 2008, Interactions among genetic variants from contractile pathway of vascular smooth muscle cell in essential hypertension susceptibility of Chinese Han population., Pharmacogenet Genomics

Beitelshees AL et al., 2007, KCNMB1 genotype influences response to verapamil SR and adverse outcomes in the INternational VErapamil SR/Trandolapril STudy (INVEST)., Pharmacogenet Genomics

VERAPAMIL MYC

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Takemura et al., 1992, Effect of verapamil on the class I major histocompatibility complex antigen expression in K562 chronic myelogenous leukemia cells treated with recombinant human interferon-gamma., Cancer Lett.

VERAPAMIL CXCL8

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Bacon et al., 1989, Potent and specific inhibition of IL-8-, IL-1 alpha- and IL-1 beta-induced in vitro human lymphocyte migration by calcium channel antagonists., Biochem. Biophys. Res. Commun.

VERAPAMIL TYMS

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Tsukamoto et al., 1987, Effect of calcium channel blockers and trifluoperazine on rat liver regeneration., Eur. J. Pharmacol.
VERAPAMIL TGFB1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
VERAPAMIL CACNG1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

DrugBank: DB00661

Version: 5.1.7

Alternate Names:

52-53-9 CAS Number

Alti-verapamil - 120mg Drug Brand

Alti-verapamil - 80mg Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories ace inhibitors and calcium channel blockers

Publications:

Dobrev D et al., 1999, The effects of verapamil and diltiazem on N-, P- and Q-type calcium channels mediating dopamine release in rat striatum., Br J Pharmacol

Morel et al., 1998, The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits., Br. J. Pharmacol.

Dilmac et al., 2004, Molecular determinants of frequency dependence and Ca2+ potentiation of verapamil block in the pore region of Cav1.2., Mol. Pharmacol.

TdgClinicalTrial: VERAPAMIL
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antihypertensive agent

Drug Class Small Molecule

FDA Approval approved

Publications:
TEND: VERAPAMIL
- Version: 01-August-2011
Alternate Names:

Drug Info:

Year of Approval 1981

Drug Class anti-arrhythmia agents

Publications:

DTC: VERAPAMIL

Version: 02-September-2020

Alternate Names:

CHEMBL6966 ChEMBL Drug ID

Drug Info:

Publications:

Chae SW et al., 2015, Xanthone analogues as potent modulators of intestinal P-glycoprotein., Eur J Med Chem

Perestelo NR et al., 2011, Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes., Eur J Med Chem

Nesi G et al., 2014, SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity., Eur J Med Chem

NCI: VERAPAMIL

Version: 14-September-2017

Alternate Names:

C928 NCI drug code

Drug Info:

Publications:

Bacon et al., 1989, Potent and specific inhibition of IL-8-, IL-1 alpha- and IL-1 beta-induced in vitro human lymphocyte migration by calcium channel antagonists., Biochem. Biophys. Res. Commun.

Liu et al., 2003, Calmodulin is involved in heat shock signal transduction in wheat., Plant Physiol.

Mickisch et al., 1991, Transgenic mice that express the human multidrug-resistance gene in bone marrow enable a rapid identification of agents that reverse drug resistance., Proc. Natl. Acad. Sci. U.S.A.

PharmGKB: verapamil

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Chang SW et al., 2018, Genome-wide association study identifies pharmacogenomic loci linked with specific antihypertensive drug treatment and new-onset diabetes., Pharmacogenomics J

Beitelshees AL et al., 2007, KCNMB1 genotype influences response to verapamil SR and adverse outcomes in the INternational VErapamil SR/Trandolapril STudy (INVEST)., Pharmacogenet Genomics

Zhao Q et al., 2008, Interactions among genetic variants from contractile pathway of vascular smooth muscle cell in essential hypertension susceptibility of Chinese Han population., Pharmacogenet Genomics

TTD: Verapamil
- Version: 2020.06.01
Alternate Names:

D0R0FE TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL6966
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
GuideToPharmacology: 135651305
- Version: 29-September-2020
Alternate Names:

Drug Info:

Publications:
CGI: Verapamil
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False
Direct Interaction?	False

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Antagonist

Details of the Assay for Interaction	Inhibition of testosterone 6β-hydroxylation.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Trial Name	Verapamil,Calan, Covera-HS
Novel drug target	Established target

52-53-9	CAS Number
Alti-verapamil - 120mg	Drug Brand
Alti-verapamil - 80mg	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	ace inhibitors and calcium channel blockers

VERAPAMIL Drug Record

VERAPAMIL chembl:CHEMBL6966 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory) blocker (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Antagonist

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of testosterone 6&beta;-hydroxylation. Specific Action of the Ligand Inhibition Endogenous Drug? False

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand None

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Inhibition Direct Interaction? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Verapamil,Calan, Covera-HS Novel drug target Established target

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Verapamil,Calan, Covera-HS Novel drug target Established target

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Verapamil,Calan, Covera-HS Novel drug target Established target

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality: other/unknown

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Verapamil,Calan, Covera-HS Novel drug target Established target

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name Verapamil,Calan, Covera-HS

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache Dobrev D et al., 1999, The effects of verapamil and diltiazem on N-, P- and Q-type calcium channels mediating dopamine release in rat striatum., Br J Pharmacol

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache Dobrev D et al., 1999, The effects of verapamil and diltiazem on N-, P- and Q-type calcium channels mediating dopamine release in rat striatum., Br J Pharmacol

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Perez-Reyes et al., 2009, Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Publications: Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Publications: Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Publications: Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation

Interaction Types & Directionality: n/a

Interaction Info: Drug family Na-Ca chanel blocker Alteration KCNJ5:L168R

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of testosterone 6β-hydroxylation.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand None

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Verapamil,Calan, Covera-HS

Novel drug target Established target

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Verapamil,Calan, Covera-HS

Novel drug target Established target

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Verapamil,Calan, Covera-HS

Novel drug target Established target

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality:

other/unknown

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Verapamil,Calan, Covera-HS

Novel drug target Established target

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Verapamil,Calan, Covera-HS

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Dobrev D et al., 1999, The effects of verapamil and diltiazem on N-, P- and Q-type calcium channels mediating dopamine release in rat striatum., Br J Pharmacol

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache

Dobrev D et al., 1999, The effects of verapamil and diltiazem on N-, P- and Q-type calcium channels mediating dopamine release in rat striatum., Br J Pharmacol

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Perez-Reyes et al., 2009, Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality:

antagonist (inhibitory)

Publications:

Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation

Interaction Types & Directionality:

antagonist (inhibitory)

Publications:

Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation

Interaction Types & Directionality:

antagonist (inhibitory)

Publications:

Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Na-Ca chanel blocker

Alteration KCNJ5:L168R

Interaction Types & Directionality:

n/a

Publications:

Bacon et al., 1989, Potent and specific inhibition of IL-8-, IL-1 alpha- and IL-1 beta-induced in vitro human lymphocyte migration by calcium channel antagonists., Biochem. Biophys. Res. Commun.

Interaction Types & Directionality:

n/a

Publications:

Xu et al., 2008, Effect of amiodarone on Kv1.4 channel C-type inactivation: comparison of its effects with those induced by propafenone and verapamil., Pharmazie

Interaction Types & Directionality:

n/a

Publications:

van Noord C et al., 2009, Calcium channel blockers, NOS1AP, and heart-rate-corrected QT prolongation., Pharmacogenet Genomics

Interaction Types & Directionality:

n/a

Publications:

Dahllöf et al., Characterization of multidrug resistance in SEWA mouse tumor cells: increased glutathione transferase activity and reversal of resistance with verapamil., Anticancer Res.

Interaction Types & Directionality:

n/a

Publications:

Aguirre Ghiso et al., 1998, Secretion of urokinase and metalloproteinase-9 induced by staurosporine is dependent on a tyrosine kinase pathway in mammary tumor cells., Int. J. Cancer

Interaction Types & Directionality:

n/a

Publications:

Shchepotin et al., Apoptosis induced by hyperthermia and verapamil in vitro in a human colon cancer cell line., Int J Hyperthermia

Interaction Types & Directionality:

n/a

Publications:

Gong Y et al., 2015, PTPRD gene associated with blood pressure response to atenolol and resistant hypertension., J Hypertens

Interaction Types & Directionality:

n/a

Publications:

Jacob et al., 1996, Effects of trandolapril and verapamil on glucose transport in insulin-resistant rat skeletal muscle., Metab. Clin. Exp.

Interaction Types & Directionality:

n/a