DGIdb - DESIPRAMINE Drug Record

DESIPRAMINE chembl:CHEMBL72 Approved

Alternate Names:

DESIPRAMINE
DESIPRAMINUM
5-(GAMMA-METHYLAMINOPROPYL)IMINODIBENZYL
JB-8181
MONODEMETHYLIMIPRAMINE
NORIMIPRAMINE
DESIPRAMIN
DMI
EX-4355
DÉMÉTHYLIMIPRAMINE
3-(10,11-DIHYDRO-5H-DIBENZO[B,F]AZEPIN-5-YL)-N-METHYLPROPAN-1-AMINE
TREYZAFAGIT®
DEMETHYLIMIPRAMINE
DESMETHYLIMIPRAMINE
N-(3-METHYLAMINOPROPYL)IMINOBIBENZYL
5-(Γ-METHYLAMINOPROPYL)IMINODIBENZYL
NORPRAMIN®
DESIPRAMINA
PERTROFANE®
chemidplus:50-47-5
pubchem.compound:2995
chembl:CHEMBL72
rxcui:3247
drugbank:01151

Drug Info:

FDA Approval	Approved before 1982
Drug Class	small molecule
Drug Indications	Antidepressive Agents, Tricyclic
Year of Approval	approved before 1982
Drug Class	antidepressive agents, tricyclic

(3 More Sources)

Publications:

Sawynok et al., 1999, Peripheral antinociceptive actions of desipramine and fluoxetine in an inflammatory and neuropathic pain test in the rat., Pain
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
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
Mudunkotuwa et al., 1996, Desipramine administration in the olfactory bulbectomized rat: changes in brain beta-adrenoceptor and 5-HT2A binding sites and their relationship to behaviour., Br. J. Pharmacol.
Matsumoto et al., 1994, Beta 2- but not beta 1-adrenoceptors are involved in desipramine enhancement of aggressive behavior in long-term isolated mice., Pharmacol. Biochem. Behav.
Sapena et al., 1996, Desipramine treatment differently down-regulates beta-adrenoceptors of freshly isolated neurons and astrocytes., Eur. J. Pharmacol.
Samnick et al., 2004, Technetium-99m labeled 1-(4-fluorobenzyl)-4-(2-mercapto-2-methyl-4-azapentyl)-4-(2-mercapto-2-methylpropylamino)-piperidine and iodine-123 metaiodobenzylguanidine for studying cardiac adrenergic function: a comparison of the uptake characteristics in vascular smooth muscle cells and neonatal cardiac myocytes, and an investigation in rats., Nucl. Med. Biol.
Bürgi et al., 2003, Antidepressant-induced switch of beta 1-adrenoceptor trafficking as a mechanism for drug action., J. Biol. Chem.
Leathart JB et al., 1998, CYP2D6 phenotype-genotype relationships in African-Americans and Caucasians in Los Angeles., Pharmacogenetics
Dalén P et al., 1998, 10-Hydroxylation of nortriptyline in white persons with 0, 1, 2, 3, and 13 functional CYP2D6 genes., Clin Pharmacol Ther
Spina E et al., 1997, Relationship between plasma desipramine levels, CYP2D6 phenotype and clinical response to desipramine: a prospective study., Eur J Clin Pharmacol
Chen S et al., 1996, The cytochrome P450 2D6 (CYP2D6) enzyme polymorphism: screening costs and influence on clinical outcomes in psychiatry., Clin Pharmacol Ther
Dahl ML et al., 1996, Steady-state plasma levels of nortriptyline and its 10-hydroxy metabolite: relationship to the CYP2D6 genotype., Psychopharmacology (Berl)
Bluhm RE et al., 1993, Genetically determined drug-metabolizing activity and desipramine-associated cardiotoxicity: a case report., Clin Pharmacol Ther
Nielsen KK et al., 1994, Single-dose kinetics of clomipramine: relationship to the sparteine and S-mephenytoin oxidation polymorphisms., Clin Pharmacol Ther
Spina E et al., 1984, Phenotypic consistency in hydroxylation of desmethylimipramine and debrisoquine in healthy subjects and in human liver microsomes., Clin Pharmacol Ther
Brøsen K et al., 1986, Imipramine demethylation and hydroxylation: impact of the sparteine oxidation phenotype., Clin Pharmacol Ther
Brøsen K et al., 1986, Steady-state concentrations of imipramine and its metabolites in relation to the sparteine/debrisoquine polymorphism., Eur J Clin Pharmacol
Brøsen K et al., 1988, First-pass metabolism of imipramine and desipramine: impact of the sparteine oxidation phenotype., Clin Pharmacol Ther
Nguyen HQ et al., 2016, The Use of In Vitro Data and Physiologically-Based Pharmacokinetic Modeling to Predict Drug Metabolite Exposure: Desipramine Exposure in Cytochrome P4502D6 Extensive and Poor Metabolizers Following Administration of Imipramine., Drug Metab Dispos
Hicks JK et al., 2013, Clinical Pharmacogenetics Implementation Consortium guideline for CYP2D6 and CYP2C19 genotypes and dosing of tricyclic antidepressants., Clin Pharmacol Ther
de Vos A et al., 2011, Association between CYP2C19*17 and metabolism of amitriptyline, citalopram and clomipramine in Dutch hospitalized patients., Pharmacogenomics J
Forget P et al., 2008, Life-threatening dextromethorphan intoxication associated with interaction with amitriptyline in a poor CYP2D6 metabolizer: a single case re-exposure study., J Pain Symptom Manage
Koski A et al., 2007, A fatal doxepin poisoning associated with a defective CYP2D6 genotype., Am J Forensic Med Pathol
Schenk PW et al., 2008, Association of graded allele-specific changes in CYP2D6 function with imipramine dose requirement in a large group of depressed patients., Mol Psychiatry
Johnson M et al., 2006, A poor metabolizer for cytochromes P450 2D6 and 2C19: a case report on antidepressant treatment., CNS Spectr
Stephan PL et al., 2006, Adverse drug reactions following nonresponse in a depressed patient with CYP2D6 deficiency and low CYP 3A4/5 activity., Pharmacopsychiatry
Goetz MP et al., 2005, Pharmacogenetics of tamoxifen biotransformation is associated with clinical outcomes of efficacy and hot flashes., J Clin Oncol
Koski A et al., 2006, CYP2D6 and CYP2C19 genotypes and amitriptyline metabolite ratios in a series of medicolegal autopsies., Forensic Sci Int
Vandel P et al., 2004, Clomipramine, fluoxetine and CYP2D6 metabolic capacity in depressed patients., Hum Psychopharmacol
Steimer W et al., 2004, Allele-specific change of concentration and functional gene dose for the prediction of steady-state serum concentrations of amitriptyline and nortriptyline in CYP2C19 and CYP2D6 extensive and intermediate metabolizers., Clin Chem
Furman KD et al., 2004, Impact of CYP2D6 intermediate metabolizer alleles on single-dose desipramine pharmacokinetics., Pharmacogenetics
Roberts RL et al., 2004, No evidence of increased adverse drug reactions in cytochrome P450 CYP2D6 poor metabolizers treated with fluoxetine or nortriptyline., Hum Psychopharmacol
Kawanishi C et al., 2004, Increased incidence of CYP2D6 gene duplication in patients with persistent mood disorders: ultrarapid metabolism of antidepressants as a cause of nonresponse. A pilot study., Eur J Clin Pharmacol
Kirchheiner J et al., 2003, Trimipramine pharmacokinetics after intravenous and oral administration in carriers of CYP2D6 genotypes predicting poor, extensive and ultrahigh activity., Pharmacogenetics
Kirchheiner J et al., 2003, Effects of polymorphisms in CYP2D6, CYP2C9, and CYP2C19 on trimipramine pharmacokinetics., J Clin Psychopharmacol
Dahl ML et al., 1992, Analysis of the CYP2D6 gene in relation to debrisoquin and desipramine hydroxylation in a Swedish population., Clin Pharmacol Ther
Kirchheiner J et al., 2002, Contributions of CYP2D6, CYP2C9 and CYP2C19 to the biotransformation of E- and Z-doxepin in healthy volunteers., Pharmacogenetics
Murphy GM Jr et al., 2001, CYP2D6 genotyping with oligonucleotide microarrays and nortriptyline concentrations in geriatric depression., Neuropsychopharmacology
Bergmann TK et al., 2001, Duplication of CYP2D6 predicts high clearance of desipramine but high clearance does not predict duplication of CYP2D6., Eur J Clin Pharmacol
Shimoda K et al., 2000, Metabolism of desipramine in Japanese psychiatric patients: the impact of CYP2D6 genotype on the hydroxylation of desipramine., Pharmacol Toxicol
1999, Clomipramine dose-effect study in patients with depression: clinical end points and pharmacokinetics. Danish University Antidepressant Group (DUAG)., Clin Pharmacol Ther
Paczkowski FA et al., 2007, chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model., J Biol Chem
Weinshenker et al., 2002, Regulation of norepinephrine transporter abundance by catecholamines and desipramine in vivo., Brain Res.
Bryan-Lluka et al., 2003, chi-Conopeptide MrIA partially overlaps desipramine and cocaine binding sites on the human norepinephrine transporter., J. Biol. Chem.
Zavosh et al., 1999, Desipramine treatment decreases 3H-nisoxetine binding and norepinephrine transporter mRNA in SK-N-SHSY5Y cells., Brain Res. Bull.
Zhu et al., 2004, The persistent membrane retention of desipramine causes lasting inhibition of norepinephrine transporter function., Neurochem. Res.
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Ordway et al., 2005, Norepinephrine transporter function and desipramine: residual drug effects versus short-term regulation., J. Neurosci. Methods
Osadchii et al., 2007, Temporal changes in myocardial adrenergic regulation with the progression to pump dysfunction after chronic beta-adrenoreceptor activation in rats., Pflugers Arch.
Prenner et al., 2007, Reduction of high-affinity beta2-adrenergic receptor binding by hyperforin and hyperoside on rat C6 glioblastoma cells measured by fluorescence correlation spectroscopy., Biochemistry
Abadie et al., 1996, Modulation of noradrenaline release from isolated human atrial appendages., J. Auton. Nerv. Syst.
Hoffman et al., 1998, In vivo electrochemical studies of dopamine clearance in the rat substantia nigra: effects of locally applied uptake inhibitors and unilateral 6-hydroxydopamine lesions., J. Neurochem.
Holmes et al., 2002, Evaluation of antidepressant-related behavioral responses in mice lacking the serotonin transporter., Neuropsychopharmacology
Gould et al., 2006, A comparison of the chronic treatment effects of venlafaxine and other antidepressants on serotonin and norepinephrine transporters., Biol. Psychiatry
Zhou et al., 2006, Evidence that serotonin reuptake modulators increase the density of serotonin innervation in the forebrain., J. Neurochem.
Wu GS et al., 2011, Sequence polymorphisms of MC1R gene and their association with depression and antidepressant response., Psychiatr Genet

DESIPRAMINE MC1R

Interaction Score: 2.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21052032

Sources:
PharmGKB
DESIPRAMINE SLC6A2

Interaction Score: 1.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17428804 12137927 12837768 10424850 15002740 9537821 11752352 15814154

Sources:
DTC TdgClinicalTrial TEND PharmGKB
DESIPRAMINE SLC6A4

Interaction Score: 0.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
9422361 12464448 16140280 9537821 16300628

Sources:
TdgClinicalTrial TEND
DESIPRAMINE CHRM2

Interaction Score: 0.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7855217 17016423 17139284

Sources:
TdgClinicalTrial TEND
DESIPRAMINE ADRB1

Interaction Score: 0.35

Interaction Types & Directionality:

other/unknown

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8730743 7816863 8741184 15093822 12393876

Sources:
TdgClinicalTrial TEND
DESIPRAMINE CYP2D6

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9918137 9585799 9049581 8941025 8867869 8422746 8181196 6488689 3769385 3533565 3356084 27440861 23486447 20531370 18359183 17721180 17667959 17008819 16871470 16361630 16024198 15252821 15205367 15115913 14716707 14652703 14646691 14520122 1346258 12360109 11682257 11417443 10895986 10460069

Sources:
DTC PharmGKB FDA
DESIPRAMINE CHRM1

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7855217 17016423 17139284

Sources:
TdgClinicalTrial TEND
DESIPRAMINE ADRB2

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7816863 17558518 17417877 8741184 8988485

Sources:
TdgClinicalTrial TEND
DESIPRAMINE ARSA

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DESIPRAMINE HRH1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10467920 7855217

Sources:
TdgClinicalTrial TEND
DESIPRAMINE BDNF

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
DESIPRAMINE THPO

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DESIPRAMINE ABCB1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
DESIPRAMINE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC PharmGKB
DESIPRAMINE CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

TEND: DESIPRAMINE
- Version: 01-August-2011
Alternate Names:

DESIPRAMINE Primary Drug Name

Drug Info:

Drug Class antidepressive agents, tricyclic

Year of Approval approved before 1982

Publications:
TdgClinicalTrial: DESIPRAMINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Antidepressive Agents, Tricyclic

Drug Class small molecule

FDA Approval Approved before 1982

Publications:
DTC: DESIPRAMINE
- Version: 02-September-2020
Alternate Names:

CHEMBL72 ChEMBL Drug ID

Drug Info:

Publications:

Paczkowski FA et al., 2007, chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model., J Biol Chem

PharmGKB: desipramine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Leathart JB et al., 1998, CYP2D6 phenotype-genotype relationships in African-Americans and Caucasians in Los Angeles., Pharmacogenetics

Bluhm RE et al., 1993, Genetically determined drug-metabolizing activity and desipramine-associated cardiotoxicity: a case report., Clin Pharmacol Ther

de Vos A et al., 2011, Association between CYP2C19*17 and metabolism of amitriptyline, citalopram and clomipramine in Dutch hospitalized patients., Pharmacogenomics J

TTD: Desipramine
- Version: 2020.06.01
Alternate Names:

D01UTL TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL72
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Desipramine
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Trial Name	-
Novel drug target	Established target

Trial Name	-
Novel drug target	Established target

Trial Name	-
Novel drug target	Established target

Trial Name	-
Novel drug target	Established target

DESIPRAMINE Drug Record

DESIPRAMINE chembl:CHEMBL72 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21052032

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17428804 12137927 12837768 10424850 15002740 9537821 11752352 15814154

Sources: DTC TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 9422361 12464448 16140280 9537821 16300628

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 7855217 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: other/unknown

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 8730743 7816863 8741184 15093822 12393876

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

Sources: DTC PharmGKB FDA

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 7855217 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 7816863 17558518 17417877 8741184 8988485

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10467920 7855217

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

TEND: DESIPRAMINE

Alternate Names: DESIPRAMINE Primary Drug Name

Drug Info: Drug Class antidepressive agents, tricyclic Year of Approval approved before 1982

Publications:

TdgClinicalTrial: DESIPRAMINE

Alternate Names:

Drug Info: Drug Indications Antidepressive Agents, Tricyclic Drug Class small molecule FDA Approval Approved before 1982

Publications:

DTC: DESIPRAMINE

Alternate Names: CHEMBL72 ChEMBL Drug ID

Drug Info:

Publications: Paczkowski FA et al., 2007, chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model., J Biol Chem

PharmGKB: desipramine

Alternate Names:

Drug Info:

TTD: Desipramine

Interaction Types & Directionality:

n/a

PMIDs:
21052032

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17428804 12137927 12837768 10424850 15002740 9537821 11752352 15814154

Sources:
DTC TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
9422361 12464448 16140280 9537821 16300628

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7855217 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

other/unknown

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8730743 7816863 8741184 15093822 12393876

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

Sources:
DTC PharmGKB FDA

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7855217 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7816863 17558518 17417877 8741184 8988485

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10467920 7855217

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Alternate Names:

DESIPRAMINE Primary Drug Name

Drug Info:

Drug Class antidepressive agents, tricyclic

Year of Approval approved before 1982

Drug Info:

Drug Indications Antidepressive Agents, Tricyclic

Drug Class small molecule

FDA Approval Approved before 1982

Alternate Names:

CHEMBL72 ChEMBL Drug ID

Publications:

Paczkowski FA et al., 2007, chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model., J Biol Chem

Alternate Names:

D01UTL TTD Drug ID