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Identification
NameDesipramine
Accession NumberDB01151  (APRD00022, DB07682)
Typesmall molecule
Groupsapproved
Description

Desipramine hydrochloride is a dibenzazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, desipramine does not affect mood or arousal, but may cause sedation. In depressed individuals, desipramine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Secondary amine TCAs, such as desipramine and nortriptyline, are more potent inhibitors of norepinephrine reuptake than tertiary amine TCAs, such as amitriptyline and doxepine. TCAs also down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Desipramine exerts less anticholinergic and sedative side effects compared to tertiary amine TCAs, such as amitriptyline and clomipramine. Desipramine may be used to treat depression, neuropathic pain (unlabeled use), agitation and insomnia (unlabeled use) and attention-deficit hyperactivity disorder (unlabeled use).

Structure
Thumb
Synonyms
SynonymLanguageCode
5-(γ-methylaminopropyl)iminodibenzylNot AvailableNot Available
DéméthylimipramineFrenchNot Available
DesipraminDutchNot Available
DesmethylimipramineNot AvailableNot Available
DMINot AvailableNot Available
MonodemethylimipramineNot AvailableNot Available
N-(3-methylaminopropyl)iminobibenzylNot AvailableNot Available
NorimipramineNot AvailableNot Available
Salts
Name/CAS Structure Properties
Desipramine Hydrochloride
Thumb
  • InChI Key: XAEWZDYWZHIUCT-UHFFFAOYSA-N
  • Monoisotopic Mass: 302.154976453
  • Average Mass: 302.842
DBSALT000042
Brand names
NameCompany
NorpraminSanofi-Aventis
PertofranNot Available
PertofraneNot Available
Brand mixturesNot Available
Categories
CAS number50-47-5
WeightAverage: 266.3807
Monoisotopic: 266.178298714
Chemical FormulaC18H22N2
InChI KeyInChIKey=HCYAFALTSJYZDH-UHFFFAOYSA-N
InChI
InChI=1S/C18H22N2/c1-19-13-6-14-20-17-9-4-2-7-15(17)11-12-16-8-3-5-10-18(16)20/h2-5,7-10,19H,6,11-14H2,1H3
IUPAC Name
(3-{2-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl}propyl)(methyl)amine
SMILES
CNCCCN1C2=CC=CC=C2CCC2=CC=CC=C12
Mass Specshow(11 KB)
Taxonomy
KingdomOrganic Compounds
SuperclassHeterocyclic Compounds
ClassBenzazepines
SubclassDibenzazepines
Direct parentDibenzazepines
Alternative parentsAzepines; Benzene and Substituted Derivatives; Tertiary Amines; Polyamines; Dialkylamines
Substituentsazepine; benzene; tertiary amine; secondary amine; secondary aliphatic amine; polyamine; amine; organonitrogen compound
Classification descriptionThis compound belongs to the dibenzazepines. These are compounds with two benzene rings connected by an azepine ring.
Pharmacology
IndicationFor relief of symptoms in various depressive syndromes, especially endogenous depression. It has also been used to manage chronic peripheral neuropathic pain, as a second line agent for the management of anxiety disorders (e.g. panic disorder, generalized anxiety disorder), and as a second or third line agent in the ADHD management.
PharmacodynamicsDesipramine, a secondary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. It is the active metabolite of imipramine, a tertiary amine TCA. The acute effects of desipramine include inhibition of noradrenaline re-uptake at noradrenergic nerve endings and inhibition of serotonin (5-hydroxy tryptamine, 5HT) re-uptake at the serotoninergic nerve endings in the central nervous system. Desipramine exhibits greater noradrenergic re-uptake inhibition compared to the tertiary amine TCA imipramine. In addition to inhibiting neurotransmitter re-uptake, desipramine down-regulates beta-adrenergic receptors in the cerebral cortex and sensitizes serotonergic receptors with chronic use. The overall effect is increased serotonergic transmission. Antidepressant effects are typically observed 2 - 4 weeks following the onset of therapy though some patients may require up to 8 weeks of therapy prior to symptom improvement. Patients experiencing more severe depressive episodes may respond quicker than those with mild depressive symptoms.
Mechanism of actionDesipramine is a tricyclic antidepressant (TCA) that selectively blocks reuptake of norepinephrine (noradrenaline) from the neuronal synapse. It also inhibits serotonin reuptake, but to a lesser extent compared to tertiary amine TCAs such as imipramine. Inhibition of neurotransmitter reuptake increases stimulation of the post-synaptic neuron. Chronic use of desipramine also leads to down-regulation of beta-adrenergic receptors in the cerebral cortex and sensitization of serotonergic receptors. An overall increase in serotonergic transmission likely confers desipramine its antidepressant effects. Desipramine also possesses minor anticholinergic activity, through its affinity for muscarinic receptors. TCAs are believed to act by restoring normal levels of neurotransmitters via synaptic reuptake inhibition and by increasing serotonergic neurotransmission via serotonergic receptor sensitization in the central nervous system.
AbsorptionDesipramine hydrochloride is rapidly and almost completely absorbed from the gastrointestinal tract. It undergoes extensive first-pass metabolism. Peak plasma concentrations are attained 4 - 6 hours following oral administration.
Volume of distributionNot Available
Protein binding73-92% bound to plasma proteins
Metabolism

Desipramine is extensively metabolized in the liver by CYP2D6 (major) and CYP1A2 (minor) to 2-hydroxydesipramine, an active metabolite. 2-hydroxydesipramine is thought to retain some amine reuptake inhibition and may possess cardiac depressant activity. The 2-hydroxylation metabolic pathway of desipramine is under genetic control.

SubstrateEnzymesProduct
Desipramine
2-hydroxydesipramineDetails
2-hydroxydesipramine
    2-hydroxy-desipramine glucuronideDetails
    Route of eliminationDesipramine is metabolized in the liver, and approximately 70% is excreted in the urine.
    Half life7-60+ hours; 70% eliminated renally
    ClearanceNot Available
    ToxicityMale mice: LD50 = 290 mg/kg, female rats: LD50 = 320 mg/kg. Antagonism of the histamine H1 and α1 receptors can lead to sedation and hypotension. Antimuscarinic activity confers anticholinergic side effects such as blurred vision, dry mouth, constipation and urine retention may occur. Cardiotoxicity may occur with high doses of desipramine. Cardiovascular side effects in postural hypotension, tachycardia, hypertension, ECG changes and congestive heart failure. Psychotoxic effects include impaired memory and delirium. Induction of hypomanic or manic episodes may occur in patients with a history of bipolar disorder. Withdrawal symptoms include GI disturbances (e.g. nausea, vomiting, abdominal pain, diarrhea), anxiety, insomnia, nervousness, headache and malaise.
    Affected organisms
    • Humans and other mammals
    Pathways
    PathwayCategorySMPDB ID
    Imipramine Action PathwayDrug actionSMP00422
    Desipramine Action PathwayDrug actionSMP00423
    Desipramine Metabolism PathwayDrug metabolismSMP00626
    Imipramine Metabolism PathwayDrug metabolismSMP00625
    SNP Mediated Effects
    Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
    Cytochrome P450 2D6
    Gene symbol: CYP2D6
    UniProt: P10635
    rs3892097 CYP2D6*4A AllelePoor drug metabolizer, lower dose requirements, higher risk for adverse side effects18070221
    SNP Mediated Adverse Drug ReactionsNot Available
    ADMET
    Predicted ADMET features
    Property Value Probability
    Human Intestinal Absorption + 0.9958
    Blood Brain Barrier + 0.9854
    Caco-2 permeable + 0.8868
    P-glycoprotein substrate Substrate 0.7945
    P-glycoprotein inhibitor I Inhibitor 0.8564
    P-glycoprotein inhibitor II Non-inhibitor 0.6353
    Renal organic cation transporter Inhibitor 0.7955
    CYP450 2C9 substrate Non-substrate 0.7684
    CYP450 2D6 substrate Substrate 0.8918
    CYP450 3A4 substrate Non-substrate 0.5117
    CYP450 1A2 substrate Inhibitor 0.9029
    CYP450 2C9 substrate Non-inhibitor 0.9125
    CYP450 2D6 substrate Inhibitor 0.8931
    CYP450 2C19 substrate Non-inhibitor 0.9241
    CYP450 3A4 substrate Inhibitor 0.744
    CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8478
    Ames test Non AMES toxic 0.9132
    Carcinogenicity Non-carcinogens 0.9476
    Biodegradation Not ready biodegradable 0.9686
    Rat acute toxicity 2.8197 LD50, mol/kg Not applicable
    hERG inhibition (predictor I) Weak inhibitor 0.8569
    hERG inhibition (predictor II) Inhibitor 0.8604
    Pharmacoeconomics
    Manufacturers
    • Actavis totowa llc
    • Pliva inc
    • Sandoz inc
    • Usl pharma inc
    • Sanofi-Aventis
    Packagers
    Dosage forms
    FormRouteStrength
    TabletOral10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg
    Prices
    Unit descriptionCostUnit
    Desipramine hcl powder14.4USDg
    Norpramin 150 mg tablet6.08USDtablet
    Desipramine HCl 150 mg tablet4.67USDtablet
    Norpramin 100 mg tablet4.2USDtablet
    Norpramin 75 mg tablet3.19USDtablet
    Desipramine HCl 100 mg tablet2.81USDtablet
    Desipramine HCl 75 mg tablet2.63USDtablet
    Norpramin 50 mg tablet2.51USDtablet
    Desipramine 150 mg tablet2.18USDtablet
    Desipramine HCl 50 mg tablet1.64USDtablet
    Desipramine 100 mg tablet1.5USDtablet
    Norpramin 25 mg tablet1.33USDtablet
    Desipramine 75 mg tablet1.15USDtablet
    Norpramin 10 mg tablet1.11USDtablet
    Apo-Desipramine 75 mg Tablet0.93USDtablet
    Desipramine 50 mg tablet0.92USDtablet
    Desipramine HCl 10 mg tablet0.87USDtablet
    Desipramine HCl 25 mg tablet0.83USDtablet
    Apo-Desipramine 50 mg Tablet0.7USDtablet
    Desipramine 25 mg tablet0.49USDtablet
    Desipramine 10 mg tablet0.4USDtablet
    Apo-Desipramine 10 mg Tablet0.4USDtablet
    Apo-Desipramine 25 mg Tablet0.4USDtablet
    DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
    PatentsNot Available
    Properties
    Statesolid
    Experimental Properties
    PropertyValueSource
    melting point214-218 °CNot Available
    water solubility58.6 mg/L (at 24 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
    logP4.90HANSCH,C ET AL. (1995)
    logS-3.66ADME Research, USCD
    Caco2 permeability-4.67ADME Research, USCD
    pKa10.4SANGSTER (1994)
    Predicted Properties
    PropertyValueSource
    water solubility3.96e-02 g/lALOGPS
    logP4.02ALOGPS
    logP3.9ChemAxon
    logS-3.8ALOGPS
    pKa (strongest basic)10.02ChemAxon
    physiological charge1ChemAxon
    hydrogen acceptor count2ChemAxon
    hydrogen donor count1ChemAxon
    polar surface area15.27ChemAxon
    rotatable bond count4ChemAxon
    refractivity85.31ChemAxon
    polarizability31.74ChemAxon
    number of rings3ChemAxon
    bioavailability1ChemAxon
    rule of fiveYesChemAxon
    Ghose filterYesChemAxon
    Veber's ruleYesChemAxon
    MDDR-like ruleNoChemAxon
    Spectra
    SpectraNot Available
    References
    Synthesis ReferenceNot Available
    General ReferenceNot Available
    External Links
    ResourceLink
    KEGG DrugD07791
    KEGG CompoundC06943
    PubChem Compound2995
    PubChem Substance46504624
    ChemSpider2888
    BindingDB35229
    ChEBI47781
    ChEMBLCHEMBL72
    Therapeutic Targets DatabaseDAP001151
    PharmGKBPA449233
    IUPHAR2399
    Guide to Pharmacology2399
    HETDSM
    Drug Product Database2216272
    RxListhttp://www.rxlist.com/cgi/generic2/desipram.htm
    Drugs.comhttp://www.drugs.com/cdi/desipramine.html
    WikipediaDesipramine
    ATC CodesN06AA01
    AHFS Codes
    • 28:16.04.28
    PDB EntriesNot Available
    FDA labelshow(152 KB)
    MSDSshow(73.6 KB)
    Interactions
    Drug Interactions
    Drug
    AltretamineRisk of severe hypotension
    ArtemetherAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
    AtazanavirAtazanavir may increase the effect and toxicity of the tricyclic antidepressant, desipramine, by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if atazanavir is initiated, discontinued or dose changed.
    AvanafilCo-administration with avanafil resulted in an approximate 5.7% increase in AUC0-inf and 5.2% decrease in Cmax of rosiglitazone.
    ButabarbitalBarbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like desipramine. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
    ButalbitalBarbiturates such as butalbital may increase the metabolism of tricyclic antidepressants such as desipramine. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
    CarbamazepineCarbamazepine may decrease the serum concentration of the tricyclic antidepressant, desipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if carbamazepine is initiated, discontinued or dose changed.
    CimetidineCimetidine may increase the effect of the tricyclic antidepressant, desipramine, by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if cimetidine is initiated, discontinued or dose changed.
    CisaprideIncreased risk of cardiotoxicity and arrhythmias
    ClonidineThe tricyclic antidepressant, desipramine, decreases the effect of clonidine.
    DesvenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
    Dihydroquinidine barbiturateDihydroquinidine barbiturate increases the effect of the tricyclic antidepressant, desipramine.
    DobutamineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of dobutamine.
    DonepezilPossible antagonism of action
    DopamineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of dopamine.
    DuloxetinePossible increase in the levels of this agent when used with duloxetine
    EphedraThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of ephedra.
    EphedrineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of ephedrine.
    EpinephrineTrimipramine may increase the vasopressor effect of the direct-acting alpha-/beta-agonist, Epinephrine. Avoid combination if possible. Monitor sympathetic response to therapy if used concomitantly.
    FenoterolThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of fenoterol.
    FluoxetineThe SSRI, fluoxetine, may increase the serum concentration of the tricyclic antidepressant, desipramine, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of desipramine if fluoxetine is initiated, discontinued or dose changed.
    FluvoxamineThe SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, desipramine, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of desipramine if fluvoxamine is initiated, discontinued or dose changed.
    GalantaminePossible antagonism of action
    GrepafloxacinIncreased risk of cardiotoxicity and arrhythmias
    GuanethidineThe tricyclic antidepressant, desipramine, decreases the effect of guanethidine.
    IndacaterolConcomitant therapy with monoamine oxidase inhibitors, tricyclic antidepressants, or other drugs that prolong the QTc interval should be monitored closely. These drugs may potentiate the effect of adrenergic agonist on the cardiovascular system.
    IsocarboxazidPossibility of severe adverse effects
    IsoprenalineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of isoproterenol.
    MephentermineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of mephentermine.
    MetaraminolThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of metaraminol.
    MethoxamineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of methoxamine.
    Mirabegron Mirabegron is a moderate CYP2D6 inhibitor and may cause an increase in exposure of CYP2D6 substrates. Monitor concomitant therapy closely.
    MoclobemidePossible severe adverse reaction with this combination
    NorepinephrineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of norepinephrine.
    OrciprenalineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of orciprenaline.
    PhenelzinePossibility of severe adverse effects
    PhenylephrineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of phenylephrine.
    PhenylpropanolamineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of phenylpropanolamine.
    PirbuterolThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of pirbuterol.
    ProcaterolThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of procaterol.
    PseudoephedrineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of pseudoephedrine.
    QuinidineAdditive QTc-prolonging effects may occur. Quinidine may also increase the serum concentration of the tricyclic antidepressant, desipramine, by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if quinidine is initiated, discontinued or dose changed. Monitor for the development of torsades de pointes during concomitant therapy.
    Quinidine barbiturateQuinidine barbiturate increases the effect of tricyclic antidepressant, desipramine.
    RasagilinePossibility of severe adverse effects
    RifabutinThe rifamycin, rifabutin, may decrease the effect of the tricyclic antidepressant, desipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if rifabutin is initiated, discontinued or dose changed.
    RifampicinThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, desipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if rifampin is initiated, discontinued or dose changed.
    RitonavirRitonavir may increase the effect and toxicity of the tricyclic antidepressant, desipramine, by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if ritonavir if initiated, discontinued or dose changed.
    RivastigminePossible antagonism of action
    SalbutamolThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of salbutamol.
    SibutramineIncreased risk of CNS adverse effects
    SparfloxacinIncreased risk of cardiotoxicity and arrhythmias
    TacrineThe therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Desipramine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
    TacrolimusAdditive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
    TamoxifenDesipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
    TamsulosinDesipramine, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Desipramine is initiated, discontinued, or dose changed.
    TerbinafineTerbinafine may increase the effect and toxicity of the tricyclic antidepressant, desipramine, by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of desipramine if terbinafine is initiated, discontinued or dose changed.
    TerbutalineThe tricyclic antidepressant, desipramine, increases the sympathomimetic effect of terbutaline.
    TerfenadineIncreased risk of cardiotoxicity and arrhythmias
    ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
    TipranavirTipranavir, co-administered with Ritonavir, may increase the concentration of Desipramine. Monitor Desipramine concentration and efficacy/toxicity and adjust dose as required.
    TolterodineDesipramine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
    ToremifeneAdditive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
    TramadolTramadol increases the risk of serotonin syndrome and seizures. Desipramine may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Desipramine may decrease the effect of Tramadol by decreasing active metabolite production.
    TranylcypromineIncreased risk of serotonin syndrome. Concomitant therapy should be avoided. A significant washout period, dependent on the half-lives of the agents, should be employed between therapies.
    TrazodoneIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
    TrimipramineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. Additive QTc-prolongation may also occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
    TriprolidineTriprolidine and Desipramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
    TrospiumTrospium and Desipramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
    VenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
    VilazodoneMonitor for toxic effects of tricyclic antidepressants if a selective serotonin reuptake inhibitor (SSRI) is initiated or the dose is increased. The influence of the SSRI may take several days or weeks to be fully realized or resolved.
    VoriconazoleAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
    VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
    ZiprasidoneAdditive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
    ZolmitriptanUse of two serotonin modulators, such as zolmitriptan and desipramine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    ZuclopenthixolAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
    Zuclopenthixol acetateAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
    Zuclopenthixol decanoateAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
    Food Interactions
    • Avoid alcohol.
    • Take with food to reduce irritation, limit caffeine intake.

    1. Sodium-dependent noradrenaline transporter

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Sodium-dependent noradrenaline transporter P23975 Details

    References:

    1. Zavosh A, Schaefer J, Ferrel A, Figlewicz DP: Desipramine treatment decreases 3H-nisoxetine binding and norepinephrine transporter mRNA in SK-N-SHSY5Y cells. Brain Res Bull. 1999 Jul 1;49(4):291-5. Pubmed
    2. Weinshenker D, White SS, Javors MA, Palmiter RD, Szot P: Regulation of norepinephrine transporter abundance by catecholamines and desipramine in vivo. Brain Res. 2002 Aug 16;946(2):239-46. Pubmed
    3. Bryan-Lluka LJ, Bonisch H, Lewis RJ: chi-Conopeptide MrIA partially overlaps desipramine and cocaine binding sites on the human norepinephrine transporter. J Biol Chem. 2003 Oct 10;278(41):40324-9. Epub 2003 Jul 1. Pubmed
    4. Zhu MY, Kyle PB, Hume AS, Ordway GA: The persistent membrane retention of desipramine causes lasting inhibition of norepinephrine transporter function. Neurochem Res. 2004 Feb;29(2):419-27. Pubmed
    5. Ordway GA, Jia W, Li J, Zhu MY, Mandela P, Pan J: Norepinephrine transporter function and desipramine: residual drug effects versus short-term regulation. J Neurosci Methods. 2005 Apr 30;143(2):217-25. Epub 2004 Dec 30. Pubmed
    6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
    7. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. Pubmed

    2. Sodium-dependent serotonin transporter

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Sodium-dependent serotonin transporter P31645 Details

    References:

    1. Holmes A, Yang RJ, Murphy DL, Crawley JN: Evaluation of antidepressant-related behavioral responses in mice lacking the serotonin transporter. Neuropsychopharmacology. 2002 Dec;27(6):914-23. Pubmed
    2. Gould GG, Altamirano AV, Javors MA, Frazer A: A comparison of the chronic treatment effects of venlafaxine and other antidepressants on serotonin and norepinephrine transporters. Biol Psychiatry. 2006 Mar 1;59(5):408-14. Epub 2005 Sep 2. Pubmed
    3. Zhou L, Huang KX, Kecojevic A, Welsh AM, Koliatsos VE: Evidence that serotonin reuptake modulators increase the density of serotonin innervation in the forebrain. J Neurochem. 2006 Jan;96(2):396-406. Epub 2005 Nov 21. Pubmed
    4. Hoffman AF, Gerhardt GA: 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. 1998 Jan;70(1):179-89. Pubmed
    5. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. Pubmed

    3. 5-hydroxytryptamine receptor 2A

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: antagonist

    Components

    Name UniProt ID Details
    5-hydroxytryptamine receptor 2A P28223 Details

    References:

    1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed

    4. Beta-2 adrenergic receptor

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: antagonist

    Components

    Name UniProt ID Details
    Beta-2 adrenergic receptor P07550 Details

    References:

    1. Matsumoto K, Ojima K, Ohta H, Watanabe H: Beta 2- but not beta 1-adrenoceptors are involved in desipramine enhancement of aggressive behavior in long-term isolated mice. Pharmacol Biochem Behav. 1994 Sep;49(1):13-8. Pubmed
    2. Sapena R, Morin D, Zini R, Morin C, Tillement JP: Desipramine treatment differently down-regulates beta-adrenoceptors of freshly isolated neurons and astrocytes. Eur J Pharmacol. 1996 Apr 4;300(1-2):159-62. Pubmed
    3. Abadie C, Foucart S, Page P, Nadeau R: Modulation of noradrenaline release from isolated human atrial appendages. J Auton Nerv Syst. 1996 Dec 14;61(3):269-76. Pubmed
    4. Prenner L, Sieben A, Zeller K, Weiser D, Haberlein H: Reduction of high-affinity beta2-adrenergic receptor binding by hyperforin and hyperoside on rat C6 glioblastoma cells measured by fluorescence correlation spectroscopy. Biochemistry. 2007 May 1;46(17):5106-13. Epub 2007 Apr 7. Pubmed
    5. Osadchii OE, Woodiwiss AJ, Deftereos D, Norton GR: Temporal changes in myocardial adrenergic regulation with the progression to pump dysfunction after chronic beta-adrenoreceptor activation in rats. Pflugers Arch. 2007 Nov;455(2):251-60. Epub 2007 Jun 9. Pubmed

    5. Beta-1 adrenergic receptor

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: other

    Components

    Name UniProt ID Details
    Beta-1 adrenergic receptor P08588 Details

    References:

    1. Sapena R, Morin D, Zini R, Morin C, Tillement JP: Desipramine treatment differently down-regulates beta-adrenoceptors of freshly isolated neurons and astrocytes. Eur J Pharmacol. 1996 Apr 4;300(1-2):159-62. Pubmed
    2. Burgi S, Baltensperger K, Honegger UE: Antidepressant-induced switch of beta 1-adrenoceptor trafficking as a mechanism for drug action. J Biol Chem. 2003 Jan 10;278(2):1044-52. Epub 2002 Oct 21. Pubmed
    3. Matsumoto K, Ojima K, Ohta H, Watanabe H: Beta 2- but not beta 1-adrenoceptors are involved in desipramine enhancement of aggressive behavior in long-term isolated mice. Pharmacol Biochem Behav. 1994 Sep;49(1):13-8. Pubmed
    4. Samnick S, Scheuer C, Munks S, El-Gibaly AM, Menger MD, Kirsch CM: Technetium-99m labeled 1-(4-fluorobenzyl)-4-(2-mercapto-2-methyl-4-azapentyl)-4-(2-mercapto-2-met hylpropylamino)-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. 2004 May;31(4):511-22. Pubmed
    5. Mudunkotuwa NT, Horton RW: 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. 1996 Apr;117(7):1481-6. Pubmed

    6. Sphingomyelin phosphodiesterase

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Sphingomyelin phosphodiesterase P17405 Details

    References:

    1. Testai FD, Landek MA, Dawson G: Regulation of sphingomyelinases in cells of the oligodendrocyte lineage. J Neurosci Res. 2004 Jan 1;75(1):66-74. Pubmed
    2. Kolzer M, Werth N, Sandhoff K: Interactions of acid sphingomyelinase and lipid bilayers in the presence of the tricyclic antidepressant desipramine. FEBS Lett. 2004 Feb 13;559(1-3):96-8. Pubmed
    3. Erdreich-Epstein A, Tran LB, Cox OT, Huang EY, Laug WE, Shimada H, Millard M: Endothelial apoptosis induced by inhibition of integrins alphavbeta3 and alphavbeta5 involves ceramide metabolic pathways. Blood. 2005 Jun 1;105(11):4353-61. Epub 2005 Feb 10. Pubmed
    4. Zeidan YH, Pettus BJ, Elojeimy S, Taha T, Obeid LM, Kawamori T, Norris JS, Hannun YA: Acid ceramidase but not acid sphingomyelinase is required for tumor necrosis factor-{alpha}-induced PGE2 production. J Biol Chem. 2006 Aug 25;281(34):24695-703. Epub 2006 Jun 27. Pubmed
    5. Hurwitz R, Ferlinz K, Sandhoff K: The tricyclic antidepressant desipramine causes proteolytic degradation of lysosomal sphingomyelinase in human fibroblasts. Biol Chem Hoppe Seyler. 1994 Jul;375(7):447-50. Pubmed
    6. Kornhuber J, Tripal P, Reichel M, Muhle C, Rhein C, Muehlbacher M, Groemer TW, Gulbins E: Functional Inhibitors of Acid Sphingomyelinase (FIASMAs): a novel pharmacological group of drugs with broad clinical applications. Cell Physiol Biochem. 2010;26(1):9-20. Epub 2010 May 18. Pubmed

    7. Histamine H1 receptor

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Actions: antagonist

    Components

    Name UniProt ID Details
    Histamine H1 receptor P35367 Details

    References:

    1. Sawynok J, Esser MJ, Reid AR: Peripheral antinociceptive actions of desipramine and fluoxetine in an inflammatory and neuropathic pain test in the rat. Pain. 1999 Aug;82(2):149-58. Pubmed
    2. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed

    8. Alpha-1A adrenergic receptor

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Actions: antagonist

    Components

    Name UniProt ID Details
    Alpha-1A adrenergic receptor P35348 Details

    References:

    1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed

    9. Muscarinic acetylcholine receptor M1

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Actions: antagonist

    Components

    Name UniProt ID Details
    Muscarinic acetylcholine receptor M1 P11229 Details

    References:

    1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed
    2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
    3. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

    10. Muscarinic acetylcholine receptor M2

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Actions: antagonist

    Components

    Name UniProt ID Details
    Muscarinic acetylcholine receptor M2 P08172 Details

    References:

    1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed
    2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
    3. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

    11. Muscarinic acetylcholine receptor M3

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Actions: antagonist

    Components

    Name UniProt ID Details
    Muscarinic acetylcholine receptor M3 P20309 Details

    References:

    1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed

    12. Muscarinic acetylcholine receptor M4

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Actions: antagonist

    Components

    Name UniProt ID Details
    Muscarinic acetylcholine receptor M4 P08173 Details

    References:

    1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed

    13. Muscarinic acetylcholine receptor M5

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Actions: antagonist

    Components

    Name UniProt ID Details
    Muscarinic acetylcholine receptor M5 P08912 Details

    References:

    1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed

    14. Transporter

    Kind: protein

    Organism: Aquifex aeolicus (strain VF5)

    Pharmacological action: unknown

    Components

    Name UniProt ID Details
    Transporter O67854 Details

    References:

    1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed

    1. Cytochrome P450 2D6

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate inhibitor

    Components

    Name UniProt ID Details
    Cytochrome P450 2D6 P10635 Details

    References:

    1. Baumann P: Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet. 1996 Dec;31(6):444-69. Pubmed
    2. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
    3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
    4. Lewis DF, Modi S, Dickins M: Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82. Pubmed

    2. Cytochrome P450 2C19

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate inhibitor

    Components

    Name UniProt ID Details
    Cytochrome P450 2C19 P33261 Details

    References:

    1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    3. Cytochrome P450 2C18

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Cytochrome P450 2C18 P33260 Details

    References:

    1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    4. Cytochrome P450 1A2

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Cytochrome P450 1A2 P05177 Details

    References:

    1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    5. Cytochrome P450 3A4

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Cytochrome P450 3A4 P08684 Details

    References:

    1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    6. Cytochrome P450 2A6

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Cytochrome P450 2A6 P11509 Details

    References:

    1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    7. Cytochrome P450 2B6

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Cytochrome P450 2B6 P20813 Details

    References:

    1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    8. Cytochrome P450 2E1

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Cytochrome P450 2E1 P05181 Details

    References:

    1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    1. Alpha-1-acid glycoprotein 1

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Components

    Name UniProt ID Details
    Alpha-1-acid glycoprotein 1 P02763 Details

    References:

    1. Ferry DG, Caplan NB, Cubeddu LX: Interaction between antidepressants and alpha 1-adrenergic receptor antagonists on the binding to alpha 1-acid glycoprotein. J Pharm Sci. 1986 Feb;75(2):146-9. Pubmed

    1. Multidrug resistance protein 1

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Multidrug resistance protein 1 P08183 Details

    References:

    1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. Pubmed
    2. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. Pubmed

    2. Solute carrier family 22 member 1

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Solute carrier family 22 member 1 O15245 Details

    References:

    1. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. Pubmed
    2. Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, Koepsell H: Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. Am J Physiol Renal Physiol. 2001 Sep;281(3):F454-68. Pubmed
    3. Grundemann D, Gorboulev V, Gambaryan S, Veyhl M, Koepsell H: Drug excretion mediated by a new prototype of polyspecific transporter. Nature. 1994 Dec 8;372(6506):549-52. Pubmed

    3. Solute carrier family 22 member 2

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Solute carrier family 22 member 2 O15244 Details

    References:

    1. Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE, Koepsell H: Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol. 1997 Jul;16(7):871-81. Pubmed
    2. Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, Koepsell H: Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. Am J Physiol Renal Physiol. 2001 Sep;281(3):F454-68. Pubmed

    4. Solute carrier family 22 member 3

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Solute carrier family 22 member 3 O75751 Details

    References:

    1. Wu X, Huang W, Ganapathy ME, Wang H, Kekuda R, Conway SJ, Leibach FH, Ganapathy V: Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney. Am J Physiol Renal Physiol. 2000 Sep;279(3):F449-58. Pubmed
    2. Kekuda R, Prasad PD, Wu X, Wang H, Fei YJ, Leibach FH, Ganapathy V: Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta. J Biol Chem. 1998 Jun 26;273(26):15971-9. Pubmed
    3. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. Pubmed

    5. Solute carrier family 22 member 5

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Solute carrier family 22 member 5 O76082 Details

    References:

    1. Wu X, Huang W, Prasad PD, Seth P, Rajan DP, Leibach FH, Chen J, Conway SJ, Ganapathy V: Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter. J Pharmacol Exp Ther. 1999 Sep;290(3):1482-92. Pubmed

    6. Solute carrier family 22 member 4

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Solute carrier family 22 member 4 Q9H015 Details

    References:

    1. Wu X, George RL, Huang W, Wang H, Conway SJ, Leibach FH, Ganapathy V: Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta. Biochim Biophys Acta. 2000 Jun 1;1466(1-2):315-27. Pubmed

    Comments
    Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:13