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Drug

D0089 | Nefazodone

Molecular Formula C25H32ClN5O2
Molecular Weight 470
Structure
State solid
Volume of distribution * 0.22 to 0.87 L/kg
Route of elimination Nefazodone is extensively metabolized after oral administration by n-dealkylation and aliphatic and aromatic hydroxylation, and less than 1% of administered nefazodone is excreted unchanged in urine.
Protein binding Greater than 99% (in vitro, human plasma proteins).
Half life 2-4 hours
Absorption Nefazodone is rapidly and completely absorbed. Its absolute bioavailability is low (about 20%).
Trade names Serzone
Description antidepressant

N

N06AX06 Nefazodone


[N06AX] Other antidepressants


[N06A] ANTIDEPRESSANTS


[N06] PSYCHOANALEPTICS


[N] Nervous system

Toxicity Dose Time Species Model Method Action Positive criterion Reference
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex I activity decrease p < 0.001 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex II + III activity decrease p < 0.01 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex II + III activity decrease p < 0.01 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex IV activity decrease p < 0.001 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex V activity decrease p < 0.001 3
ELECTRON TRANSPORT CHAIN decrease 35
ELECTRON TRANSPORT CHAIN inhibit 197
GLUCOSE GALACTOSE IC50 RATIO 10 LUHMES (Lund human mesencephalic) cells Glc–Gal–NeuriTox assay EC25(NA) [Glc/Gal] 326

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase 50 μM bovine heart mitochondria Measurement of complex I activity inhibitor p < 0.001 3
NADH:ubiquinone reductase inhibitor 35
Succinate dehydrogenase 50 μM bovine heart mitochondria Measurement of complex II + III activity inhibitor p < 0.01 3
Quinol--cytochrome-c reductase 50 μM bovine heart mitochondria Measurement of complex II + III activity inhibitor p < 0.01 3
Cytochrome c oxidase 50 μM bovine heart mitochondria Measurement of complex IV activity inhibitor p < 0.001 3
ATP synthase 50 μM bovine heart mitochondria Measurement of complex V activity inhibitor p < 0.001 3

  • Agitation

  • Asthenia

  • Bradyphrenia

  • Decreased interest

  • Depressed mood

  • Depression

  • Disturbance in attention

  • Drug abuse

  • Dysphoria

  • Fatigue

  • Feeling guilty

  • Hypersomnia

  • Insomnia

  • Mental disability

  • Suicidal ideation

  • Suicide attempt

  • Agitation (0.012)

  • Nausea (0.035)

    • 1-(3-(4-(3-Chlorophenyl)piperazin-1-yl)propyl)-3-ethyl-4-(2-phenoxyethyl)-1H-1,2,4-triazol-5(4H)-one 1-(3-(4-(3-Chlorpheyl-1-piperazinylpropyl)-3-ethyl-4,5-dihydro-4-(2-phenoxyethyl)-1,2,4-triazol-5-on 1-(3-(4-(m-Chlorophenyl)-1-piperazinyl)propyl)-3-ethyl-4-(2-phenoxyethyl)-delta2-1,2,4-triazolin-5-one
    1-{3-[4-(3-chlorophenyl)piperazin-1-yl]propyl}-3-ethyl-4-(2-phenoxyethyl)-4,5-dihydro-1H-1,2,4-triazol-5-one 117201-EP2275420A1 117201-EP2298764A1
    117201-EP2298765A1 117201-EP2298776A1 2-(3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl)-5-ethyl-4-(2-phenoxyethyl)-2,4-dihydro-3H-1,2,4-triazol-3-one #
    2-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxyethyl)-1,2,4-triazol-3-one 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxyethyl)-2H-1,2,4-triazol-3(4H)-one
    2-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-ethyl-4-(2-phenoxyethyl)-1,2,4-triazol-3-one 2-{3-[4-(3-chlorophenyl)piperazin-1-yl]propyl}-5-ethyl-4-(2-phenoxyethyl)-2,4-dihydro-3H-1,2,4-triazol-3-one 2-{3-[4-(3-chlorophenyl)piperazin-1-yl]propyl}-5-ethyl-4-[2-(phenyloxy)ethyl]-2,4-dihydro-3H-1,2,4-triazol-3-one
    366N669 3H-1,2,4-Triazol-3-one, 2,4-dihydro-2-3-(4-(3-chlorophenyl)-1-piperazinyl)propyl)-5-ethyl-4-(2-phenoxyethyl)- 3H-1,2,4-Triazol-3-one, 2-(3-(4-(3-chlorophenyl)-1-piperazinyl)propyl)-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-
    59H4FCV1TF 83366-66-9 A840565
    AB00640019-14 AB00640019_15 AKOS015907198
    API0003523 AX8022765 BCP30990
    BDBM50069447 BIDD:GT0789 BRD-K90789829-003-03-3
    C07256 C25H32ClN5O2 CCG-213026
    CHEBI:7494 CHEMBL623 D08257
    DB01149 DTXSID2023357 Dutonin pound>> Nefadar pound>> Serzone
    FT-0654783 GTPL7247 HMS2090D17
    HMS2231I17 HMS3264K04 HMS3372C02
    L001196 LS-156497 MLS001165769
    MLS001195657 NCGC00165846-01 NCGC00165846-02
    NCGC00165846-03 NSC-760344 NSC760344
    Nefadar Nefazodona Nefazodona [Spanish]
    Nefazodone (INN) Nefazodone [INN:BAN] Nefazodonum
    Nefazodonum [Latin] Pharmakon1600-01502314 Q416632
    SCHEMBL35089 SMR000550487 SR-01000759312
    SR-01000759312-5 UNII-59H4FCV1TF VA11366
    VRBKIVRKKCLPHA-UHFFFAOYSA-N ZINC538065 nefazodone

    DrugBank Name Nefazodone
    DrugBank DB01149
    CAS Number 82752-99-6, 83366-66-9
    PubChem Compound 4449
    KEGG Compound ID C07256
    KEGG Drug D08257
    PubChem.Substance 46508323
    ChEBI 7494
    PharmGKB PA450603
    ChemSpider 4294
    BindingDB 50069447.0
    TTD DAP000042
    Wikipedia Nefazodone
    DPD 449

    1. Dykens et al. (2007)
    2. Vuda et al. (2016)