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Drug

D0492 | darifenacin

Molecular Formula C28H30N2O2
Molecular Weight 426.5
Structure
State solid
Clearance * 40 L/h [extensive metabolizers] * 32 L/h [poor metabolizers]
Volume of distribution * 163 L
Protein binding Darifenacin is approximately 98% bound to plasma proteins (primarily to alpha-1-acid-glycoprotein).
Half life The elimination half-life of darifenacin following chronic dosing is approximately 13-19 hours.
Absorption The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.

G

G04BD10 Darifenacin


[G04BD] Drugs for urinary frequency and incontinence


[G04B] UROLOGICALS


[G04] UROLOGICALS


[G] Genitourinary system and reproductive hormones

Toxicity Dose Time Species Model Method Action Positive criterion Reference
UNCOUPLING rat isolated liver mitochondria measurements of mitochondrial respiration; RST inhibition assay, RST uncoupling assay; IC 50ratio of glucose/galactose assay increase 53
ELECTRON TRANSPORT CHAIN rat isolated liver mitochondria measurements of mitochondrial respiration; RST inhibition assay, RST uncoupling assay; IC 50ratio of glucose/galactose assay decrease 53


  • (S)-1-(2-(2,3-Dihydro-5-benzofuranyl)ethyl)-alpha,alpha-diphenyl-3-pyrrolidineacetamide (S)-2-(1-(2-(2,3-dihydrobenzofuran-5-yl)ethyl)pyrrolidin-3-yl)-2,2-diphenylacetamide (S)-2-{1-[2-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-pyrrolidin-3-yl}-2,2-diphenyl-acetamide
    (S)-2-{1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide (s)-1-[2-(2,3-dihydro-5-benzofuranyl) ethyl]-alpha,alpha-diphenyl-3-pyrrolidine acetamide 099D044
    133099-04-4 2-((3S)-1-(2-(2,3-Dihydrobenzofuran-5-yl)ethyl)pyrrolidin-3-yl)-2,2-diphenylacetamide 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-di(phenyl)acetamide
    2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide 2-{(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl}-2,2-diphenylacetamide 2-{1-[2-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-pyrrolidin-3-yl}-2,2-diphenyl-acetamide (Darifenacin)
    3-(S)-(-)-(1-carbamoyl-1,1-diphenylmethyl)-1-[2-(2,3-dihydrobenzofuran-5-y l)ethyl]pyrrolidine; 3-(S)-(-)-(1-carbamoyl-1,1-diphenylmethyl)-1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]pyrrolidine 3-Pyrrolidineacetamide, 1-(2-(2,3-dihydro-5-benzofuranyl)ethyl)-alpha,alpha-diphenyl-, (3S)-
    AB01566824_01 AC-302 AKOS015907962
    APG9819VLM API0002219 BDBM50109647
    CHEBI:391960 CHEMBL1346 CS-1168
    D03654 DB00496 DTXSID2048290
    Darifenacin Darifenacin (USAN/INN) Darifenacin [USAN:INN:BAN]
    Emselex Enablex FT-0652801
    GTPL319 GTPL321 HXGBXQDTNZMWGS-RUZDIDTESA-N
    HY-A0033 LS-187359 MCULE-4616748439
    MLS003876823 NCGC00168775-01 Q166476
    SB17425 SCHEMBL56574 SMR002533186
    ST24039043 UK-88525 UNII-APG9819VLM
    W-5196 ZINC1996117 [3H]darifenacin

    DrugBank Name darifenacin
    DrugBank DB00496
    CAS Number 133099-04-4, 133099-07-7
    PubChem Compound 444031
    KEGG Drug D03654
    ChEBI 391960
    PharmGKB PA164774901