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Drug

D0782 | aranidipine

Molecular Formula C19H20N2O7
Molecular Weight 388.4
Structure
State solid
Route of elimination Unchanged aranidipine is found in plasma but not in the urine after 1 hour of administration. Just a small amount of drug was found in the bile. These results indicate that the excretion profile of aranidipine is mainly driven by metabolism and not by excretion. When including the metabolites, 52-56% of the original dose is disposed in the urine, 34-45% in feces and 3-4% in expired air. The excretion in the bile was 59% of the administered dose and 63% of this portion is reabsorbed.[L1343]
Protein binding The binding ratio of plasma proteins of aranidipine varies from 84-95%. This ratio of the drug is similar to the unchanged form and for the M-1 metabolite. Most of the binding happens towards serum albumin and a lower amount corresponds to the alpha1-acid glycoprotein.[L1343]
Half life The elimination half-life of aranidipine and the M-1 metabolite are 1.1-1.2 hour and 2.7-3.5 hour respectively.[L1343]
Absorption After administration, aranidipine is rapidly absorbed from the gastrointestinal tract. After absorption, the AUC and Cmax increased linearly in a dose-dependent manner, the Cmax was attained in approximate 3.8-4.8 hours for aranidipine and 4.8-6 hours for the metabolite M-1. The bioavailability of aranidipine in rat, dog, and monkey was about 48%, 41% and 3% respectively.[L1343]

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 12.83±3.68 human qHTS-HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL human HepG2 MMP assay Negative IC50 163
MEMBRANE POTENTIAL rat hepatocytes MMP assay Negative IC50 163


  • (+-)-Acetonyl methyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-pyridinedicarboxylate 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, methyl 2-oxopropyl ester 3-METHYL 5-(2-OXOPROPYL) 2,6-DIMETHYL-4-(2-NITROPHENYL)-1,4-DIHYDROPYRIDINE-3,5-DICARBOXYLATE
    3-O-methyl 5-O-(2-oxopropyl) 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 780A907 86780-90-7
    AC-907 AKOS015967075 Aranidipine (JAN/INN)
    Aranidipine [INN] CAS-86780-90-7 CCRIS 6724
    CHEBI:31232 CHEMBL2104030 CS-7341
    D01562 DB-090281 DB09229
    DSSTox_CID_28575 DSSTox_GSID_48649 DSSTox_RID_82847
    DTXSID9048649 FT-0705721 HY-U00212
    K547 LS-131299 MPC 1304
    Mpc-1304 NCGC00182054-02 NCGC00182054-03
    Q4784109; SCHEMBL49910 Sapresta
    Sapresta (TN) Tox21_113003 Tox21_113003_1
    ZINC000000600803 aranidipine methyl 2-oxopropyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid

    DrugBank Name aranidipine
    DrugBank DB09229
    CAS Number 86780-90-7, 93017-04-0
    PubChem Compound 2225
    KEGG Drug D01562
    ChEBI 31232