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Drug

D0849 | cilnidipine

Molecular Formula C27H28N2O7
Molecular Weight 492.5
Structure
State solid
Volume of distribution Drugs on the group of dihydropyridines such as cilnidipine tend to have a large volume of distribution.[T119]
Route of elimination Cilnidipine gets eliminated through the urine in a proportion of 20% of the administered dose and 80% is eliminated by the feces.[L1440]
Protein binding Cilnidipine presents a very high protein binding that represents to even 98% of the administered dose.[L1444]
Half life The half-life of the hypotensive effect for cilnidipine is of about 20.4 min.[A32004]
Absorption Cilnidipine presents a very rapid absorption with a maximum peaked concentration after 2 hours. Its distribution tends to be higher in the liver as well as in kidneys, plasma and other tissues. Cilnidipine does not present a high accumulation in the tissue after repeated oral administration.[L1444] Cilnidipine is reported to present very low bioavailability determined to be approximately 13%. This low bioavailability is suggested to be due to its low aqueous solubility and high permeability. Hence, efforts have been made in order to find an innovative formulation that can significantly improve the bioavailability of this drug. One of these formulations corresponds to the generation of polymeric nanoparticles which enhance the bioavailability by 2.5-3-fold.[L6124]

C

C08CA14 Cilnidipine


[C08CA] Dihydropyridine derivatives


[C08C] SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS


[C08] CALCIUM CHANNEL BLOCKERS


[C] Cardiovascular system

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 12.53±1.78 human qHTS-HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 12.27 human HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 14.79±8.07 rat hepatocytes MMP assay decrease IC50 163

Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 39 companies from 2 notifications to the ECHA C&L Inventory.


H318 (97.44%): Causes serious eye damage [Danger Serious eye damage/eye irritation]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


 P280, P305+P351+P338, and P310; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Organism Test type Route Dose (normalized dose) Effect Source
mouse LD50 subcutaneous > 5gm/kg (5000mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 20(Suppl,
rat LD50 subcutaneous > 5gm/kg (5000mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 20(Suppl,
mouse LD50 intraperitoneal 1845mg/kg (1845mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 20(Suppl,
rat LD50 oral 4412mg/kg (4412mg/kg) skin and appendages (skin): hair: other Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 20(Suppl,
dog LD50 oral > 2gm/kg (2000mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 20(Suppl,
rat LD50 intraperitoneal 426mg/kg (426mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 20(Suppl,
mouse LD50 oral > 5gm/kg (5000mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 20(Suppl,


  • (+-)-(E)-Cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methoxyethyl (2E)-3-phenyl-2-propenyl ester 132203-70-4
    2-Methoxyethyl (2E)-3-Phenyl-2-propenyl 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate 2-methoxyethyl (2E)-3-phenylprop-2-en-1-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 2-methoxyethyl-3-phenyl-2-propen-1-yl-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylate
    203C704 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 2-methoxyethyl 3-phenyl-2-propenyl ester, (E)-(+-)- 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 3-(2-methoxyethyl) 5-[(2E)-3-phenyl-2-propen-1-yl] ester
    3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-,2-methoxyethyl 3-phenyl-2-propenyl ester, (E)-(+-)- 3-cinnamyl 5-(2-methoxyethyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate AB0004990
    AB01274755-01 AB01274755-02 AB01274755_03
    AB2000034 AC-270 AKOS005558085
    Atelec Atelec (TN) BCP22689
    BDBM50101813 BRD-A07875874-001-01-6 C27H28N2O7
    CAS-132203-70-4 CCG-221188 CCG-221726
    CHEBI:31399 CHEBI:91506 CHEMBL452076
    CS-1133 Cilnidipine (JP17/INN) Cilnidipine [INN]
    Cilnidipine, 99% Cilnidipine, >=98% (HPLC), powder Cinaldipine
    Cinalong D01173 DB09232
    DSSTox_CID_26309 DSSTox_GSID_46309 DSSTox_RID_81530
    DTXSID0046309 EBD38396 F2173-0669
    FRC 8653 FRC 8653 FRC 8653, 132203-70-4
    FRC-8653 FRC-8653 FRC8653
    GTPL7767 H738 HMS2089J07
    HMS3261E06 HMS3413L13 HMS3677L13
    HMS3715N17 HY-17404 J-006141
    K-4145 KS-1294 LP00422
    LS-131293 MFCD00865853 NCGC00162150-01
    NCGC00162150-02 NCGC00162150-03 NCGC00162150-04
    NCGC00261107-01 O3-(2-methoxyethyl) O5-(3-phenylprop-2-enyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate; Q731525
    RT-012023 SC-25763 SCHEMBL25550
    SR-05000001454 SR-05000001454-1 SR-05000001454-2
    ST24042102 STK623341 SW219784-1
    Siscard Tox21_112001 Tox21_112001_1
    Tox21_500422 cilnidipine s1293

    DrugBank Name cilnidipine
    DrugBank DB09232
    CAS Number 132203-70-4, 80621-81-4
    PubChem Compound 5282138
    KEGG Drug D01173
    ChEBI 31399