Cilnidipine

Cilnidipine Basic information
Description References
Product Name:Cilnidipine
Synonyms:(+/-)-(e)-cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate;O3-(2-Methoxyethyl) O5-[(E)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid 3-(2-methoxyethyl)5-[(E)-3-phenyl-2-propenyl] ester;2,6-Dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid 3-(2-methoxyethyl)5-[(E)-3-phenyl-2-propenyl] ester;Frc 8653,1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methoxyethyl (2E)-3-phenyl-2-propenyl ester;1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic Acid 2-Methoxyethyl (2E)-3-Phenyl-2-propenyl Ester 2-Methoxyethyl (2E)-3-Phenyl-2-propenyl 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate;ilnidipine;3-CinnaMyl 5-(2-Methoxyethyl) 2,6-diMethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
CAS:132203-70-4
MF:C27H28N2O7
MW:492.52
EINECS:634-350-6
Product Categories:Dihydropyridine Class Chemicals;Intermediates & Fine Chemicals;Pharmaceuticals;Calcium channel;API;FRC 8653;Dihydropyridine;APIs;Active Pharmaceutical Ingredients;132203-70-4
Mol File:132203-70-4.mol
Cilnidipine Structure
Cilnidipine Chemical Properties
Melting point 97-99°C
Boiling point 652.6±55.0 °C(Predicted)
density 1.240±0.06 g/cm3(Predicted)
storage temp. Keep in dark place,Sealed in dry,Room Temperature
solubility H2O: ≤2mg/mL
pka2.61±0.70(Predicted)
form powder
color light yellow
Merck 14,2275
InChIKeyKJEBULYHNRNJTE-DHZHZOJOSA-N
CAS DataBase Reference132203-70-4(CAS DataBase Reference)
Safety Information
Hazard Codes Xi
Risk Statements 41
Safety Statements 26-39
WGK Germany 3
RTECS US7975550
HS Code 29333990
ToxicityLD50 in male, female mice, rats (mg/kg): 5000, 5000, 5000, 4412 orally; 5000 all species s.c.; 1845, 2353, 441, 426 i.p. (Wada)
MSDS Information
ProviderLanguage
Cilnidipine English
Cilnidipine Usage And Synthesis
DescriptionClinidipine is a kind of calcium channel blocker. It is a kind of novel calcium antagonist with the blocking effect on both L-type and N-type calcium channels. It is mainly used for the treatment of hypertension. Based on its effect on both N-type and L-type calcium channel, it can dilate both arterioles and venules, further reducing the pressure in the capillary bed. In addition, cilinidipine can attenuate the platelet activation associated with catecholamines.
Referenceshttps://www.drugbank.ca/drugs/DB09232
https://en.wikipedia.org/wiki/Cilnidipine
DescriptionCilnidipine is a dihydropyridine calcium antagonist introduced for the treatment of essential and severe hypertension and hypertension associated with renopathy. Cilnidipine has been demonstrated to exert a potent vasodilating effect by blocking calcium influx via dihydropyridine-sensitive, voltage-dependent calcium channels. Compared to nifedipine and nicardipine, cilnidipine is superior, especially for long-term treatment, due to its characteristics of slow onset and long duration with less cardiodepressant activity. Cilnidipine is reportedly well tolerated with low toxicity. It may also be useful in ischemic heart disease.
DescriptionCilnidipine is a dihydropyridine calcium channel blocker that blocks L- and N-type high-voltage-activated calcium currents in rat hippocampal CA1 pyramidal neurons when used at a concentration of 10 μM. Cilnidipine (3 mg/kg) reduces the pressor response to acute cold stress, as well as mean blood pressure, in spontaneously hypertensive rats. It dose-dependently reduces mean blood pressure and cerebral vascular resistance without affecting cerebral blood flow in anesthetized rats at doses ranging from 3-100 μg/kg. Cilnidipine (100 μg/kg, i.p.) reduces cerebral infarction area in a rat model of focal brain ischemia.
Chemical PropertiesYellow Crystalline Solid
OriginatorFujirebio (Japan)
UsesCilnidipine has been used:
  • in cell viability assay of pheochromocytoma (nPC12) cells
  • in photoirradiation and photodegradation studies
  • to understand effect on albuminuria in diabetic nephropathy
UsesA dihydropyridine calcium channel blocker.
Usesantihypertensive;dihydropyridine calcium channel blocker
DefinitionChEBI: A diesterified 1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium channel blocker, it is used as an antihypertensive.
Brand nameCinalong;Siscard;Atelec
Biological ActivityDual L- and N-type calcium channel blocker that displays antihypertensive, sympatholytic and neuroprotective activity. Lowers mean blood pressure and reduces the size of cerebral infarction in the rat model of focal brain ischemia.
Biochem/physiol ActionsCilnidipine is a slow-acting Ca2+ channel blocker; antihypertensive; vasodilator; dual blocker of L-type voltage-gated Ca2+ channels in vascular smooth muscle and N-type Ca2+ channels in sympathetic nerve terminals that supply blood vessels. Cilnidipine may offer an advantage over nifedipine as the long term intake of the latter has been linked to increased risk of myocardial infarction and mortality in patients with coronary artery disease. Cilnidipine lowers blood pressure, but has less effect on sympathetic activity. Unlike nifedipine, cilnidipine does not inhibit PKC.
storage+4°C
Cilnidipine Preparation Products And Raw materials
Raw materialsMethyl 3-aminocrotonate-->2-Methoxyethyl 2-[(3-nitrophenyl)methylene]acetoacetate
TRIETHYL ACONITATE Cilnidipine Impurity 2 1-Propene-1,2,3-tricarboxylicacid, triethyl ester, (E)- (9CI) Cilnidipine Impurity 4 Cilnidipine Impurity 3 NIMODIPINE RELATED COMPOUND B (50 MG) (BIS(2-METHOXYETHYL) 2,6-DIMETHYL-4-(3-NITROPHE-NYL)-1,4-DIHYDROPYRIDINE-3,5-DICARBOXYLATE) (AS) Cilnidipine Impurity 1 Sitagliptin EP Impurity C FEMA 2296 Dacthal FEMA 2302 Diethyl2,6-dimethyl-4-phenyl-1,4-dihydropyridine-3,5-dicarboxylate M-NIFEDIPINE Cinnamyl alcohol 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic Acid 3-Methyl Ester cinnamyl valerate CINNAMYL METHACRYLATE Cinnamyl propionate

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