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Benidipine

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CAS: 105979-17-7
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CAS:105979-17-7
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Benidipine manufacturers

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  • Benidipine
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  • 2021-07-13
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  • Benidipine
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  • 2021-07-10
  • CAS:105979-17-7
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Benidipine Basic information
Product Name:Benidipine
Synonyms:(R*,R*)-(±)-(3,5-Pyridinedicarboxylic acid 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-methyl 1- (phenylmethyl)-3-piperidinyl ester monohydrochloride;3,5-Pyridinedicarboxylicacid, 1,4-dihydro-2,6-diMethyl-4-(3-nitrophenyl)-, 3-Methyl5-[(3R)-1-(phenylMethyl)-3-piperidinyl] ester, (4R)-rel-;NACADIPINE;BENIDIPINE;BENIDIPINE HCL;CAPADIPINE;CONIEL;KW-3049
CAS:105979-17-7
MF:C28H31N3O6
MW:505.56
EINECS:857-680-4
Product Categories:Aromatics;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Pharmaceutical
Mol File:105979-17-7.mol
Benidipine Structure
Benidipine Chemical Properties
Boiling point 625.2±55.0 °C(Predicted)
density 1.29±0.1 g/cm3(Predicted)
pkapKa 7.34(H2O(long extrapolation) ) (Uncertain)
Water Solubility 316μg/L at 25℃
InChIKeyQZVNQOLPLYWLHQ-GRHWAJSLNA-N
SMILES[C@H]1(C(C(=O)OC)=C(NC(C)=C1C(=O)O[C@@H]1CCCN(CC2=CC=CC=C2)C1)C)C1=CC=CC([N+]([O-])=O)=C1 |&1:0,14,r|
LogP4.61
CAS DataBase Reference105979-17-7(CAS DataBase Reference)
Safety Information
MSDS Information
Benidipine Usage And Synthesis
UsesBenidipine (CAS# 105979-17-7) is a 1,4-dihydropyridine and a calcium channel antagonist. Antihypertensive.
in vivo

Benidipine (3, 5, 10 μg/kg; i.v.) shows significant anti-apoptosis effects in a haemodynamically independent manner[2].
Benidipine (5 mg/kg; i.v.; every other day for 6 weeks) increases the activity of endothelial cell-type nitric oxide synthase (eNOS) and improves coronary circulation in hypertensive rats[3].
Benidipine (1, 3, 10 mg/kg; p.o.; once daily for 1 week) significant cardioprotective effects against ischemia-reperfusion injury[4].

Animal Model:Sham MI (myocardial ischaemia)/R (ischmia reperfused injury) rabbits and MI/R rabbits[2]
Dosage:3, 5, 10 μg/kg
Administration:I.v.
Result:Caused a significant decreased in HR ( heart rate), MABP (mean arterial blood pressure), PRI (pressure-rateindex) at 10 μg/kg, decreased apoptotic positive cells to7.4% at 3 μg/kg and not significantly different from that seen in the group treated with higher dose.
Animal Model:Renovascular hypertensive rats (RHR)[3]
Dosage:5 mg/kg (dissolved in peanut oil)
Administration:I.v.; every other day for 6 weeks
Result:Significantly decreased the blood pressure and coronary vascular resistance index, but increased nitrite production and eNOS mRNA expression and significantly increased the coronary flow at rest, the capillary density.
Animal Model:Rats (heart model (Langendorff perfusion))[4]
Dosage:1, 3, 10 mg/kg
Administration:P.o.; once daily for 1 week
Result:Significantly increased the post-ischemic recovery of LVDP and LV dP/dt max (LVDP: 87.5±10.1 vs 64.6±11.9%; LV dP/dt max: 97.8±10.4 vs 70.2±15.7%; p<0.05) at 3 mg/kg.
Enzyme inhibitorThis oral, once-daily antihypertensive agent (FW = 505.57 g/mol; CAS 105979-17-7), also known by its code name KW-3049, trade name Coniel?, and systematic name O -methyl,O -[(3R)-1-(phenylmethyl)piperidin-3-yl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, is a dihydropyridine-class calcium ion blocker that is effective against L-, N-, and T-channels, with potent and selective inhibitory action on cardiac slow calcium channels. Benidipine bound stereospecifically to nitrendipine binding sites of rat myocardium with high affinity (Ki = 0.13 nM) and to the rat brain a1-adrenergic receptor (Ki = 1.2 μM). KW-3049 exhibited no remarkable binding affinity to a2 adrenergic, b-adrenergic, D2 dopamine, H1 histamine, S2 serotonin, A1 adenosine, A2 adenosine and muscarinic cholinergic receptors at 100 μM.
Tag:Benidipine(105979-17-7) Related Product Information
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