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Benidipine

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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
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Benidipine Chemical Properties

Boiling point:
625.2±55.0 °C(Predicted)
Density 
1.29±0.1 g/cm3(Predicted)
pka
pKa 7.34(H2O(long extrapolation) ) (Uncertain)
Water Solubility 
316μg/L at 25℃
InChIKey
QZVNQOLPLYWLHQ-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|
LogP
4.61
CAS DataBase Reference
105979-17-7(CAS DataBase Reference)
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Benidipine Usage And Synthesis

Uses

Benidipine (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 inhibitor

This 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.

Benidipine Preparation Products And Raw materials

Raw materials

Methyl 3-aminocrotonateDiethyl 1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate3,5-Pyridinedicarboxylic acid1-Benzyl-3-piperidinol

BenidipineSupplier

Jinan Xuanzheng Pharmaceutical Co. LTD Gold
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18610218799
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xuanzhengyaoye@126.com
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
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3bsc@sina.com
LGM Pharma
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1-(800)-881-8210
Email
inquiries@lgmpharma.com
Hangzhou Yuhao Chemical Technology Co., Ltd
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0571-82693216
Email
info@yuhaochemical.com
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
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