| Identification | More | [Name]
Benidipine | [CAS]
105979-17-7 | [Synonyms]
BENIDIPINE
BENIDIPINE HCL
BENIDIPINE HYDROCHLORIDE
CAPADIPINE
CONIEL
KW-3049
NACADIPINE
3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl (3R)-1-(phenylmethyl)-3-piperidinyl ester, (4R)-rel-
3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl 1-(phenylmethyl)-3-piperidinyl ester, (R*,R*)-
3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl 1-(phenylmethyl)-3-piperidinyl ester, (R*,R*)-(+-)-
(+/-)-(R*)-3-((R*)-1-Benzyl-3-piperidyl) methyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate
(+/-)-(R*)-3-((R*)-1-Benzyl-3-piperidyl) methyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate
(R^<*>^，R^<*>^)-(±)-2，6-dimethyl-4-(3-nitrophenyl)-1，4-dihydro-3，5-pyridinedicarboxylic acid methyl(R^<*>^)-1-BenzyI-3-piperidylester
(4R)-1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid 3-methyl 5-[(3R)-1-benzylpiperidin-3-yl] ester
(4R)-2,6-Dimethyl-1,4-dihydro-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid 3-methyl 5-[(3R)-1-benzylpiperidin-3-yl] ester | [EINECS(EC#)]
857-680-4 | [Molecular Formula]
C28H32ClN3O6 | [MDL Number]
MFCD00906929 | [Molecular Weight]
542.02 | [MOL File]
105979-17-7.mol |
| Hazard Information | Back Directory | [Uses]
Benidipine (CAS# 105979-17-7) is a 1,4-dihydropyridine and a calcium channel antagonist. Antihypertensive. | [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. | [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. |
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