Benidipine
Based on 1 publication(s) in Google Scholar
Benidipine is a potent and orally active calcium channel antagonist. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats.
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- CAS No.: 105979-17-7
- Formule: C28H31N3O6
- Masse moléculaire:505.56
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sham MI (myocardial ischaemia)/R (ischmia reperfused injury) rabbits and MI/R rabbits[2]
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Dosage:3, 5, 10 µg/kg
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Administration:I.v.
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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.
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Animal Model:Renovascular hypertensive rats (RHR)[3]
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Dosage:5 mg/kg (dissolved in peanut oil)
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Administration:I.v.; every other day for 6 weeks
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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.
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Animal Model:Rats (heart model (Langendorff perfusion))[4]
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Dosage:1, 3, 10 mg/kg
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Administration:P.o.; once daily for 1 week
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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.
Chemical Information
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CAS No. 105979-17-7
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Masse moléculaire 505.56
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Formule C28H31N3O6
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SMILES
O=C(C1=C(C)NC(C)=C(C(O[C@H]2CN(CC3=CC=CC=C3)CCC2)=O)[C@@H]1C4=CC=CC([N+]([O-])=O)=C4)OC
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Synonyms
KW-3049 free base
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Metab
Hepatocyte-to-intestinal stem cell remote communication regulates blood glucose homeostasis. [Abstract]2026 Jul 7;38(7):1367-1384.e9. PMID: 42309059
Pureté et documentation
Références
[1]. Yao K, et al. Pharmacological, pharmacokinetic, and clinical properties of benidipine hydrochloride, a novel, long-acting calcium channel blocker. J Pharmacol Sci. 2006 Apr;100(4):243-61. [Content Brief]
[2]. Gao F, et al. Anti-apoptotic effect of benidipine, a long-lasting vasodilating calcium antagonist, in ischaemic/reperfused myocardial cells. Br J Pharmacol. 2001 Feb;132(4):869-78. [Content Brief]
[3]. Kobayashi N, et al. Benidipine stimulates nitric oxide synthase and improves coronary circulation in hypertensive rats. Am J Hypertens. 1999 May;12(5):483-91. [Content Brief]
[4]. Masanori S, et al. Orally administered benidipine and manidipine prevent ischemia-reperfusion injury in the rat heart. Circ J. 2004 Mar;68(3):241-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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