Barnidipine
(Synonyms: 巴尼地平,Mepirodipine; YM-09730-5(Free base)) 目录号 : GC35469
A calcium channel blocker
Cas No.:104713-75-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Barnidipine is a dihydropyridine calcium channel blocker that has an IC50 value of 0.35 nM in potassium-induced tonic contraction of pig coronary artery.1 It demonstrates antihypertensive activity by reducing peripheral vascular resistance. It decreases blood pressure in spontaneously hypertensive rats when administered orally at 1 and 3 mg/kg per day.2 Formulations containing barnidipine have been used as a treatment for hypertension.
1.Nakayama, K., Kashiwabara, T., Yamada, S., et al.Assessment in pig coronary artery of long-lasting and potent calcium antagonistic actions of the novel dihydropyridine derivative mepirodipine hydrochlorideArzneimittelforschung39(1)50-55(1989) 2.Kawashima, K., Toda, H., Oohata, H., et al.Antihypertensive and diuretic effects of YM-09730-5, a new calcium antagonist, in stroke-prone spontaneously hypertensive ratsGen. Pharmacol.22(2)263-266(1991)
| Cas No. | 104713-75-9 | SDF | |
| 别名 | 巴尼地平,Mepirodipine; YM-09730-5(Free base) | ||
| Canonical SMILES | O=C(C1=C(C)NC(C)=C(C(O[C@@H]2CN(CC3=CC=CC=C3)CC2)=O)[C@H]1C4=CC=CC([N+]([O-])=O)=C4)OC | ||
| 分子式 | C27H29N3O6 | 分子量 | 491.54 |
| 溶解度 | DMSO : 98mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0344 mL | 10.1721 mL | 20.3442 mL |
| 5 mM | 0.4069 mL | 2.0344 mL | 4.0688 mL |
| 10 mM | 0.2034 mL | 1.0172 mL | 2.0344 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Barnidipine
Drugs 2001;61(7):989-96; discussion 997-8.PMID:11434453DOI:10.2165/00003495-200161070-00007.
Bamidipine is an antihypertensive drug belonging to the dihydropyridine (DHP) group of calcium antagonists. It is available in a modified-release formulation which has a gradual onset of action and is effective in a single daily oral dose of 10 to 20 mg. Bamidipine has selective action against cardiovascular calcium antagonist receptors and its antihypertensive action is related to the reduction of peripheral vascular resistance secondary to its vasodilatory action. The clinical antihypertensive efficacy of Barnidipine is similar to that of other DHP calcium antagonists such as nitrendipine and amlodipine, and antihypertensives belonging to other drug classes such as atenolol and enalapril. Barnidipine has been found to be as efficacious and well tolerated as hydrochlorothiazide in the management of hypertension in elderly patients. Barnidipine is generally well tolerated. As with other DHP calcium antagonists, vasodilator adverse events such as headache, flushing and peripheral oedema account for most of the adverse events reported with its use and are usually transient. Oedema is less frequent than with amlodipine and nitrendipine. Its use is not associated with reflex tachycardia.
Interaction profile and tolerability of Barnidipine
Int J Clin Pract Suppl 2000 Nov;(114):36-40.PMID:11221293doi
Introduction: Barnidipine is a new dihydropyridine calcium antagonist that is presented in modified-release capsules containing a single S-S optical isomer of the molecule. Its characteristics are of interest, as there is evidence of differences in kinetics, dynamics, interactions and safety of individual enantiomers in traditional racemic preparations of calcium antagonists. The safety of Barnidipine and its interaction profile are reviewed. Safety: Adverse events with Barnidipine are of mild to moderate intensity, most commonly of type I and occur in the early phase of treatment. Furthermore, safety results in elderly patients are comparable with those in the general population, indicating that Barnidipine can be used without dose adjustment in elderly hypertensive patients. Interactions: Barnidipine has a pharmacokinetic interaction profile that compares favourably with those from other calcium antagonists. The pharmacokinetic properties of Barnidipine are unaffected by food. Minor increases in its availability may occur with concomitant use of alcohol or grapefruit juice, but these are unlikely to have clinical relevance. In contrast with several other calcium antagonists, Barnidipine does not affect the steady-state kinetics of digoxin, whereas, like other calcium antagonists its bioavailability may be increased by the concomitant administration of cimetidine. In addition, the potential of Barnidipine and its major metabolites to affect the metabolism of concomitant medication is unlikely to be of clinical relevance. Conclusion: The interaction and tolerability profile of Barnidipine is well established in all age groups.
Barnidipine ameliorates the vascular and renal injury in L-NAME-induced hypertensive rats
Eur J Pharmacol 2015 Oct 5;764:433-442.PMID:26187312DOI:10.1016/j.ejphar.2015.07.033.
The present study was aimed to investigate the influence of Barnidipine treatment on early stage hypertension by determining the function and morphology of the mesenteric and renal arteries as well as the kidney in N(ω)-Nitro-L-Arginine Methyl Ester (L-NAME)-induced hypertensive rats. Barnidipine (3 mg/kg/day p.o) was applied to rats after 2 weeks of L-NAME (60 mg/kg/day) administration, and continued for the next 3 weeks concomitantly with L-NAME. The systolic blood pressure (SBP) of rats was determined to decrease significantly in Barnidipine treated hypertensive group when compared to that of rats received L-NAME alone. Myograph studies demonstrated that the contractile reactivity to noradrenaline were significantly reduced in both of the resistance arteries while endothelium-dependent relaxations to acethylcholine were significantly diminished particularly in the mesenteric arteries of L-NAME-induced hypertensive rats. The impaired contractile and endothelial responses were completely restored by concomitant treatment of Barnidipine with L-NAME. Histopathological examinations verified structural alterations in the arteries as well as the kidney. Moreover, a decrease in endothelial nitric oxide synthase (eNOS) expression was presented both in the arteries and kidney of hypertensive rats which were increased following Barnidipine treatment. Elevated plasma levels of malondialdehyde (MDA) and myeloperoxidase (MPO) were also reduced in Barnidipine treated hypertensive rats. In conclusion, besides to its efficacy in reducing the elevated SBP, amelioration of vascular function, modulation of arterial and renal eNOS expressions as well as reduction of the plasma levels of oxidative and inflammatory biomarkers are possible supportive mechanisms mediating the favorable implications of Barnidipine in L-NAME-induced hypertension model.
Barnidipine: a new calcium channel blocker for hypertension treatment
Expert Rev Cardiovasc Ther 2005 Mar;3(2):207-13.PMID:15853594DOI:10.1586/14779072.3.2.207.
Although it is commonly agreed that all antihypertensive medications have similar efficacy, there are important differences related to safety, tolerability, patient adherence, cost effectiveness and effects on the prevention or retardation of associated disease progression. It is desirable for antihypertensives to have a long duration of action so that once-daily dosing is possible. In addition, antihypertensive medication must be able to be administered concomitantly with other drugs likely to be taken by the patients. This is particularly critical in the elderly population. Barnidipine, a novel, long-acting calcium antagonist, has met these challenges of modern pharmacotherapy. Its once-daily dosing, good tolerability and durable antihypertensive effect contribute to excellent patient adherence and make this drug a valuable addition to the antihypertensive formulary.
Barnidipine, a long-acting slow onset calcium antagonist
Int J Clin Pract Suppl 2000 Nov;(114):2-5.PMID:11221290doi
Barnidipine is a stereochemically pure dihydropyridine calcium antagonist with a high potency. The drug showed a slow onset and long-lasting vasorelaxating effect in vitro, and strong antihypertensive activity in hypertension models. Barnidipine was shown to have a high vasoselectivity and offered protection in cardiac and renal ischaemia models. The in vitro drug:drug interaction profile suggests a low potential for clinically relevant interactions with concomitant medication. It can be anticipated that Barnidipine is an attractive calcium antagonist, offering good blood pressure control without compensatory baroreflex activity.