Levamlodipine
(Synonyms: (S)-Amlodipine;左旋氨氯地平;S-amlodipine) 目录号 : GC20097
Levamlodipine 是一种二氢吡啶钙通道阻滞剂，具有舒张血管的作用，可用于高血压和心绞痛的研究。
Cas No.:103129-82-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Levamlodipine belongs to the dihydropyridine group of calcium channel blockers. Levamlodipine, also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive and anti-anginal medication. The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however, with differing nomenclature. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.
| Cas No. | 103129-82-4 | SDF | |
| 别名 | (S)-Amlodipine;左旋氨氯地平;S-amlodipine | ||
| 分子式 | C20H25ClN2O5 | 分子量 | 408.88 |
| 溶解度 | DMSO:10 mM | 储存条件 | -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 | 2.4457 mL | 12.2285 mL | 24.4571 mL |
| 5 mM | 0.4891 mL | 2.4457 mL | 4.8914 mL |
| 10 mM | 0.2446 mL | 1.2229 mL | 2.4457 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Effect of low-dose Levamlodipine Besylate in the treatment of vascular dementia
Sci Rep 2019 Dec 3;9(1):18248.PMID:31796756DOI:10.1038/s41598-019-47868-0.
Vascular dementia (VaD) is a complex disorder caused by reduced blood flow in the brain. However, there is no effective pharmacological treatment option available until now. Here, we reported that low-dose Levamlodipine besylate could reverse the cognitive impairment in VaD mice model of right unilateral common carotid arteries occlusion (rUCCAO). Oral administration of Levamlodipine besylate (0.1 mg/kg) could reduce the latency to find the hidden platform in the MWM test as compared to the vehicle group. Furthermore, vehicle-treated mice revealed reduced phospho-CaMKII (Thr286) levels in the hippocampus, which can be partially restored by Levamlodipine besylate (0.1 mg/kg and 0.5 mg/kg) treatment. No significant outcome on microglia and astrocytes were observed following Levamlodipine besylate treatment. This data reveal novel findings of the therapeutic potential of low-dose Levamlodipine besylate that could considerably enhance the cognitive function in VaD mice.
Bioequivalence of Levamlodipine besylate tablets in healthy Chinese subjects: a single-dose and two-period crossover randomized study
BMC Pharmacol Toxicol 2020 Nov 19;21(1):80.PMID:33213527DOI:10.1186/s40360-020-00459-6.
Background: Levamlodipine, a calcium channel blocker, has been show act as a cardiovascular drug. To compare the pharmacokinetic parameters between Levamlodipine (test formulation) at a single dose of 5 mg and amlodipine (reference formulation) at a single dose of 10 mg, the bioequivalence study was carried out. Methods: A single-dose randomized, open-label, two-period crossover study was designed in healthy Chinese subjects. 48 subjects were divided into fasted and fed groups equally. The subjects randomly received the test or reference formulations at the rate of 1:1. Following a 21-day washout period, the alternative formulations were received. The blood samples were collected at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 h later. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was applied to determine the plasma concentrations of Levamlodipine. Adverse events were recorded. Results: The 90% confidence intervals (CIs) of the ratio of geometric means (GMRs) of Cmax, AUC0-t, and AUC0-∞ under both fasted and fed conditions were within the prespecified bioequivalence limits between 80 ~ 125%. Under fasted conditions, 24 subjects were enrolled and completed the study. The mean Cmax was (2.70 ± 0.49) ng/mL, AUC0-t was (141.32 ± 36.24) ng × h/mL and AUC0-∞ was (157.14 ± 45.65) ng × h/mL after a single dose of 5 mg Levamlodipine. The mean Cmax was (2.83 ± 0.52) ng/mL, AUC0-t was (153.62 ± 33.96) ng × h/mL and AUC0-∞ was (173.05 ± 41.78) ng × h/mL after a single dose of 10 mg amlodipine. Under fed conditions, 24 subjects were enrolled and completed the study. The mean Cmax was (2.73 ± 0.55) ng/mL, AUC0-t was (166.93 ± 49.96) ng × h/mL and AUC0-∞ was (190.99 ± 70.89) ng × h/mL after a single dose of 5 mg Levamlodipine. The mean Cmax was (2.87 ± 0.81) ng/mL AUC0-t was (165.46 ± 43.58) ng × h/mL and AUC0-∞ was (189.51 ± 64.70) ng × h/mL after a single dose of 10 mg amlodipine. Serious adverse event was not observed. Conclusion: The trial confirmed that Levamlodipine at a single dose of 5 mg and amlodipine at a single dose of 10 mg were bioequivalent under both fasted condition and fed condition. Trial registration: Cinicaltrials, NCT04411875 . Registered 3 June 2020 - Retrospectively registered.
Clinical assessment of Levamlodipine besylate combination therapy for essential hypertension: A protocol for systematic review and meta-analysis
Medicine (Baltimore) 2022 Apr 1;101(13):e29148.PMID:35421067DOI:10.1097/MD.0000000000029148.
Background: Essential hypertension has been regarded a significant risk factor for cardiovascular disease across the globe, and a significant escapable causation of early death as well as morbidity in the U.S. When angiotensin II receptor blockers and calcium channel blockers are used to treat essential hypertension, most patients will have inadequate blood pressure management. As a result, including a diuretic in the regimen is necessary. The current study's aim is to investigate the effectiveness as well as safety of Levamlodipine besylate combination therapy in treating essential hypertension at varying degrees of severity. Methods: In establishing the effectiveness and safety of the mix of Levamlodipine besylate and dihydropyridine for essential hypertension, the authors will conduct a systematic review and, where applicable, a meta-analysis of randomized controlled clinical trials. A total of 8 electronic databases will be used in the search, including 4 English databases (PubMed, Web of Science, EMBASE, and Cochrane Library) and 4 Chinese databases (China National Knowledge Infrastructure, Chinese BioMedical Literature database, Chinese Scientific Journal database, and WanFang database). All articles published in the databases will be considered between their inception and January 18, 2022. Only articles published in English or Mandarin Chinese will be picked. A group of writers will independently evaluate each reference to see if it is eligible and whether there are any duplicates. The same authors will do data extraction for all eligible studies and use the Cochrane risk of bias tool to evaluate the risk of bias in the trials chosen for inclusion. Results: The analysis will evaluate the efficiency and level of safeness of Levamlodipine besylate combined treatment for essential hypertension. Conclusions: Our systematic review will offer evidence for judging whether Levamlodipine besylate combination therapy can be considered an effective intercession for essential hypertension. Ethics and dissemination: Ethical approval will not be required as no original data will be collected as part of this review. Registration number: DOI 10.17605/OSF.IO/H8ZR2.
Investigation of the binding properties between Levamlodipine and HSA based on MCR-ALS and computer modeling
Spectrochim Acta A Mol Biomol Spectrosc 2021 Jan 15;245:118929.PMID:32961448DOI:10.1016/j.saa.2020.118929.
Levamlodipine (LEE) is a drug commonly used for antihypertensive treatment in clinical therapy. The overlapping fluorescence spectra of LEE and human serum albumin (HSA) cause some trouble in analysis of interactions between them by using the classic fluorescence method. Here, the multivariate curve resolution-alternating least squares (MCR-ALS) approach was used to overcome this disadvantage. Meanwhile, the binding properties of LEE-HSA complex were then explored through computer modeling. The MCR-ALS results suggested that LEE-HSA complex was present in the mixture solution of LEE and HSA. This conclusion was then confirmed by the Stern-Volmer equation and time-resolved fluorescence experiment. The binding constant (Ka) was 2.139 × 104 L·mol-1 at 298 K. LEE was located close to the Trp-214 residue of HSA, with van der Waals forces and hydrogen bonding as main driving forces for this interaction. LEE can alter the conformation of HSA, in which the content of α-helix reduced from 57.2% to 52.3%. The Pi-Alkyl interactions contributed to maintaining the stability of the LEE-HSA complex. The results of molecular dynamics simulations showed that LEE-HSA complex was formed within 5 ns, and the particle size (Rg) of HSA was altered by the binding reaction. This study would promote better understanding of the transportation and distribution mechanisms of LEE in the human body.
Probing the interaction between Levamlodipine and hemoglobin based on spectroscopic and molecular docking methods
Spectrochim Acta A Mol Biomol Spectrosc 2019 Dec 5;223:117306.PMID:31255862DOI:10.1016/j.saa.2019.117306.
In recent years, Levamlodipine (LAML) has been widely used as a common drug for the treatment of hypertension. However, no reports exist that focus on the binding process of LAML with the transport proteins present in blood circulation. Here, several spectroscopy techniques, molecular docking and a molecular dynamics simulation were employed to comprehensively analyze the mechanism underlying the interaction between bovine hemoglobin (BHb) and LAML, as well as the effect of other drugs on the BHb-LAML system. The results indicated that a stable BHb-LAML complex was formed and that the binding site for LAML was located at β-37 tryptophan in the central cavity of BHb. Van der Waals force and hydrogen bonds played major roles in this binding process, and the number of binding sites (n) in the binary system was approximately equal to 1. Multiple spectroscopy experiments (FT-IR and three-dimensional fluorescence spectrometry) and a dynamics simulation revealed that LAML could induce a conformational in BHb and that the microenvironment of Trp/Tyr changed. Interestingly, the values of the binding constant between LAML and BHb significantly increased due to the effect of rofecoxib, propranolol and enalapril. Meanwhile, these drugs did not produce synergistic or negative synergistic effects on the LAML binding with BHb. These results provide new insight into the transport mechanisms for LAML in the human body.