L-Phenylephrine
(Synonyms: 去氧肾上腺素; (R)-(-)-Phenylephrine; L-Phenylephrine) 目录号 : GC17319
A selective adrenergic α1A receptor agonist
Cas No.:59-42-7
Sample solution is provided at 25 µL, 10mM.
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Target: adrenergic α1A receptor
Ki: 1.4 μM
L-Phenylephrine is a selective agonist of adrenergic α1A receptor, with the Ki value of 1.4 μM, while having less effect against the α1B and α1C receptor subtypes, with the Ki values of 23.9 μM and 47.8 μM, respectively [1].
In Vitro: In neonatal rat cardiomyocytes, 50 μM L-Phenylephrine treatment could protect cells from apoptosis induced by hypoxia (95% N2 and 5% CO2) and serum deprivation through α-adrenergic receptor stimulation [2]. Besides, in neural progenitor cells (NPCs), 10 μM L-Phenylephrine could increase NPCs proliferation by approximately 160% [3]. Furthermore, in cultured rat neonatal CMs (NCMs), L-Phenylephrine could increase cross-sectional area, and significantly increase IL-6 mRNA levels, while decreasing PGC1α mRNA levels [4].
In Vivo: Studies in Sprague-Dawley male rats found that, local infiltration of L-phenylephrine could induce cutaneous anesthesia in a dose dependent manner, which could be significantly inhibited by α1-adrenergic receptor antagonists [5].
Clinical trial: Based on 8 unpublished studies that included 138 patients with nasal congestion, oral administration with 25 mg L-Phenylephrine could significantly reduce maximal nasal airway resistance (NAR) compared with placebo of 27.6% (95% CI 17.5% to 37.7%) [6].
References:
[1] Lomasney J W, Cotecchia S, Lorenz W, et al. Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. The gene for which is located on human chromosome 5.[J]. Journal of Biological Chemistry, 1991, 266(10): 6365-6369.
[2] Zhu H, Mcelweewitmer S, Perrone M, et al. Phenylephrine protects neonatal rat cardiomyocytes from hypoxia and serum deprivation-induced apoptosis.[J]. Cell Death & Differentiation, 2000, 7(9): 773-784.
[3] Hiramoto T, Ihara Y, Watanabe Y, et al. α-1 Adrenergic receptors stimulation induces the proliferation of neural progenitor cells in vitro[J]. Neuroscience Letters, 2006, 408(1): 25-28.
[4] Planavila A, Redondo I, Hondares E, et al. Fibroblast growth factor 21 protects against cardiac hypertrophy in mice[J]. Nature Communications, 2013.
[5] Shieh J, Chu C, Wang J, et al. Epinephrine, phenylephrine, and methoxamine induce infiltrative anesthesia via α1-adrenoceptors in rats[J]. Acta Pharmacologica Sinica, 2009, 30(9): 1227-1236.
[6] Hatton R C, Winterstein A G, Mckelvey R P, et al. Efficacy and Safety of Oral Phenylephrine: Systematic Review and Meta-Analysis[J]. Annals of Pharmacotherapy, 2007, 41(3): 381-390.
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Animal experiment: |
Rats: A total of 170 male Wistar rats are randomLy allocated into 17 groups (n=10) using random number tables. Short-term (40 minutes) mechanical ventilation with high tidal volume is performed to induce lung injury, impair active Na+ transport and lung liquid clearance in the rats. Unventilated rats serves as controls. To demonstrate the effect of phenylephrine on alveolar fluid clearance, phenylephrine at different concentrations (10, 1, 0.1, 0.01, and 0.001 μM) is injected into the alveolar space of the HVT ventilated rats[5]. |
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References: [1]. Ford AP, et al. Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications foralpha1-adrenoceptor classification. Br J Pharmacol. 1997 Jul;121(6):1127-35. |
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| Cas No. | 59-42-7 | SDF | |
| 别名 | 去氧肾上腺素; (R)-(-)-Phenylephrine; L-Phenylephrine | ||
| 化学名 | 3-hydroxy-αR-[(methylamino)methyl]-benzenemethanol | ||
| Canonical SMILES | OC1=CC=CC([C@@H](O)CNC)=C1 | ||
| 分子式 | C9H13NO2 | 分子量 | 167.2 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml,PBS (pH 7.2): 15 mg/ml | 储存条件 | Store at RT |
| 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 | 5.9809 mL | 29.9043 mL | 59.8086 mL |
| 5 mM | 1.1962 mL | 5.9809 mL | 11.9617 mL |
| 10 mM | 0.5981 mL | 2.9904 mL | 5.9809 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet