L-Phenylephrine (Synonyms: (R)-(-)-Phenylephrine) |
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Catalog No.GC17319
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(R)-(-)-L-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 59-42-7
Sample solution is provided at 25 µL, 10mM.
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Clinical trial: Based on 8 unpublished studies that included 138 patients with nasal congestion, oral administration with 25 mg L-Phenylephrine could significantly reduce maximal nasal airway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 | |
| Synonyms | (R)-(-)-Phenylephrine | ||
| Chemical Name | 3-hydroxy-αR-[(methylamino)methyl]-benzenemethanol | ||
| Canonical SMILES | OC1=CC=CC([C@@H](O)CNC)=C1 | ||
| Formula | C9H13NO2 | M.Wt | 167.2 |
| Solubility | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml,PBS (pH 7.2): 15 mg/ml | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 | 598.1 μL | 2.9904 mL | 5.9809 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)