Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
H1 Receptor 1.01 mM (IC50)
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ln Vitro |
In order to extend the duration of antihistaminic effects and delay metabolic time, pheniramine inhibits CYP2D6, a particular P450-isozyme[1]. By blocking histamine with an IC50 value of 1.01 mM, pheniramine prevents Ca2+ influx into BC3H-1 cells and controls the activity of the Ca2+ transmembrane in cells[2].In human T-cell acute lymphoblastic leukemia cell lines, pheniramine (0.5, 1.0 mM; 24 h) induces cell apoptosis[3]. The time-dependent inhibition of cell proliferation by pheniramine (1 μM-1 mM; 12-48 h) had inhibitory concentration IC50s of 550 μM for CCRF-CEM cells and 420 μM for Jurkat cells, respectively[3].
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ln Vivo |
In rats, pheniramine (1.75 μM) causes spinal block and a local anesthetic effect[4].
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Cell Assay |
Apoptosis Analysis [3]
Cell Types: Human T-cell acute lymphoblastic leukemia Cell Types: CCRF-CEM and Jurkat ALL Tested Concentrations: 0.5, 1.0 mM Incubation Duration: 24 hrs (hours) Experimental Results: Induced cells apoptosis with chromatin condenses and marginalizes, and nuclear debris spread into the cytoplasm. Cell Viability Assay[3] Cell Types: Human T-cell acute lymphoblastic leukemia Cell Types: CCRF-CEM and Jurkat ALL Tested Concentrations: 1 μM-1 mM Incubation Duration: 12, 24, 48 hrs (hours) Experimental Results: Inhibited cell proliferation and survival in a time- and dose-dependent manner. |
Animal Protocol |
Animal/Disease Models: Sprague–Dawley rats (300-350 g ; male)[4]
Doses: 0.30, 0.60, 0.90, 1.50, 1.75 μM Route of Administration: Intrathecal injection; one time Experimental Results: Resulted the spinal block and displayed dose-dependent effect. demonstrated 100% blockades in motor function, proprioception, and nociception , with full recovery duration of action about 41, 56, and 88 min, respectively, at 1.75 μM. |
References |
[1]. Sharma A, et al. Classic histamine H1 receptor antagonists: a critical review of their metabolic and pharmacokinetic fate from a bird's eye view. Curr Drug Metab. 2003 Apr;4(2):105-29.
[2]. Brown RD, et al. Alpha 1-adrenergic and H1-histamine receptor control of intracellular Ca2+ in a muscle cell line: the influence of prior agonist exposure on receptor responsiveness. Mol Pharmacol. 1986 Jun;29(6):531-9. [3]. Jangi SM, et al. Apoptosis of human T-cell acute lymphoblastic leukemia cells by diphenhydramine, an H1 histamine receptor antagonist. Oncol Res. 2004;14(7-8):363-72. [4]. Hung CH, et al. Spinal anesthesia with diphenhydramine and pheniramine in rats. Eur J Pharmacol. 2011 Dec 30;673(1-3):20-4. |
Molecular Formula |
C16H20N2
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Molecular Weight |
240.34
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CAS # |
86-21-5
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Related CAS # |
Pheniramine maleate;132-20-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CN(C)CCC(C1=CC=CC=C1)C2=CC=CC=N2
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.1608 mL | 20.8039 mL | 41.6077 mL | |
5 mM | 0.8322 mL | 4.1608 mL | 8.3215 mL | |
10 mM | 0.4161 mL | 2.0804 mL | 4.1608 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.