| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Pheniramine Maleate specifically targets the histamine H1 receptor, acting as an antagonist. By binding to H1 receptors, it competes with histamine and blocks its pharmacological effects, which include vasodilation and increased vascular permeability. This action is responsible for its antihistaminic and antipruritic effects. It also inhibits phospholipase A2 and the production of endothelium-derived relaxing factor, nitric oxide.
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| ln Vitro |
Pheniraminemaleate slows down metabolism and prolongs the effects of antihistamines by inhibiting CYP2D6, a particular P450 isoenzyme [1]. With an IC50 value of 1.01 mM, pheniraminemaleate suppresses histamine, which modifies cellular Ca2+ transmembrane effects and prevents Ca2+ influx into BC3H-1 cells[2]. Within 24 hours, human T-cell acute lymphoblastic leukemia cell lines treated with pheniraminemaleate (0.5, 1.0 mM) undergo apoptosis [3]. IC50s for pheniraminemaleate (1 μM-1 mM; 12-48 h) are 550 μM for CCRF-CEM cells and 420 μM for Jurkat cells, respectively, showing a time-dependent inhibition of cell growth [3].
In vitro, Pheniramine Maleate acts as a histamine H1 receptor antagonist. It has also been shown to display antitumor effects and induce apoptosis in leukemia cells. Its activity is characterized by its ability to inhibit histamine-induced responses and to modulate cell signaling pathways in cancer cells. It also has anticholinergic properties. |
| ln Vivo |
In rats, pheniraminemaleate (1.75 μM) results in spinal cord block and local anesthesia [4].
In vivo, Pheniramine Maleate is used as an antihistamine for the symptomatic treatment of allergic conditions. It is administered orally and acts on H1 receptors in various tissues. It is also used as a safe and effective local agent that can suppress or relieve pain. Its in vivo effects are dose-dependent and are related to its antihistaminic and anticholinergic activities. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for Pheniramine Maleate are performed using radioligand binding assays. In these assays, membrane preparations from cells expressing histamine H1 receptors are incubated with a radiolabeled H1 antagonist and varying concentrations of Pheniramine Maleate. The displacement of the radioligand is measured to determine its affinity (Ki) for the receptor.
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| Cell Assay |
Cell viability assay [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: Induction of apoptosis, chromatin condensation and marginalization, and nuclear fragments diffuse 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: Inhibition of cell proliferation and survival time and dose-dependent manner. In vitro cellular assays for Pheniramine Maleate are used to study its effects on cells. In immune cells, its ability to inhibit histamine-induced calcium mobilization or cytokine production can be measured. In cancer cells, its effects on cell viability, apoptosis, and signaling pathways are assessed. These assays confirm its mechanism as an H1 antagonist and its potential antitumor activity. |
| Animal Protocol |
Animal/Disease Models: Sprague–Dawley rat (300-350 g; male) [4]
Doses: 0.30, 0.60, 0.90, 1.50, 1.75 μM Route of Administration: Intrathecal; Primary Experimental Results:Spinal block produced, and dose indicated Dependency effect. At 1.75 μM, motor function, proprioception, and nociception were 100% blocked, and the duration of action for complete recovery was approximately 41, 56, and 88 minutes, respectively. In vivo animal studies for Pheniramine Maleate are conducted in models of allergic reactions, such as histamine-induced wheal formation or anaphylaxis. Animals are treated with the compound, and the reduction of these responses is measured. These studies confirm its antihistaminic efficacy in vivo. It has also been studied for its analgesic and antipruritic effects in animal models. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Pheniramine Maleate include a molecular weight of 356.42 g/mol and a molecular formula of C₁₆H₂₀N₂·C₄H₄O₄. It is water-soluble. It is a white powder with a faint amine-like odor and a melting point of 107°C. As a first-generation antihistamine, it can cross the blood-brain barrier, leading to sedation. Its half-life and other PK parameters are consistent with other antihistamines in its class.
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| Toxicity/Toxicokinetics |
Toxicological data for Pheniramine Maleate indicate that it is generally safe at therapeutic doses. Common side effects include drowsiness, blurred vision, and dry mouth. It may also cause euphoria, nervousness, insomnia, and tremors in some individuals. Overdose can lead to severe anticholinergic effects. It is contraindicated in patients with narrow-angle glaucoma and prostatic hypertrophy.
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| References |
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| Additional Infomation |
Pheniramine maleate is a white powder with a slightly amine odor. Melting point: 107℃. pH (1% solution): 4.5-5.5. It is a pharmaceutical antihistamine. Pheniramine maleate is an organic molecular entity. Pheniramine maleate is the maleate salt form of Pheniramine, an alkylamine derivative with antihistamine and vasodilatory effects. Pheniramine maleate binds to histamine H1 receptors, thereby inhibiting the production of phospholipase A2 and endothelial relaxing factor (nitric oxide). Subsequently, because nitric oxide cannot activate guanylate cyclase, the level of cyclic guanosine monophosphate (cGMP) decreases, thereby inhibiting smooth muscle tissue contraction, reducing capillary permeability, and alleviating histamine-activated allergic reactions. It is one of the histamine H1 receptor antagonists with a weak sedative effect. It is used to treat hay fever, rhinitis, allergic dermatitis, and pruritus.
Pheniramine Maleate is a first-generation antihistamine used for the symptomatic treatment of allergic conditions. Its CAS number is 132-20-7. It is also known as Trimetose and Prophenpyridamine maleate. In addition to its antihistaminic properties, it has been shown to display antitumor effects and induce leukemia cell apoptosis, making it a compound of interest for cancer research. It is available for research and clinical use. |
| Molecular Formula |
C20H24N2O4
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| Molecular Weight |
356.4156
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| Exact Mass |
356.173
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| CAS # |
132-20-7
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| Related CAS # |
Pheniramine;86-21-5
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| PubChem CID |
5282139
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| Appearance |
White to off-white solid powder
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| Boiling Point |
348.3ºC at 760 mmHg
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| Melting Point |
104-108°C
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| Flash Point |
164.5ºC
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| Vapour Pressure |
5.07E-05mmHg at 25°C
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| LogP |
2.877
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
340
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCC(C1=CC=CC=C1)C2=CC=CC=N2.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
SSOXZAQUVINQSA-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C16H20N2.C4H4O4/c1-18(2)13-11-15(14-8-4-3-5-9-14)16-10-6-7-12-17-16;5-3(6)1-2-4(7)8/h3-10,12,15H,11,13H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;N,N-dimethyl-3-phenyl-3-pyridin-2-ylpropan-1-amine
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ≥ 38 mg/mL (~106.62 mM)
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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 | 2.8057 mL | 14.0284 mL | 28.0568 mL | |
| 5 mM | 0.5611 mL | 2.8057 mL | 5.6114 mL | |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8057 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.
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