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| Targets |
Naphazoline nitrate targets α-adrenergic receptors. It is an α-adrenergic receptor agonist. By stimulating adrenergic receptors, it produces vasoconstriction and reduces vascular hyperpermeability. The compound reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6). It produces inotropic effects via α-adrenoceptor stimulation. Naphazoline nitrate is a sympathomimetic agent.
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| ln Vitro |
In vitro, Naphazoline nitrate is an α-adrenergic receptor agonist. It reduces vascular hyperpermeability and promotes vasoconstriction. It reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6). The compound produces inotropic effects via α-adrenoceptor stimulation. Detailed in vitro data are available in the primary literature. Naphazoline nitrate is a well-characterized α-adrenergic agonist.
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| ln Vivo |
By influencing inflammation, NGF, and VEGF Mouse conjunctivitis, naphazine nitrate (0.2 mg/kg, 10 µl per eye; IP once) decreases conjunctival vascular hyperpermeability in mice caused by histamines or antigens[1].
In vivo, Naphazoline nitrate is used as a decongestant in eye drops and nasal sprays. It constricts blood vessels, reducing inflammation and swelling. The compound has been studied for the treatment of seasonal allergy rhinitis. It has also been investigated as a radioprotector for mice treated with ionizing radiation. Naphazoline nitrate is a clinically used topical decongestant. |
| Enzyme Assay |
In vitro receptor binding assays for Naphazoline nitrate typically use membrane preparations from cells expressing α₁- or α₂-adrenergic receptors. Radioligand binding is performed using [³H]-prazosin (α₁) or [³H]-clonidine (α₂) as tracers. Membranes are incubated with radioligand and varying concentrations of Naphazoline nitrate in assay buffer at room temperature for 60-90 minutes. Nonspecific binding is determined using excess phentolamine. Bound radioactivity is measured by filtration and scintillation counting. Ki values are calculated from competition curves. Functional assays measure receptor-mediated calcium mobilization.
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| Cell Assay |
For cell-based assays, cells expressing α-adrenergic receptors are cultured in appropriate medium. Cells are seeded in 96-well plates and loaded with calcium-sensitive dye. Cells are treated with Naphazoline nitrate at various concentrations (0.001-100 μM) and calcium flux is measured. IC₅₀ and EC₅₀ values are calculated from dose-response curves. Cell viability is assessed by standard assays. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
Animal/Disease Models: Female wild-type balb/c (Bagg ALBino) mouse (4-5 weeks, 18±2g, n=8/group, using histamine or antigen (ovalbumin) to establish allergic conjunctivitis mouse model) [1]
Doses: 0.2mg/mL, 10 µl per eye Route of Administration: intraperitoneal (ip) injection, once Experimental Results: Dramatically inhibited conjunctival dye leakage in mice with histamine- or antigen-induced conjunctival vascular hyperpermeability. Reduces inflammatory responses and levels of IL-1β, IL-6, IFN-γ, and IL-4. Reduces the levels of IgE, GMCSF, NGF and VEGF in mice with antigen-induced conjunctival vascular hyperpermeability. In vivo, Naphazoline nitrate is typically administered topically as eye drops or nasal spray. For animal studies, the compound is applied topically at various concentrations (e.g., 0.2 mg/kg, 10 μl per eye). Endpoints include vasoconstriction, reduced congestion, and reduced inflammation. For radioprotection studies, the compound is administered to mice before ionizing radiation exposure. All procedures follow institutional guidelines. |
| ADME/Pharmacokinetics |
Naphazoline nitrate (MW 273.29, C₁₄H₁₅N₃O₃) is an α-adrenergic receptor agonist. It is a white or almost white crystalline powder soluble 1 in 36 water. The compound is used as a topical decongestant. Detailed pharmacokinetic parameters are available from pharmacological literature. It is a clinically used pharmaceutical agent.
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| Toxicity/Toxicokinetics |
Naphazoline nitrate is a clinically used decongestant with an established safety profile. Common side effects include local irritation. It is available as an over-the-counter pharmaceutical product. The compound has been studied for radioprotective effects in mice. Standard precautions for topical decongestant use apply.
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| References |
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| Additional Infomation |
Naphazoline nitrate belongs to the naphthalene family of compounds. It is an adrenergic vasoconstrictor used as a decongestant.
Naphazoline nitrate is a clinically used topical decongestant for the treatment of rhinitis and conjunctivitis. It is the nitrate salt form of naphazoline, an α-adrenergic receptor agonist. It reduces vascular hyperpermeability and promotes vasoconstriction. It is available as a pharmaceutical product and from chemical suppliers for research purposes. Its mechanism involves α-adrenergic receptor agonism. |
| Molecular Formula |
C14H15N3O3
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|---|---|
| Molecular Weight |
273.29
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| Exact Mass |
273.111
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| CAS # |
5144-52-5
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| Related CAS # |
Naphazoline hydrochloride;550-99-2;Naphazoline;835-31-4
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| PubChem CID |
82332
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| Appearance |
White to off-white solid powder
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| Boiling Point |
440.5ºC at 760mmHg
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| Melting Point |
167-170 °C
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| Flash Point |
220.2ºC
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| LogP |
2.323
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
297
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZAHXYMFVNNUHCP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14N2.HNO3/c1-2-7-13-11(4-1)5-3-6-12(13)10-14-15-8-9-16-14;2-1(3)4/h1-7H,8-10H2,(H,15,16);(H,2,3,4)
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| Chemical Name |
2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole;nitric acid
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| Synonyms |
Naphazoline nitrate Clera Benil
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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) |
DMSO : ~100 mg/mL (~365.91 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6591 mL | 18.2956 mL | 36.5912 mL | |
| 5 mM | 0.7318 mL | 3.6591 mL | 7.3182 mL | |
| 10 mM | 0.3659 mL | 1.8296 mL | 3.6591 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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