| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 500mg |
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| 1g |
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Naphazoline (Naphcon-a, AK-Con) is an imidazoline-based ocular vasoconstrictor and sympathomimetic amine, acting as an α-adrenergic receptor agonist and used as a nasal decongestant.
| ln Vivo |
Through effects on inflammation, NGF, and VEGF, napazoline (0.2 mg/kg, 10 µl per eye; IP, once) decreases conjunctivitis and conjunctival vascular hyperpermeability in mice produced by histamine or antigen [1].
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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. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Absorption data for naphazoline are scarce but imidazoline compounds in general are weakly basic and lipophilic, with high bioavailability from the gastrointestinal tract. Imidazoline compounds undergo some hepatic metabolism but a large fraction of the dose may be excreted unchanged in the urine. Urinary excretion is higher with more acidic urine. Distribution data for naphazoline are scarce but imidazoline compounds are distributed throughout the body, and can cross the blood-brain barrier. Clearance data for naphazoline is unavailable. Metabolism / Metabolites Metabolism data for naphazoline are scarce. Imidazoline compounds undergo some hepatic metabolism but a large fraction of the dose may be excreted unchanged in the urine. Biological Half-Life Half life has not been determined but effects last for 4 to 8 hours. Other imidazoline compounds have half lives varying from 2 to 12 hours. |
| Toxicity/Toxicokinetics |
Protein Binding
Protein binding data for naphazoline is unavailable. |
| References |
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| Additional Infomation |
2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole is a member of naphthalenes.
Naphazoline is a rapid acting imidazoline sympathomimetic vasoconstrictor of ocular or nasal artierioles. It acts to decrease congestion and is found in many over the counter (OTC) eye drops and nasal preparations. Naphazoline was first developed in 1942 as a nasal formulation for congestion. Naphazoline is an imidazole derivative and a direct-acting sympathomimetic amine with vasoconstrictive activity. Upon ocular administration, naphazoline exerts its effect by acting on alpha-adrenergic receptors in the arterioles of the conjunctiva to produce vasoconstriction, resulting in decreased conjunctival congestion and diminished itching, irritation and redness. An adrenergic vasoconstrictor agent used as a decongestant. See also: Naphazoline Hydrochloride (has salt form). Drug Indication Naphazoline is indicated for use as OTC eyedrops for ocular vasoconstriction or as a nasal preparation for nasal congestion. Mechanism of Action Naphazoline is a vasoconstrictor that functions by stimulating alpha adrenergic receptors in arterioles leading to decreased congestion at the site of administration. Naphazoline causes the release of norepinephrine in sympathetic nerves. Norepinephrine binds to alpha adrenergic receptors and causes vasoconstriction. Naphazoline is also a mild beta adrenergic receptor agonist, which can cause rebound vasodilation after the alpha adrenergic stimulation has ended. Naphazoline's release of norepinephrine also triggers a negative feedback loop which decreases production of norepinephrine, which can lead to rhinitis medicamentosa after long term use when naphazoline is stopped. Pharmacodynamics Naphazoline is a sympathomimetic alpha adrenergic agonist that acts to vasoconstrict nasal or ocular arterioles, resulting in reduced congestion at the site of administration. |
| Molecular Formula |
C14H14N2
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|---|---|
| Molecular Weight |
210.27436
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| Exact Mass |
210.115
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| CAS # |
835-31-4
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| Related CAS # |
Naphazoline nitrate;5144-52-5;Naphazoline hydrochloride;550-99-2;Naphazoline-d4 hydrochloride
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| PubChem CID |
4436
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
440.5±24.0 °C at 760 mmHg
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| Melting Point |
254ºC
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| Flash Point |
220.2±22.9 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.640
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| LogP |
3.88
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
272
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1CCNC=1CC1C2C(=CC=CC=2)C=CC=1
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| InChi Key |
CNIIGCLFLJGOGP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14N2/c1-2-7-13-11(4-1)5-3-6-12(13)10-14-15-8-9-16-14/h1-7H,8-10H2,(H,15,16)
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| Chemical Name |
2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole
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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 | 4.7558 mL | 23.7790 mL | 47.5579 mL | |
| 5 mM | 0.9512 mL | 4.7558 mL | 9.5116 mL | |
| 10 mM | 0.4756 mL | 2.3779 mL | 4.7558 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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