Absorption, Distribution and Excretion
There is currently no information available regarding the pharmacokinetics of xylometazoline. (Repeated 5 times) Metabolism/Metabolites There is currently no information available regarding the pharmacokinetics of xylometazoline. Biological Half-Life There is currently no information available regarding the pharmacokinetics of xylometazoline.

Protein Binding
Currently, there is no information regarding the pharmacokinetics of xylometazoline.

Xylometazoline is an alkylbenzene. Xylometazoline is an imidazoline derivative with sympathomimetic and nasal decongestant effects. Xylometazoline exerts its effect by binding to α-adrenergic receptors, causing vasoconstriction in the nasal cavity. Xylometazoline is sold as an over-the-counter (OTC) nasal spray or drops for temporary relief of nasal congestion caused by colds, hay fever, or other respiratory allergies. In some countries, it is used in combination with ipratropium bromide, domiphene, or dextropanol in combination formulations. See also: Xylometazoline hydrochloride (in saline form). Indications: Xylometazoline is indicated for the temporary relief of nasal congestion caused by colds, hay fever, or other respiratory allergies. Mechanism of Action: Nasal congestion is caused by a variety of factors, such as sinusitis, allergic rhinitis, or non-allergic rhinitis, leading to congestion of the nasal mucosa's venous sinuses. Activation of α-adrenergic receptors causes vasoconstriction in the nasal mucosa, thereby restoring airflow into the nasal cavity. α1A and α2B adrenergic receptors are most abundantly expressed in the human nasal mucosa and may play a crucial role in nasal mucosal vasoconstriction. Xylometazoline is a selective agonist of α2B adrenergic receptors and has affinity for α1A, α2A, α2C, α1B, and α1D adrenergic receptors. Xylometazoline reduces nasal resistance during inspiration and expiration and increases nasal airflow. Compared to another imidazoline nasal decongestant, oxymetazoline, xylometazoline has a faster onset of action, but a similar duration of action. In one study, patients with nasal congestion reported relief from ear pain and sore throat in addition to nasal congestion relief. It is speculated that oxymetazoline exerts this effect by inducing vasoconstriction in the nasal mucosa containing venous sinuses. After nasal congestion relief, patients can breathe normally through their nose, thereby alleviating sore throat caused by mouth breathing due to dryness and irritation.

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Pharmacodynamics
Xylometazoline is a sympathomimetic drug that causes vasoconstriction in the nasal mucosa. In a study of patients with nasal congestion associated with the common cold, the median onset time for subjective relief of nasal congestion was approximately 1.7 minutes, with a peak time of 30 minutes. Previous studies have reported rebound swelling, rebound nasal congestion, drug-induced rhinitis, and a shortened duration of decongestion after long-term use of xylometazoline in healthy volunteers, suggesting that short-term use of this drug is most effective. An early in vitro study showed that xylometazoline has antioxidant activity, inhibiting microsomal lipid peroxidation and scavenging hydroxyl radicals. This suggests that xylometazoline has a certain protective effect against oxidants, which play a role in tissue damage caused by inflammation.

C16H24N2

244.37

244.194

526-36-3

Xylometazoline hydrochloride;1218-35-5

5709

Typically exists as solid at room temperature

1g/cm3

394.2ºC at 760mmHg

317-329
131 - 133 °C

192.2ºC

2.909

1

1

3

18

302

0

CC1=C(CC2=NCCN2)C(=CC(=C1)C(C)(C)C)C

HUCJFAOMUPXHDK-UHFFFAOYSA-N

InChI=1S/C16H24N2/c1-11-8-13(16(3,4)5)9-12(2)14(11)10-15-17-6-7-18-15/h8-9H,6-7,10H2,1-5H3,(H,17,18)

2-[(4-tert-butyl-2,6-dimethylphenyl)methyl]-4,5-dihydro-1H-imidazole

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)