Alpha-1A adrenergic receptor ( Ki = 0.05 μM ); Alpha-1B adrenergic receptor ( Ki = 0.30 μM ); Alpha-1D adrenergic receptor ( Ki = 0.15 μM ); Alpha-2A adrenergic receptor ( Ki = 0.88 μM ); Alpha-2B adrenergic receptor ( Ki = 1.7 μM ); Alpha-2C adrenergic receptor ( Ki = 0.19 μM nM )

体外活性：Xylometazoline 是一种 α-肾上腺素受体激动剂，通常用作鼻减充血剂，对 α2B-肾上腺素受体亚型表现出最高效力，EC50 为 99 μM。 Xylometazoline 与肾上腺素受体亚型 α1A、α1B、α1D、α2A、α2B、α2C 结合，IC50 分别为 0.08、0.56、0.45、0.98、1.8、0.22μM。

Absorption, Distribution and Excretion
No information is available on xylometazoline pharmacokinetics.
No information is available on xylometazoline pharmacokinetics.
No information is available on xylometazoline pharmacokinetics.
No information is available on xylometazoline pharmacokinetics.

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Metabolism / Metabolites
No information is available on xylometazoline pharmacokinetics.

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Biological Half-Life
No information is available on xylometazoline pharmacokinetics.

Protein Binding
No information is available on xylometazoline pharmacokinetics.

[1]. Fundam Clin Pharmacol . 2010 Dec;24(6):729-39.

Xylometazoline is an alkylbenzene.
Xylometazoline is an imidazoline derivative with sympathomimetic and nasal decongestant activity. Xylometazoline works by binding to alpha (α)-adrenergic receptors to cause vasoconstriction of nasal blood vessels. Xylometazoline is available in over-the-counter (OTC) nasal sprays or drops to temporarily relieve nasal congestion due to cold, hay fever or other respiratory allergies. In some countries, it is available as combination products with [ipratropium], [domiphen], or [dexpanthenol].
See also: Xylometazoline Hydrochloride (has salt form).

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Drug Indication
Xylometazoline is indicated for the temporary relief of nasal congestion due to cold, hay fever or other respiratory allergies.

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Mechanism of Action
Nasal congestion is caused by various etiologies, such as rhinosinusitis and allergic or non-allergic rhinitis, leading to congestion of the venous sinusoids lining the nasal mucosa. Activation of α-adrenergic receptors leads to vasoconstriction of the blood vessels of the nasal mucosa and resumption of nasal airflow. As the most abundantly expressed in the human nasal mucosa, α_1A- and α_2B-adrenoceptors may play the most important role in vasoconstriction of the human nasal mucosa. Xylometazoline is a more selective agonist at α_2B-adrenoceptors, with affinity at α_1A-, α_2A-, α_2C-, α_1B-, and α_1D-adrenoceptors. Xylometazoline decreases nasal resistance during inspiration and expiration and increases the volume of nasal airflow. Compared to [oxymetazoline], another imidazoline nasal decongestant, xylometazoline had a slightly faster onset of action although they had a similar duration of action. In one study, subjects with nasal congestion reported relief of earache and sore throat in addition to nasal decongestion: it is speculated that oxymetazoline mediates this effect by causing vasoconstriction of the nasal mucosa that contains the venous sinuses and nasal decongestion allows breathing through the nose, providing relief from sore throat caused by mouth breathing that dries and irritates the throat.

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Pharmacodynamics
Xylometazoline is a sympathomimetic agent that causes vasoconstriction of the nasal mucosa. In one study comprising subjects with nasal congestion associated with the common cold, the median time of onset of subjective relief of nasal congestion was about 1.7 minutes and the time of subjective peak relief of nasal congestion was 30 minutes. Previous studies reported rebound swelling, rebound nasal congestion, rhinitis medicamentosa, and shorter duration of decongestant effect from the long-term use of xylometazoline in healthy volunteers, suggesting that the drug is most effective if used temporarily. An early _in vitro_ study demonstrated xylometazoline to exert anti-oxidant actions, where it inhibited microsomal lipid peroxidation and mediated hydroxyl radical scavenging activity. This suggests that xylometazoline has a beneficial effect against oxidants, which play a role in tissue damage in inflammation.

C16H25CLN2

280.84

280.17

C, 68.43; H, 8.97; Cl, 12.62; N, 9.98

1218-35-5

Xylometazoline; 526-36-3

5709

White to off-white crystalline powder

394.2ºC at 760 mmHg

131-133ºC

192.2ºC

4.56E-06mmHg at 25°C

3.711

24.39

1

1

3

18

302

0

Cl[H].N1([H])C([H])([H])C([H])([H])N=C1C([H])([H])C1C(C([H])([H])[H])=C([H])C(=C([H])C=1C([H])([H])[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]

YGWFCQYETHJKNX-UHFFFAOYSA-N

InChI=1S/C16H24N2.ClH/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);1H

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

xylomethazoline; Xylometazoline HCl; Brand name: Decongest; Otrivine; Balkis; Amidrin; Chlorohist-LA; espa-rhin; Gelonasal

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

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

配方 1 中的溶解度: ≥ 2.5 mg/mL (8.90 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (8.90 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (8.90 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 16.67 mg/mL (59.36 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。