Epinastine 能够在低浓度下取代蝗虫神经组织中的特异性 [3H]NC-5Z 结合。 Epinastine 与蜜蜂神经元章鱼胺受体结合，Ki 为 1.1 nM。 Epinastine 拮抗章鱼胺诱导的昆虫大脑中 cAMP 的形成[2]。 Epinastine 可抑制由抗原抗体反应和化合物 48/80 诱导的大鼠腹膜肥大细胞释放组胺。 Epinastine 同样有效地抑制化合物 48/80 诱导的组胺释放，不仅从分离的大鼠腹膜肥大细胞中释放，而且从大鼠肠系膜碎片中释放。 Epinastine 不仅能有效抑制主动致敏豚鼠肺肥大细胞中 Ca2+ 的摄取，还能有效抑制暴露于化合物 48/80 和 P 物质的大鼠腹膜肥大细胞的细胞内 Ca2+ 释放 Ca2+ [3]。 Epinastine 对 IL-8 显示出剂量和时间依赖性的抑制作用，IL-8 是嗜酸性粒细胞的趋化因子之一，从特应性疾病中分离的嗜酸性粒细胞中释放出来[4]。

在豚鼠回肠的受体结合研究中，依匹斯汀显示出与 H1 受体的高亲和力。 Epinastine 可抑制组胺引起的大鼠、狗和豚鼠皮肤或肺部反应[1]。

Absorption, Distribution and Excretion
The absolute bioavailability of epinastine is approximately 40%. Epinastine is primarily excreted unchanged. Renal excretion is mainly through active secretion by the renal tubules. 56 L/hr [For patients with allergic conjunctivitis, administer one drop of ELESTAT® eye drops twice daily for 7 days.] Metabolism/Metabolites Primarily excreted unchanged, less than 10% is metabolized. Biological Half-Life 12 hours

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Evidence from 7 subjects suggests that epinastine likely enters breast milk and results in extremely low serum concentrations in infants, making adverse effects on breastfed infants unlikely. In the United States, epinastine is only available as eye drops. Due to limited ocular absorption, no adverse effects of epinastine are expected on breastfed infants. To significantly reduce the amount of medication entering breast milk after using eye drops, press your finger against the tear duct near the corner of your eye for 1 minute or longer, then blot away excess medication with absorbent tissue.
◉ Effects on Breastfed Infants
A study of 7 lactating mothers who took 20 mg of epinastine once daily. No adverse reactions were reported in infants.
◉ Effects on Lactation and Breast Milk
Higher doses of antihistamines can lower basal serum prolactin levels in non-lactating women and early postpartum women. However, pre-treatment with antihistamines by postpartum mothers does not affect suckling-induced prolactin secretion. Prolactin levels in established lactating mothers are unlikely to affect their breastfeeding ability. Low-dose ophthalmic epinastine is unlikely to have the same effect on serum prolactin.

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Protein binding rate
64%

[1]. In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung, 1988. 38(10): p. 1446-53.

[2]. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol, 1998. 349(2-3): p. 171-7.

[3]. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol, 1992. 14(1-2): p. 191-205.

[4]. A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun, 1997. 230(1): p. 125-8.

Epinastine is a benzodiazepine drug with the chemical name 6,11-dihydro-5H-dibenzo[b,e]azazepine, in which the azazepine ring is fused to the e-side of 4,5-dihydro-1H-imidazol-2-amine. It has anti-allergic, histamine antagonist, ophthalmic, and H1 receptor antagonist effects. It belongs to the guanidine and benzodiazepine classes. Epinastine is used to prevent itching caused by allergic conjunctivitis. It has multiple effects, inhibiting allergic reactions in three ways: 1. By stabilizing mast cells and preventing mast cell degranulation, it controls allergic reactions; 2. By preventing histamine from binding to H1 and H2 receptors, it relieves itching and provides long-lasting protection; 3. By preventing the release of pro-inflammatory chemical mediators from blood vessels, it prevents the progression of allergic reactions. Epinastine is an adrenergic receptor agonist and histamine-1 receptor inhibitor. The mechanism of action of epinastine is as an adrenergic agonist and histamine H1 receptor antagonist. Epinastine's physiological action is achieved by reducing histamine release. See also: Epinastine hydrochloride (in salt form). Drug Indications For the prevention of itching caused by allergic conjunctivitis. FDA Label Mechanism of Action Epinastine has multiple mechanisms of action, inhibiting allergic reactions in three ways: 1. By stabilizing mast cells and preventing mast cell degranulation, thus controlling allergic reactions; 2. By preventing histamine from binding to H1 and H2 receptors, thus relieving itching and providing long-lasting protection; 3. By preventing the release of pro-inflammatory chemical mediators from the bloodstream, thus preventing the progression of allergic reactions. Pharmacodynamics Epinastine is an antihistamine that inhibits the release of histamine from mast cells and is used for topical ocular administration. Epinastine is indicated for the prevention of itching caused by allergic conjunctivitis. Epinastine is a locally effective direct H1 receptor antagonist that inhibits the release of histamine from mast cells. Epinastine is selective for histamine H1 receptors and has affinity for histamine H2 receptors. In addition, epinastine also has affinity for α1, α2, and 5-HT2 receptors. Epinastine does not cross the blood-brain barrier, therefore, central nervous system side effects are not expected.

C₁₆H₁₅N₃

249.31

249.127

C, 77.08; H, 6.06; N, 16.85

80012-43-7

Epinastine hydrochloride; 108929-04-0; Epinastine-13C,d3 hydrobromide; 127786-29-2 (HBr)

3241

White to off-white solid powder

1.32 g/cm3

428ºC at 760 mmHg

270ºC

212.7ºC

1.727

2.667

41.62

1

1

0

19

378

0

N1CC2N(C3C(CC4C2=CC=CC=4)=CC=CC=3)C=1N

WHWZLSFABNNENI-UHFFFAOYSA-N

InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18)

2,4-diazatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine

WAL801; WAL 801; WAL-801; Epinastine; brand names Alesion, Elestat, Purivist, Relestat

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： (1). 本产品在运输和储存过程中需避光。  (2). 请将本产品存放在密封且受保护的环境中（例如氮气保护），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)

DMSO: ≥ 50 mg/mL (~200.6 mM)
H2O: < 0.1 mg/mL

配方 1 中的溶解度: ≥ 2.5 mg/mL (10.03 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 (10.03 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 (10.03 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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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。