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CAS No.: 80012-43-7

Epinastine/依匹斯汀 Catalog No. CSN19386

Synonyms: WAL801;brand names Alesion;Elestat

Epinastine is mast cell stabilizer and antihistamine that is used to treat allergic conjunctivitis.

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技术信息

生物活性

描述Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs^[3]. Epinastine is able to displace specific [3H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with Ki of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain. Epinastine could serve as a highly specific antagonist of octopamine receptors that enables physiological dissection of octopaminergic neurotransmission within the nervous system of insects^[4]. Epinastine was similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. The drug was effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P. No significant changes were observed in phosphodiesterase activity in rat peritoneal mast cells treated with epinastine, while adenylate cyclase activity was augmented by epinastine^[5]. Epinastine shows a dose- and time-dependent suppressive effect on IL-8, one of the chemokines for eosinophils, released from eosinophils isolated from atopic diseases. Epinastine might prevent the autocrine cycle for recruitment of human eosinophils by inhibiting IL-8 release from these cells^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01569191	Hypersensitivity	Phase 4	Completed	-	United Kingdom ... more >> National Pollen and Aerobiology Unit Worcester, United Kingdom, WR2 6AJ Collapse <<
NCT01363700	Allergic Conjunctivitis	Phase 3	Completed	-	Japan ... more >> Santen study sites Osaka, Japan Collapse <<
NCT01363700	-	-	Completed	-	-

更多
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0111 mL
- 20.0553 mL
- 40.1106 mL
- 5 mM
- 0.8022 mL
- 4.0111 mL
- 8.0221 mL
- 10 mM
- 0.4011 mL
- 2.0055 mL
- 4.0111 mL

技术信息

CAS号

80012-43-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H15N3

运输

蓝冰

分子量

249.31

别名

WAL801;brand names Alesion;Elestat;Purivist;Relestat;依匹斯汀

溶解度

DMSO	48.0 mg/mL (192.5 mM)
Water	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01569191	Hypersensitivity	Phase 4	Completed	-	United Kingdom ... more >> National Pollen and Aerobiology Unit Worcester, United Kingdom, WR2 6AJ Collapse <<
NCT01363700	Allergic Conjunctivitis	Phase 3	Completed	-	Japan ... more >> Santen study sites Osaka, Japan Collapse <<
NCT01363700	-	-	Completed	-	-
NCT00534794	Allergic Conjunctivitis	Phase 4	Completed	-	United States, Massachusetts ... more >> Ophthalmic Consultants of Boston Boston, Massachusetts, United States, 02114 Collapse <<
NCT00489398	Allergic Conjunctivitis	Phase 4	Withdrawn(Protocol changes)	December 2008	-
NCT01382654	Allergic Rhinitis	Phase 2	Completed	-	-
NCT01569191	-	-	Completed	-	-
NCT02182544	Rhinitis, Allergic, Perennial	Phase 3	Completed	-	-
NCT00534794	-	-	Completed	-	-
NCT02260050	Healthy	Phase 1	Completed	-	-
NCT02182557	Dermatitis, Atopic	Phase 3	Completed	-	-
NCT02251613	-	-	Completed	-	-
NCT02251613	Allergic Conjunctivitis	Phase 4	Completed	-	-
NCT00407927	Seasonal Allergic Rhinitis	Phase 2	Completed	-	United States, Texas ... more >> Allergy & Asthma Associates Austin, Texas, United States, 78731 Lovelace Scientific Resources, Inc. Austin, Texas, United States, 78759 Kerrville Research Associates Kerrville, Texas, United States, 78028 Central Texas Health Research New Braunfels, Texas, United States, 78130 Biogenics Research Institute San Antonio, Texas, United States, 78229 Sylvana Research Associates San Antonio, Texas, United States, 78229 Allergy Asthma Research Institute Waco, Texas, United States, 76712 Collapse <<
NCT00564421	Seasonal Allergic Rhinitis	Phase 3	Completed	-	-
NCT02182570	Dermatitis, Atopic	Phase 3	Completed	-	-
NCT02238249	-	-	Completed	-	-
NCT02238223	-	-	Completed	-	-
NCT02182518	Rhinitis, Allergic, Perennial	Phase 3	Completed	-	-
NCT02260037	Healthy	Phase 1	Completed	-	-
NCT02260063	Healthy	Phase 1	Completed	-	-
NCT02238236	-	-	Completed	-	-
NCT02182531	Healthy	Phase 1	Completed	-	-

Epinastine/依匹斯汀 Catalog No. CSN19386

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