Epinastine

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Chemical Structure| 80012-43-7 同义名 : WAL801
CAS号 : 80012-43-7
货号 : A540909
分子式 : C16H15N3
纯度 : 99%+
分子量 : 249.31
MDL号 : MFCD00865648
存储条件：

Pure form Keep in dark place, inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.01mL

0.80mL

0.40mL

20.06mL

4.01mL

2.01mL

40.11mL

8.02mL

4.01mL
参考文献

[1]Fugner A, Bechtel WD, et al. In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung. 1988 Oct;38(10):1446-53.

[2]Roeder T, Degen J, et al. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol. 1998 May 22;349(2-3):171-7.

[3]Fügner A, Bechtel WD, Kuhn FJ, Mierau J. In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung. 1988 Oct;38(10):1446-53

[4]Roeder T, Degen J, Gewecke M. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol. 1998 May 22;349(2-3):171-7

[5]Kamei C, Akagi M, Mio M, Kitazumi K, Izushi K, Masaki S, Tasaka K. 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):191-205

[6]Kohyama T, Takizawa H, Akiyama N, Sato M, Kawasaki S, Ito K. A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun. 1997 Jan 3;230(1):125-8