依匹斯汀盐酸盐 T6488

Product Introduction
Bioactivity


英文名: Epinastine hydrochloride

描述: Epinastine hydrochloride (WAL-801CL HCl) 是抗组胺剂和肥大细胞稳定剂，是一种可口服的选择性组胺 H1 受体拮抗剂，可抑制 IL-8 释放，具有抗过敏作用。

体外活性: Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. [1] 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. [2] Epinastine causes an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine is similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Epinastine is 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. [3] 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. [4]

体内活性: Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (174.97 mM)
H2O : 52 mg/mL (182 mM)
Ethanol : 53 mg/mL (185.5 mM)


关键字: antiallergic | inhibit | Epinastine Hydrochloride | Epinastine | WAL801 | WAL 801 | insect | Histamine Receptor | mast | Inhibitor | WAL-801 | Antihistamine | cell | Epinastine hydrochloride | vertebrate | neuronal

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相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Inhibitor Library | Serotonin Receptor-Targeted Compound Library | Anti-Cancer Approved Drug Library

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