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Epinastine

CAS No. : 80012-43-7

MCE 国际站：Epinastine

产品活性：Epinastine (WAL801) 是一种抗组胺剂和肥大细胞稳定剂。Epinastine 是一种有效的，选择性的，口服活性的组胺 H1 受体 (histamine H1 receptor) 拮抗剂。Epinastine 还抑制 IL-8 释放并具有抗过敏作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: 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 K_i of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain.
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.
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.

In Vivo: 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.

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