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Astemizole

CAS No. : 68844-77-9

MCE 国际站：Astemizole

产品活性：Astemizole (R 43512) 是一个长效的二代抗组胺活性分子，是常用的抗过敏活性分子，是组胺 H1 受体 (histamine H1-receptor) 的拮抗剂，IC₅₀ 值为 4 nM。Astemizole 同时还具有hERG K⁺ 通道的阻断活性，IC₅₀ 值为 0.9 nM。Astemizole 还具有抗胆碱能和止痒作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation  |  Membrane Transporter/Ion Channel

作用靶点：Histamine Receptor  |  Potassium Channel

In Vivo: Astemizole (p.o., 10 and 30 mg/kg) and (i.v., 1 and 3 mg/kg) has no effect on respiratory rate, heart rate and blood pressure, and even at high doses of 30 mg/kg and 3 mg/kg, also has no effect on body temperature and exercise capacity in male common marmosets. But Astemizole can prolong the QT interval and induce premature ventricular contractions at 30 mg/kg (po) and 1 mg/kg (iv).
Astemizole (p.o., 3 and 30 mg/kg) shows that the pre-drug control values (C) of the idioventricular rate, QT interval and QTcF are 31 beats/min, 319 ms and 256 at dose of 3 mg/kg, while those are 31 beats/min, 331 ms and 270 at dose of 30 mg/kg, respectively in mice. Moreover, Astemizole at a dose of 30 mg/kg (po) may cause tip-twisting ventricular tachycardia by inhibiting hERG K⁺ channels.

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