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Spiradoline mesylate

CAS No. : 87173-97-5

MCE 站：Spiradoline mesylate

产品活性：Spiradoline mesylate (U-62066 mesylate) 是一种芳基乙酰胺，是一种选择性 kappa 阿片受体 (κ-opioid receptor, KOR) 激动剂，在豚鼠中的 K_i 为 8.6 nM。Spiradoline mesylate 对 μ 和 δ 受体的 K_i 值分别为 252 nM 和 9400 nM。Spiradoline mesylate 具有强效的利尿，止痛，抗心律失常，镇咳，神经保护作用，并易于穿过血脑屏障。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

In Vitro: Using the patch-clamp method in isolated rat cardiac myocytes, indicated that Spiradoline mesylate (15 to 500 μM) produces its antiarrythmic effect via blockade of sodium channels (and at the higher doses also of potassium currents) in myocardial tissue. Thus, Spiradoline mesylate reduces the peak sodium current, increased the decay rate of the transient outward potassium current, and reduced the sustained plateau potassium amplitude.

In Vivo: Spiradoline mesylate (U-62066; 0.1-0.4 mg/kg; subcutaneous injection; once; Sprague-Dawley rats) treatment dose-dependently reduces social behaviors in non-stressed adults, producing social avoidance at the highest dose tested, while younger animals displays reduced sensitivity to this socially suppressing effect of Spiradoline mesylate. In stressed animals, the socially suppressing effects of the Spiradoline mesylate are blunted at all ages, with juveniles and adolescents exhibiting increased social preference in response to certain doses of U-62066.

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