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。

Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a K i of 8.6 nM in guinea pig. The K i values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier.

Solid

Ki: 8.6 nM (κ-opioid receptor in guinea pig), 252 nM (μ-receptor) and 9400 nM (δ-receptor)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Elena I Varlinskaya, et al. Stress alters social behavior and sensitivity to pharmacological activation of kappa opioid receptors in an age-specific manner in Sprague Dawley rats. Neurobiol Stress. 2018 Sep 11;9:124-132.
[2]. M-L G Wadenberg. A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist. CNS Drug Rev. Summer 2003;9(2):187-98.