Spiradoline mesylate  (Synonyms: U-62066 mesylate)

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^[1][2].

Ki: 8.6 nM (κ-opioid receptor in guinea pig), 252 nM (μ-receptor) and 9400 nM (δ-receptor)^[2]

使用膜片钳法对大鼠离体心肌细胞进行检测，结果表明 Spiradoline mesylate (15-500 μM) 通过阻断心肌组织中的钠通道 (在较高剂量下还会阻断钾电流) 产生抗心律失常作用。因此，Spiradoline mesylate 可降低峰值钠电流，增加瞬时外向钾电流的衰减率，并降低持续性平台钾幅度^[2]。

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

Spiradoline mesylate (U-62066；0.1-0.4 mg/kg；皮下注射；一次；Sprague-Dawley 大鼠) 可以剂量依赖性地减少无压力成年人的社交行为，在测试的最高剂量下产生社交回避，而较年轻的动物显示对 Spiradoline mesylate 的这种社会抑制作用的敏感性降低。在应激动物中，Spiradoline mesylate 的社交抑制作用在所有年龄段均减弱，青少年和青少年对特定剂量的 U-62066 表现出更高的社交偏好^[1]。

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

521.50

C₂₃H₃₄Cl₂N₂O₅S

87173-97-5

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*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.  [Content Brief]

  [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.  [Content Brief]