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]

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^[2].

MedChemExpress (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; 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^[1].

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

521.50

C₂₃H₃₄Cl₂N₂O₅S

87173-97-5

Solid

White to off-white

ClC1=C(C=CC(CC(N([C@H]2CC[C@@]3(C[C@@H]2N4CCCC4)OCCC3)C)=O)=C1)Cl.CS(O)(=O)=O

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]