产品
编 号：F592031
分子式：C23H34Cl2N2O5S
分子量：521.5
分子式：C23H34Cl2N2O5S
分子量：521.5
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 87173-97-5
产品详情
生物活性：
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki 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.
体内研究：
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.Animal Model:Juvenile, adolescent and adult Sprague-Dawley male and female rats exposured to repeated restraint
Dosage:0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4?mg/kg
Administration:Subcutaneous injection; once
Result:Dose-dependently reduced social behaviors in non-stressed adults, producing social avoidance at the highest dose tested.
体外研究：
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.
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki 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.
体内研究：
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.Animal Model:Juvenile, adolescent and adult Sprague-Dawley male and female rats exposured to repeated restraint
Dosage:0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4?mg/kg
Administration:Subcutaneous injection; once
Result:Dose-dependently reduced social behaviors in non-stressed adults, producing social avoidance at the highest dose tested.
体外研究：
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.
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