Spiradoline

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Spiradoline (U 62066) 是一种强效、高选择性 κ-阿片受体激动剂，具有镇痛、利尿和镇咳作用。

Spiradoline (U 62066) is a potent, highly selective κ-opioid agonist that has analgesic diuretic and antitussive effects.Pain Phase 2 Discontinued.

Using the patch-clamp method in isolated rat cardiac myocytes, indicated that Spiradoline (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 reduces the peak sodium current, increased the decay rate of the transient outward potassium current, and reduced the sustained plateau potassium amplitude.

Spiradoline (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. In stressed animals, the socially suppressing effects of the Spiradoline 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.

U 62066

Endocrinology/Hormones

Opioid Receptor

Opioid Receptor

Neurological Disease

Pain

87151-85-7

425.392

C22H30Cl2N2O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (117.54 mM)

CN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N3CCCC3)C(=O)CC4=CC(=C(C=C4)Cl)Cl.CS(=O)(=O)O

2-(3,4-dichlorophenyl)-N-methyl-N-[(5R,7S,8S)-7-pyrrolidin-1-yl-1-oxaspiro[4.5]decan-8-yl]acetamide

(-20℃)

With Ice Pack

≥ 2 years