產品屬性：
產品名稱 | BW 373U86 |
規格 | 10mg |
貨號 | EY-01Y13313 |
Cas No.: 155836-50-3
別名: N/A
化學名: 4-((R)-((2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl)-N,N-diethylbenzamide
分子式: C27H37N3O2
分子量: 435.61
溶解度: <43.56mg/ml in 1eq. HCl
儲存條件: Store at 4°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
Ki: 1.8, 15, 85 and 34 nM for delta, mu, epsilon and kappa receptorOpioid receptors are heterogeneous and at least four types, mu,.delta, kappa and epsilon, are known to exist. Currently, all clinically used opiates act through the mu receptor to induce analgesia; however, they also induce unwanted side effects such as respiratory depression, dependence, constipation and muscle rigidity.BW 373U86 is a novel, potent and selective nonpeptidic delta opioid receptor agonist. In vitro: BW 373U86 was a potent delta receptor-selective ligand in receptor binding assays. The Ki values were 1 .8 ± 0.4, 15 ± 3, 85 ± 4 and 34 ± 3 nM for delta, mu, epsilon and kappa receptor binding sites, respectively. BW 373U86 inhibited electncally evoked muscle contraction of mouse vas deferens with an ED50 value of 0.2 ± 0.06 nM [1]. In vivo: BW 373U86 inhibited the acoustic startle reflex after subcutaneous administration from 0.2- to 2-mg/kg doses in rats, and this inhibition was blocked by naltnndole. BW 373U86 also induced a dose-dependent increase of locomotor activity in rats at similar doses. This effect was inhibited by naltnndole [3]. Clinical trial: Up to now, BW 373U86 is still in the preclinical development stage.
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