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(+)-U-50488 hydrochloride (Synonyms: (+)-Trans-(1R,2R)-U-50488 hydrochloride)

カタログ番号GC12688

選択的κ-オピオイド作動薬

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(+)-U-50488 hydrochloride 化学構造

Cas No.: 114528-81-3

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10mg
$284.00
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50mg
$1,173.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

(+)-U-50488塩酸塩は、κオピオイド受容体に対する選択的アゴニストです[1]。

κ-オピオイド受容体(KOR)は、オピオイドペプチドダイノルフィンのための一種のオピオイド受容体であり、中毒を制御します。また、KORはストレス、不安、無楽感状態、うつ病および薬物探索行動の増加に重要な役割を果たしています。

(+)-U-50488塩酸塩は、選択的なKORアゴニストです[1]。孤立したラットDRGニューロンでは、U-50488(0.3?40μM)が電圧非依存性Ca2 +チャネル電流を阻害しました。KORを発現しないHeLa細胞では、U-50488(20μM)がCa2 +チャネルをブロックしました[2]。

ライサス猿では、U-50488は強力な抗痛覚作用を示し、利尿作用を引き起こしました[1]。 U-50488はウサギの精管に電気的に誘発された収縮をIC50値26.5 nMで増強しました。マウスでは、U-50488はED50値15.3 mg / kgで運動機能を障害し、自発活動を減少させました[3]。成体ラットでは、U-50488は自己刺激反応を維持するために必要な閾値を増加させる効果がありますが、うつ状態のような影響があります。一方で、オスは閾値上昇効果に対して女性よりも有意に敏感でした[4]。

References:
[1].  Tang AH, Collins RJ. Behavioral effects of a novel kappa opioid analgesic, U-50488, in rats and rhesus monkeys. Psychopharmacology (Berl), 1985, 85(3): 309-314.
[2].  Hassan B, Ruiz-Velasco V. The κ-opioid receptor agonist U-50488 blocks Ca2+ channels in a voltage- and G protein-independent manner in sensory neurons. Reg Anesth Pain Med, 2013, 38(1): 21-27.
[3].  Lu SN, Ma SC, Zhang KG, et al. Comparison of pharmacological profile of selective kappa-opioid agonist K-II and U-50488. Yao Xue Xue Bao, 1991, 26(3): 171-174.
[4].  Russell SE, Rachlin AB, Smith KL, et al. Sex differences in sensitivity to the depressive-like effects of the kappa opioid receptor agonist U-50488 in rats. Biol Psychiatry, 2014, 76(3): 213-222.

Chemical Properties

Cas No. 114528-81-3 SDF
同義語 (+)-Trans-(1R,2R)-U-50488 hydrochloride
Chemical Name 2-(3,4-dichlorophenyl)-N-methyl-N-((1R,2R)-2-(pyrrolidin-1-yl)cyclohexyl)acetamide hydrochloride
Canonical SMILES CN(C(CC1=CC(Cl)=C(Cl)C=C1)=O)[C@]2([H])CCCC[C@@]2([H])N3CCCC3.Cl
Formula C19H26Cl2N2O.HCl M.Wt 405.79
溶解度 <40.58mg/ml in DMSO; <40.58mg/ml in Water Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4643 mL 12.3216 mL 24.6433 mL
5 mM 0.4929 mL 2.4643 mL 4.9287 mL
10 mM 0.2464 mL 1.2322 mL 2.4643 mL
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