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CAS No.: 209808-47-9

AR-M 1000390 HCl Catalog No. CSN23662

Synonyms: AR-M1000390;ARM-390;ARM-390 hydrochloride

AR-M 1000390 HCl is a non-peptidic and low-internalizing δ-selective opioid receptor agonist.

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技术信息

生物活性

描述AR-M 1000390 HCl is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency. AR-M 1000390 (Compound 6a) exhibits the binding affinities (IC50) of 0.87±0.23 nM for the δ opioid receptor and extremely high selectivity over the µ receptor (IC50=3800±172 nM) and the κ receptor (IC50=7470±606 nM)^[1]. AR-M100390 (600 micromol/kg) caused vacuolation in the beta-cell of the rat pancreas that was associated with depletion of insulin and hyperglycemia after 7 days of dosing. The effects of AR-M100390 in rats were reproduced in the rat pancreatic beta-cell line RINm5F, where it inhibited intracellular insulin content and secretion without affecting cell survival. AR-M100390 inhibited KCl-mediated calcium mobilization in RINm5F cells, suggesting that L-type calcium channels found in these cells and in pancreatic beta-cells may partially play a role in the inhibition of insulin secretion by this compound. Therefore, the in vitro and in vivo studies suggest that inhibition of insulin by AR-M100390 is due to a combination of inhibition of insulin synthesis and/or release^[2]. An initial treatment with the high (SNC80) or low (AR-M100390) internalizing agonist equally reduced CFA-induced inflammatory pain. Delta agonists retain full analgesic efficacy when receptors remain on the cell surface. In contrast, delta agonist-induced analgesia is abolished following receptor internalization, and complete behavioral desensitization is observed^[3].
参考文献

[1] Wei ZY, Brown W, Takasaki B, Plobeck N, Delorme D, Zhou F, Yang H, Jones P, Gawell L, Gagnon H, Schmidt R, Yue SY, Walpole C, Payza K, St-Onge S, Labarre M, Godbout C, Jakob A, Butterworth J, Kamassah A, Morin PE, Projean D, Ducharme J, Roberts E. N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues. J Med Chem. 2000 Oct 19;43(21):3895-905
[2] Otieno MA, Bavuso N, Milano J, Foster-Brown L, Bui KH, Li Y, Hudzik T, Wescott D, Louden C, Dyroff M, Pognan F. Mechanistic investigation of N,N-diethyl-4-(phenyl-piperidin-4-ylidenemethyl)-benzamide-induced insulin depletion in the rat and RINm5F cells. Toxicol Sci. 2008 Sep;105(1):221-9
[3] Pradhan AA, Becker JA, Scherrer G, Tryoen-Toth P, Filliol D, Matifas A, Massotte D, Gavériaux-Ruff C, Kieffer BL. In vivo delta opioid receptor internalization controls behavioral effects of agonists. PLoS One. 2009;4(5):e5425

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5978 mL
- 12.9890 mL
- 25.9781 mL
- 5 mM
- 0.5196 mL
- 2.5978 mL
- 5.1956 mL
- 10 mM
- 0.2598 mL
- 1.2989 mL
- 2.5978 mL

技术信息

CAS号

209808-47-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H29ClN2O

运输

蓝冰

分子量

384.94

别名

AR-M1000390;ARM-390;ARM-390 hydrochloride

溶解度

DMSO	490.0 mg/mL (1272.9 mM)
Water	145.0 mg/mL (376.7 mM)

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AR-M 1000390 HCl Catalog No. CSN23662

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