| 产品描述： | ARN272 is a FAAH-like anandamide transporter (FLAT) inhibitor (IC50: 1.8 μM). |
| 靶点： |
FAAH |
| 体外研究： |
FLAT inhibition by ARN272 appeared to be selective because the compound had little or no inhibitory activity on several endocannabinoid-metabolizing enzymes. Moreover, ARN272 produced only weak and incomplete inhibition of rat brain FAAH activity and was not significantly hydrolyzed after incubation with recombinant human FAAH-1 (≈5% hydrolysis after 24h at 37°C) |
| 体内研究： |
Administration of ARN272 (1 mg/kg, intraperitoneal, i.p.) in mice increased plasma levels of anandamide without changing the levels of 2-AG, OEA or PEA. The inhibitory effects of ARN272 on anandamide internalization in vitro and anandamide deactivation in vivo, along with the diminished anandamide accumulation observed in faah-1/ mice. The systemic administration of ARN272 produced a dose-dependent suppression of nausea-induced conditioned gaping in rats and produced a dose-dependent reduction of vomiting in shrews. The systemic co-administration of SR141716 with ARN272 (at 3.0mg/kg) in rats produced a complete reversal of ARN272-suppressed gaping at 1.0mg/kg. SR141716 alone did not differ from the vehicle solution |
| 动物实验： |
All rats were surgically implanted with intra-oral cannula under isoflurane anaesthesia. Following recovery from surgery (3 days), rats received a single adaptation trial to habituate them to the chamber and the infusion procedure. During the adaptation trial, rats were placed individually in the TR chamber and received a 2?min intra-oral infusion of water (reverse osmosis water infused at 1mL/min). On the following day, rats received the first of two conditioning trials (separated by 72h). On each conditioning trial, rats received a pretreatment injection of ARN272 or VEH 120?min prior to the conditioning trials. During conditioning trails, rats were intra-orally infused with a saccharin solution (0.1%) for 2?min (1mL/min) and orofacial and somatic reactions were recorded on video. Immediately following the saccharin infusion, the rats were injected with LiCl (0.15M) or saline, and then returned to their home cage. Two additional groups were added (after ARN272 at 3.0mg·kg1 attenuated gaping) where pretreatm |
| 参考文献： |
1. Fu J, et al. A catalytically silent FAAH-1 variant drives anandamide transport in neurons. Nat Neurosci. 2011 Nov 20;15(1):64-9. 2. O'Brien LD, et al. Anandamide transport inhibition by ARN272 attenuates nausea-induced behaviour in rats, and vomiting in shrews (Suncus murinus). Br J Pharmacol. 2013 Nov;170(5):1130-6. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.312 ml |
11.561 ml |
23.123 ml |
| 5 mM |
0.462 ml |
2.312 ml |
4.625 ml |
| 10 mM |
0.231 ml |
1.156 ml |
2.312 ml |
| 50 mM |
0.046 ml |
0.231 ml |
0.462 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京