| 产品描述: | RF9 is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively |
| 靶点: |
hNPFF1R:58 nM (Ki);hNPFF2R:75 nM (Ki);NeuropeptideYReceptor |
| 体内研究: |
RF9 (0.1 mg/kg, s.c. ) with heroin coadministration prevents heroin-induced delayed hyperalgesia and tolerance. RF9 (10 μg) infused alone does not result in a significant alteration of MAP or heart rate. Conversely, MAP and heart rate increases evoked by NPFF are significantly blocked when NPFF is applied in conjunction with RF9. Animal Model: Rats. Dosage: 0.1 mg/kg. Administration: S.C. 30 min before 0.3 mg/kg heroin or saline on basal nociceptive threshold in rats. Result: Opposed to delaye heroin-induced hyperalgesia and associated tolerance. |
| 参考文献: |
1. Simonin F, et al. RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. Proc Natl Acad Sci U S A. 2006 Jan 10;103(2):466-71. 2. Ting Zhang, et al. Discovery of Two Novel Branched Peptidomimetics Containing endomorphin-2 and RF9 Pharmacophores: Synthesis and Neuropharmacological Evaluation. Bioorg Med Chem. 2019 Feb 15;27(4):630-643. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.676 ml |
8.38 ml |
16.76 ml |
| 5 mM |
0.335 ml |
1.676 ml |
3.352 ml |
| 10 mM |
0.168 ml |
0.838 ml |
1.676 ml |
| 50 mM |
0.034 ml |
0.168 ml |
0.335 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。 |