876310-60-0
中文名稱
2-ADAMANTANECARBONYL-ARG-PHE-NH2
英文名稱
2-ADAMANTANECARBONYL-ARG-PHE-NH2 TRIFLUOROACETATE
CAS
876310-60-0
分子式
C26H38N6O3
分子量
482.62
MOL 文件
876310-60-0.mol
更新日期
2024/12/16 11:45:51
876310-60-0 結(jié)構(gòu)式
基本信息
中文別名
化合物 T16738神經(jīng)肽FF受體拮抗劑RF9
英文別名
RD9RF 9
RF9 trifluoroacetate salt
1-Adamantanecarbonyl-Arg-Phe-NH2
2-Adamantanecarbonyl-Arg-Phe-NH2
2-ADAMANTANECARBONYL-ARG-PHE-NH2 TRIFLUOROACETATE
1-Adamantanecarbonyl-Arg-Phe-NH2 trifluoroacetate salt
L-Phenylalaninamide, N2-(tricyclo[3.3.1.13,7]dec-1-ylcarbonyl)-L-arginyl-
所屬類別
生物：拮抗劑物理化學(xué)性質(zhì)
密度1.42±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度H2O：可溶，20mg/mL
酸度系數(shù)(pKa)14.53±0.20(Predicted)
形態(tài)固體
顏色白色
常見(jiàn)問(wèn)題列表
生物活性
RF9 是一種有效且有選擇性的神經(jīng)肽 FF 受體 (Neuropeptide FF receptor) 拮抗劑 ，對(duì)于 hNPFF1R 和 hNPFF2R 的 Ki 值分別為 58 和 7 nM。靶點(diǎn)
|
hNPFF1R 58 nM (Ki) |
hNPFF2R 75 nM (Ki) |
體外研究
RF9 (10 μM) pretrement completely blocks NPFF induced neurite outgrowth of Neuro 2A cells.
體內(nèi)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. |