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• 產(chǎn)品描述： JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2?nM.

• 靶點(diǎn)： Ki: 8.2?nM (ORL1);OpioidReceptor

• 體內(nèi)研究：
  JTC-801 (≥0.01?mg/kg, i.v. or 1?mg/kg, p.o.) antagonizes the nociceptin-induced allodynia in mice. In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL) to exposed heat stimulus with minimum effective doses (MED) of 0.01?mg/kg by i.v. or 1?mg/kg by p.o. In the rat formalin test, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01?mg/kg by i.v. administration or 1?mg/kg by p.o. administration. This anti-nociceptive action of JTC-801 is not inhibited by naloxone (10?mg/kg, s.c.). JTC-801 antagonizes the ORL1 receptor response, and has efficacious and potent anti-nociceptive effects in acute pain animal models not only by intravenous injection but also oral administration. JTC-801 (0.3 mg/kg) decreases allodynia induced by the intrathecal injection of nociceptin in mice. JTC-801 (6 mg/kg i.p., once daily) reverses SPS-induced mechanical allodynia, thermal hyperalgesia, anxiety-like behaviour and hypocortisolism. JTC-801 treatment also reverses NOP receptor protein and mRNA up-regulation in amygdala and PAG. JTC-801 blocks elevated N/OFQ levels in serum, CSF, PAG and hippocampus at day 21 of SPS. JTC-801 (0.05-5 mg/kg, i.p.) supresses the the analgesic effect of N2O in 129Sv mice by the writhing test and tail flick test[

• 參考文獻(xiàn)：
  1. Yamada H, et al. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. Br J Pharmacol, 2002, 135(2), 323-332. 2. Koyama T, et al. Nociceptin receptor antagonist JTC-801 inhibits nitrous oxide-induced analgesia in mice. J Anesth. 2009;23(2):301-3. 3. Shinkai H, et al. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J Med Chem, 2000, 43(24), 4667-4677. 4. Zhang Y, et al. Nociceptin/orphanin FQ peptide receptor antagonist JTC-801 reverses pain and anxiety symptoms in a rat model of post-traumatic stress disorder. Br J Pharmacol. 2015 Jan;172(2):571-82.

• 溶解性： Soluble  in  DMSO、H2O

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.232 ml	11.162 ml	22.323 ml
  5 mM	0.446 ml	2.232 ml	4.465 ml
  10 mM	0.223 ml	1.116 ml	2.232 ml
  50 mM	0.045 ml	0.223 ml	0.446 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *