JTC-801 是一种具有选择性的 opioid receptor-like1 (ORL1) receptor 抑制剂，其 K_i 值为 8.2 nM。

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a K i value of 8.2?nM.

Solid

Ki: 8.2?nM (ORL1)

JTC-801 inhibits [H]-nociceptin binding to ORL1 receptor expressed in HeLa cells with an IC50 value of 94±8.6 nm at a [H]-nociceptin concentration of 50?pM. JTC-801 weakly inhibits the binding of the ligands to human δ receptor (IC50>10?μM), κ receptor (IC50>10?μM), and μ receptor (IC50=325?nM). In rat cerebrocortical membrane, JTC-801 inhibits ORL1 receptor (IC50=472?nM) and μ receptor (IC50=1831?nM). JTC-801 at a concentration of 10?μM reverses the inhibitory action of nociceptin against forskolin-induced increase in cyclic AMP level (IC50: 2.58?μM, 1?nM of nociceptin used). JTC-801 alone does not affect the the production of cyclic AMP. The affinity of JTC-801 for ORL1 receptor, human opioid μ-, κ-, and δ-receptors is 8.2 nM, 102.9 nM, 1057.5 nM and 8647.2 nM.

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-in

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4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 100 mg/mL (223.23 mM; Need ultrasonic)H₂O : ≥ 0.33 mg/mL (0.74 mM)