JTC-801

JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor with a Ki of 8.2 nM. JTC-801 inhibited the binding of [(3)H]-nociceptin to human ORL(1) receptors expressed in HeLa cells with a K(i) value of 44.5 nM. JTC-801 (1 mg/kg, i.p.) blocked a significant proportion of the hypothermia caused by each dose of WIN 55212-2 (2.5, 5, and 10 mg/kg, i.p.). JTC-801 (1 mg/kg, i.p.) also blocked the hypothermia caused by another cannabinoid agonist, CP-55940 (1 mg/kg, i.p.). JTC-801 exhibits anti-nociceptive effects in acute pain models in vivo. JTC-801 reduced both the first and second phases of the nociceptive response with MED of 0.01 mg kg(-1) by i.v. administration or 1 mg kg(-1) by p.o. administration in the rat formalin test.