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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats.
Rawls SM, et al. Neuropeptides. 2007 Aug;41(4):239-47. PMID: 17512052.
Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation.
Tamai H, et al. Eur J Pharmacol. 2005 Mar 14;510(3):223-8. PMID: 15763246.
Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801.
Yamada H, et al. Br J Pharmacol. 2002 Jan;135(2):323-32. PMID: 11815367.
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