Bioactivity | [Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively[1]. |
Invitro | [Arg14,Lys15]Nociceptin TFA is about 30-fold more potent than Nociceptin (NC) and produces longer lasting effects[2]. |
In Vivo | In in vivo experiments, [Arg14,Lys15]Nociceptin TFA mimics the effects of NC, producing, after intracerebroventricular administration, pronociceptive effects in the tail-withdrawal assay and inhibiting the locomotor activity of the mice[2]. |
Name | [Arg14,Lys15]Nociceptin TFA |
Shortening | FGGFTGARKSARKRKNQ |
Formula | C84H138F3N31O24 |
Molar Mass | 2023.18 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Okada K, Sujaku T, Chuman Y, et al. Highly potent nociceptin analog containing the Arg-Lys triple repeat. Biochem Biophys Res Commun. 2000;278(2):493-498. [2]. Rizzi D, Rizzi A, Bigoni R, et al. [Arg(14),Lys(15)]nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studies. J Pharmacol Exp Ther. 2002;300(1):57-63. |