Ro65-6570

Ro65-6570^[1]^[2]
Identifiers
	IUPAC name 8-(1,2-dihydroacenaphthylen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one;
PubChem CID	10022859;
IUPHAR/BPS	8864;
ChEMBL	ChEMBL281274;
Chemical and physical data
Formula	C25H25N3O
Molar mass	383.495 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)C4CC5=CC=CC6=C5C4=CC=C6;
	InChI InChI=InChI=1S/C25H25N3O/c29-24-25(28(17-26-24)20-9-2-1-3-10-20)12-14-27(15-13-25)22-16-19-8-4-6-18-7-5-11-21(22)23(18)19/h1-11,22H,12-17H2,(H,26,29); Key:BBOAHBVXCYBKLC-UHFFFAOYSA-N;

Ro65-6570 is an opioid drug. It has a potential use in preventing the addiction to other opioids.^[3]

Mechanism of action

Ro65-6570 is an opioid drug, it works by activating opioid receptors. However, instead of acting at the mu, kappa and delta receptors, it is instead an agonist at the nociceptin receptor.^[4]

Potential uses

Analgesic

Ro65-6570 has analgesic properties. In rats, it is able to reduce cancer pain.^[5] It is also able to reduce pain caused by arthritis.^[6]

Prevention of opioid addiction

While being an opioid agonist, Ro65-6570 did not display addictive properties, it instead reduced the addictive properties of other opioids, but did not affect the analgesic effect of those. This could make it useful if combined with more potent opioids, for example oxycodone and Ro65-6570 would reduce pain, but would be less addictive, unlike oxycodone alone. This effect was antagonized by the nociceptin receptor antagonist J-113,397, further suggesting that this action is linked to the NOP receptor.^[7]

References

^ "8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one". PubChem. U.S. National Library of Medicine.
^ "Ro 65-6570 Hydrochloride". Krackeler Scientific, Inc.
^ Rutten K, De Vry J, Bruckmann W, Tzschentke TM (April 2011). "Pharmacological blockade or genetic knockout of the NOP receptor potentiates the rewarding effect of morphine in rats". Drug and Alcohol Dependence. 114 (2–3): 253–6. doi:10.1016/j.drugalcdep.2010.10.004. PMID 21095077.
^ Rutten K, De Vry J, Bruckmann W, Tzschentke TM (April 2011). "Pharmacological blockade or genetic knockout of the NOP receptor potentiates the rewarding effect of morphine in rats". Drug and Alcohol Dependence. 114 (2–3): 253–256. doi:10.1016/j.drugalcdep.2010.10.004. PMID 21095077.
^ Sliepen SH, Korioth J, Christoph T, Tzschentke TM, Diaz-delCastillo M, Heegaard AM, et al. (May 2021). "The nociceptin/orphanin FQ receptor system as a target to alleviate cancer-induced bone pain in rats: Model validation and pharmacological evaluation". British Journal of Pharmacology. 178 (9): 1995–2007. doi:10.1111/bph.14899. PMC 8246843. PMID 31724155.
^ Schiene K, Schröder W, Linz K, Frosch S, Tzschentke TM, Jansen U, et al. (August 2018). "Nociceptin/orphanin FQ opioid peptide (NOP) receptor and µ-opioid peptide (MOP) receptors both contribute to the anti-hypersensitive effect of cebranopadol in a rat model of arthritic pain". European Journal of Pharmacology. 832: 90–95. doi:10.1016/j.ejphar.2018.05.005. PMID 29753041. S2CID 21663667.
^ Rutten K, De Vry J, Bruckmann W, Tzschentke TM (October 2010). "Effects of the NOP receptor agonist Ro65-6570 on the acquisition of opiate- and psychostimulant-induced conditioned place preference in rats". European Journal of Pharmacology. 645 (1–3): 119–126. doi:10.1016/j.ejphar.2010.07.036. PMID 20674566.

[1] "8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one". PubChem. U.S. National Library of Medicine.

[2] "Ro 65-6570 Hydrochloride". Krackeler Scientific, Inc.

[Rutten_2011-3] Rutten K, De Vry J, Bruckmann W, Tzschentke TM (April 2011). "Pharmacological blockade or genetic knockout of the NOP receptor potentiates the rewarding effect of morphine in rats". Drug and Alcohol Dependence. 114 (2–3): 253–6. doi:10.1016/j.drugalcdep.2010.10.004. PMID 21095077.

[4] Rutten K, De Vry J, Bruckmann W, Tzschentke TM (April 2011). "Pharmacological blockade or genetic knockout of the NOP receptor potentiates the rewarding effect of morphine in rats". Drug and Alcohol Dependence. 114 (2–3): 253–256. doi:10.1016/j.drugalcdep.2010.10.004. PMID 21095077.

[5] Sliepen SH, Korioth J, Christoph T, Tzschentke TM, Diaz-delCastillo M, Heegaard AM, et al. (May 2021). "The nociceptin/orphanin FQ receptor system as a target to alleviate cancer-induced bone pain in rats: Model validation and pharmacological evaluation". British Journal of Pharmacology. 178 (9): 1995–2007. doi:10.1111/bph.14899. PMC 8246843. PMID 31724155.

[6] Schiene K, Schröder W, Linz K, Frosch S, Tzschentke TM, Jansen U, et al. (August 2018). "Nociceptin/orphanin FQ opioid peptide (NOP) receptor and µ-opioid peptide (MOP) receptors both contribute to the anti-hypersensitive effect of cebranopadol in a rat model of arthritic pain". European Journal of Pharmacology. 832: 90–95. doi:10.1016/j.ejphar.2018.05.005. PMID 29753041. S2CID 21663667.

[7] Rutten K, De Vry J, Bruckmann W, Tzschentke TM (October 2010). "Effects of the NOP receptor agonist Ro65-6570 on the acquisition of opiate- and psychostimulant-induced conditioned place preference in rats". European Journal of Pharmacology. 645 (1–3): 119–126. doi:10.1016/j.ejphar.2010.07.036. PMID 20674566.

[1]

[2]

[3]

[4]

[5]

[6]

[7]