Ro65-6570 Explained

Drug Name:Ro65-6570[1] [2]
Pubchem:10022859
Iuphar Ligand:8864
Chembl:281274
Iupac Name:8-(1,2-dihydroacenaphthylen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
C:25
H:25
N:3
O:1
Smiles:C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)C4CC5=CC=CC6=C5C4=CC=C6
Stdinchi: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)
Stdinchikey: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]

Notes and References

  1. Web site: 8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one . PubChem . U.S. National Library of Medicine .
  2. Web site: Ro 65-6570 Hydrochloride . Krackeler Scientific, Inc .
  3. Rutten K, De Vry J, Bruckmann W, Tzschentke TM . 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 . April 2011 . 21095077 . 10.1016/j.drugalcdep.2010.10.004 .
  4. Rutten K, De Vry J, Bruckmann W, Tzschentke TM . 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 . April 2011 . 21095077 . 10.1016/j.drugalcdep.2010.10.004 .
  5. Sliepen SH, Korioth J, Christoph T, Tzschentke TM, Diaz-delCastillo M, Heegaard AM, Rutten K . 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 . May 2021 . 31724155 . 8246843 . 10.1111/bph.14899 .
  6. Schiene K, Schröder W, Linz K, Frosch S, Tzschentke TM, Jansen U, Christoph T . 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 . August 2018 . 29753041 . 10.1016/j.ejphar.2018.05.005 . 21663667 .
  7. Rutten K, De Vry J, Bruckmann W, Tzschentke TM . 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 . October 2010 . 20674566 . 10.1016/j.ejphar.2010.07.036 .

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