From Wikipedia, the free encyclopedia
Nociceptin receptor agonist
Ro65-6570
[1]
[2]
Names
IUPAC name
8-(1,2-dihydroacenaphthylen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
Other names
8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
Identifiers
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
C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)C4CC5=CC=CC6=C5C4=CC=C6
Properties
C 25 H 25 N 3 O
Molar mass
383.495 g·mol−1
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
Ro65-6570 is an opioid drug. It has a potential use in preventing the addiction to other opioids.
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 .
[3]
Potential uses
Analgesic
Ro65-6570 has
analgesic properties. In rats, it's able to reduce cancer pain.
[4] It is also able to reduce pain caused by
arthritis .
[5]
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 .
[6]
References
^
"8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one" .
^
"Ro 65-6570 Hydrochloride | Krackeler Scientific, Inc" .
^ Rutten, Kris; De Vry, Jean; Bruckmann, Walter; Tzschentke, Thomas M. (2011-04-01).
"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 .
ISSN
1879-0046 .
PMID
21095077 .
^ Sliepen, Sonny H. J.; Korioth, Johanna; Christoph, Thomas; Tzschentke, Thomas M.; Diaz-delCastillo, Marta; Heegaard, Anne-Marie; Rutten, Kris (2019-11-13).
"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 .
ISSN
1476-5381 .
PMC
8246843 .
PMID
31724155 .
^ Schiene, Klaus; Schröder, Wolfgang; Linz, Klaus; Frosch, Stefanie; Tzschentke, Thomas M.; Jansen, Ulla; Christoph, Thomas (2018-08-05).
"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 .
ISSN
1879-0712 .
PMID
29753041 .
S2CID
21663667 .
^ Rutten, Kris; De Vry, Jean; Bruckmann, Walter; Tzschentke, Thomas M. (2010-10-25).
"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 .
ISSN
1879-0712 .
PMID
20674566 .