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 Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostat ...

. However, instead of acting at the mu,

kappa Kappa (; uppercase Κ, lowercase κ or cursive ; , ''káppa'') is the tenth letter of the Greek alphabet, representing the voiceless velar plosive sound in Ancient and Modern Greek. In the system of Greek numerals, has a value of 20. It was d ...

and

delta Delta commonly refers to: * Delta (letter) (Δ or δ), the fourth letter of the Greek alphabet * D (NATO phonetic alphabet: "Delta"), the fourth letter in the Latin alphabet * River delta, at a river mouth * Delta Air Lines, a major US carrier ...

receptors, it is instead an

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

at the

nociceptin receptor The nociceptin opioid peptide receptor (NOP), also known as the nociceptin/orphanin FQ (N/OFQ) receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the ''OPRL1'' (opioid receptor-like 1) gene. The nociceptin recepto ...

Potential uses

Analgesic

Ro65-6570 has

analgesic An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...

properties. In rats, it is able to reduce cancer pain. It is also able to reduce pain caused by

arthritis Arthritis is a general medical term used to describe a disorder that affects joints. Symptoms generally include joint pain and stiffness. Other symptoms may include redness, warmth, Joint effusion, swelling, and decreased range of motion of ...

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 Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...

, but did not affect the

effect of those. This could make it useful if combined with more potent opioids, for example

oxycodone Oxycodone, sold under the brand name Roxicodone and OxyContin (which is the extended-release form) among others, is a semi-synthetic opioid used medically for the treatment of moderate to severe pain. It is highly addictive and is a commonly ...

and Ro65-6570 would reduce pain, but would be less addictive, unlike

alone. This effect was antagonized by the

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.J-113,397, further suggesting that this action is linked to the NOP receptor.

References

{{Opioid receptor modulators Nociceptin receptor agonists Imidazolidinones Piperidines Spiro compounds Anilines