Safe opioid analgesics targeting nociceptin receptor in primates

Opioid Analgesics

Intensive research on the neurobiology of pain over the past two decades has revealed many receptors, ion channels and enzymes with potential as novel targets for development of a new generation of analgesic agents. However, despite large investment in preclinical and clinical development of small molecules and biologics as potential novel pain therapeutics, very few have reached the clinic. He...

Nociceptin/Orphanin FQ Receptor Activation Attenuates Antinociception Induced by Mixed Nociceptin/Orphanin FQ/ -Opioid Receptor Agonists

Activation of brain nociceptin/orphanin FQ (NOP) receptors leads to attenuation of -opioid receptor (MOP receptor)-mediated antinociception. Buprenorphine, a high-affinity partial MOP receptor agonist also binds to NOP receptors with 80 nM affinity. The buprenorphine-induced inverted U-shaped doseresponse curve for antinociception may be due to NOP receptor activation, given that, in the presen...

Opioid and Nonopioid Analgesics

Opioid analgesics in palliative care

The discovery of the opioid receptors began in the 1970s and three (μ, δ and κ) are now recognised. Most current opioid analgesics interact preferentially with μ receptors, although some have actions at δ and κ receptors. The revelation that opioid receptors are present on peripheral sensory neurones and immune system cells, has led to the realisation that the opioid system is involved in a hos...

Non-opioid analgesics

C describe the concept of multimodal analgesia and give examples Abstract Opium is the natural substance to which modern narcotics owe their existence. First discovered in the 1500s, opium was the most potent analgesic compound in use, held in high regard, hence its Latin name laudanum (to praise). Subsequent studies into the effects of opium led to the discovery of the opioid receptors, and th...