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They are also referred to as μ(mu)-opioid peptide (MOP) receptors. The prototypical μ-opioid receptor agonist is morphine, the primary psychoactive alkaloid in opium and for which the receptor was named, with mu being the first letter of Morpheus, the compound's namesake in the original Greek.
The receptor families delta, kappa, and mu demonstrate 55–58% identity to one another, and a 48–49% homology to the nociceptin receptor. Taken together, this indicates that the NOP receptor gene, OPRL1, has equal evolutionary origin, but a higher mutation rate, than the other receptor genes.
The receptors for enkephalin are the delta opioid receptors and mu opioid receptors. Opioid receptors are a group of G-protein-coupled receptors, with other opioids as ligands as well. The other endogenous opioids are dynorphins (that bind to kappa receptors), endorphins (mu receptors), endomorphins, and nociceptin-orphanin FQ.
In addition, there are three subtypes of μ-receptor: μ 1 and μ 2, and the newly discovered μ 3. Another receptor of clinical importance is the opioid-receptor-like receptor 1 (ORL1), which is involved in pain responses as well as having a major role in the development of tolerance to μ-opioid agonists used as analgesics.
One of the ways the chemoreceptor trigger zone implements its effects on the vomiting center is by activation of the opioid mu receptors and delta receptors. [6] The activation of these opioid receptors in the CTZ are especially important for patients who take opioid based pain medications on a regular basis.
Methylnaltrexone is a peripheral acting mu-opioid receptor antagonist, and does not cross the blood brain barrier. [9] Methylnaltrexone has restricted access through the blood brain barrier because it is a quaternary amine, which carries a positive charge when in a solution.
Bound μ-opioid receptors typically induce inhibitory effects on neuronal activity. [3] Endomorphin-like immunoreactivity exists within the central and peripheral nervous systems , where endomorphin-1 appears to be concentrated in the brain and upper brainstem , and endomorphin-2 in the spinal cord and lower brainstem. [ 2 ]
Pages in category "Mu-opioid receptor agonists" The following 200 pages are in this category, out of approximately 291 total. This list may not reflect recent changes .