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*  Endomorphin
They are tetrapeptides with the highest known affinity and selectivity for the μ-opioid receptor. Endomorphin-1 is found in the ... The endomorphins are a group of endogenous opioid peptides consisting of endomorphin-1 (Tyr-Pro-Trp-Phe-NH2) and endomorphin-2 ...
*  Low-dose naltrexone
Naltrexone is an opioid receptor antagonist, meaning it binds to opioid receptors in cells. These receptors bind endogenous ... Naltrexone and its active metabolite 6-β-naltrexol are competitive antagonists at μ-opioid and κ-opioid receptors, and to a ... One hypothesis behind low-dose naltrexone's mechanism of action is that inhibiting opioid receptors at low doses might cause ... Niciu, Mark J.; Arias, Albert J. (24 July 2013). "Targeted Opioid Receptor Antagonists in the Treatment of Alcohol Use ...
*  Nalmefene
... of the κ-opioid receptor (KOR), with similar affinity for these two receptors but a several-fold preference for the KOR. In ... Nalmefene acts as a silent antagonist of the μ-opioid receptor (MOR) (Ki = 0.24 nM) and as a weak partial agonist (Ki = 0.083 ... In addition to MOR and KOR binding, nalmefene also possesses some, albeit far lower affinity for the δ-opioid receptor (DOR) ( ... Nalmefene is a partial agonist of the κ-opioid receptor and may be useful to treat cocaine addiction. Butorphanol Nalfurafine ...
*  Leumorphin
... behaves as a potent and selective κ-opioid receptor agonist, similarly to other endogenous opioid peptide ... September 1984). "Human leumorphin is a potent, kappa opioid receptor agonist". Neuroscience Letters. 50 (1-3): 49-52. doi: ... Opioid peptide Schwarzer C (September 2009). "30 years of dynorphins-new insights on their functions in neuropsychiatric ... Leumorphin, also known as dynorphin B1-29, is a naturally occurring endogenous opioid peptide. Derived as a proteolytic ...
*  Tail flick test
Opioid Receptor Agonist/Norepinephrine Reuptake Inhibitor with Broad-Spectrum Analgesic Properties". Journal of Pharmacology ... Li, G.; Rhodes, J.; Girard, I.; Gammie, S.; Garland Jr., T. (2004). "Opioid-mediated pain sensitivity in mice bred for high ... Naloxone and naltrexone, two opioid antagonists, have been used to study pain sensitivity in relation to exercise in mice. ... Lastly, many thermal tests do not distinguish between opioid agonists and mixed agonist-antagonists, and consequently a tail ...
*  Buprenorphine/naltrexone
... a μ-opioid receptor (MOR) weak partial agonist and κ-opioid receptor (KOR) antagonist, and naltrexone, a MOR and KOR silent ... "Antidepressant-Like Effects of Buprenorphine are Mediated by Kappa Opioid Receptors". Neuropsychopharmacology. 41: 2344-2351. ... to result in a selective blockade of the KOR and hence fewer MOR activation-related concerns such as euphoria and opioid ...
*  Remifentanil
... , being a μ-receptor agonist, functions like other μ-receptor agonists, such as morphine and codeine, and can cause ... "Remifentanil, IV opioid analgesic, Remi , Ultiva". www.ultiva.com. Retrieved 2015-11-30. Gesztesi Z, Mootz BL, White PF. The ... Remifentanil is used as an opioid analgesic that has a rapid onset and rapid recovery time. It has been used effectively during ... The use of remifentanil has made possible the use of high-dose opioid and low-dose hypnotic anesthesia, due to synergism ...
*  Buprenorphine/samidorphan
... a weak partial agonist of the μ-opioid receptor (MOR), antagonist/very weak partial agonist of the κ-opioid receptor (KOR), and ... to a lesser extent, antagonist of the δ-opioid receptor (DOR) and weak partial agonist of the nociceptin receptor (NOP); and (2 ... Zhu J, Luo LY, Li JG, Chen C, Liu-Chen LY (1997). "Activation of the cloned human kappa opioid receptor by agonists enhances [ ... Robinson SA, Erickson RL, Browne CA, Lucki I (2016). "A role for the mu opioid receptor in the antidepressant effects of ...
*  Morphiceptin
... is a tetrapeptide (Tyr-Pro-Phe-Pro-NH2) that is a selective μ-opioid receptor agonist. It is derived from β- ... over δ-opioid receptors. When injected intracerebroventricularly (into the ventricular system of the brain), morphiceptin had ... meaning that the analgesic effect is mediated by the μ-opioid receptor. Morphiceptin is the (1S,2S,3S,4S)-form whereas ... receptor binding affinity". Life Sciences. 30 (18): 1547-1551. doi:10.1016/0024-3205(82)90242-9. ...
*  DAMGO
... ([D-Ala2, N-MePhe4, Gly-ol]-enkephalin) is a synthetic opioid peptide with high μ-opioid receptor specificity. It was ... "Regulation of Opioid Receptor Trafficking and Morphine Tolerance by Receptor Oligomerization". Cell. 108 (2): 271. doi:10.1016/ ... synthesized as a biologically stable analog of δ-opioid receptor-preferring endogenous opioids, leu- and met-enkephalin. Its ... "Endocytosis of the Mu Opioid Receptor Reduces Tolerance And a Cellular Hallmark of Opiate Withdrawal". Neuron. 32 (5): 829-839 ...
*  Morphine/naltrexone
... morphine being an opioid receptor agonist and naltrexone an opioid receptor antagonist. It is a schedule 2 controlled substance ... The drug combination morphine/naltrexone (trade name Embeda) was an opioid combination pain medication developed by King ...
*  Μ-opioid receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low ... δ-opioid receptor κ-opioid receptor GRCh38: Ensembl release 89: ENSG00000112038 - Ensembl, May 2017 GRCm38: Ensembl release 89 ... They are also referred to as μ-opioid peptide (MOP) receptors. The prototypical μ-opioid receptor agonist is morphine, the ... both might be involved in opioid addiction and opioid-induced deficits in cognition. Activation of the μ-opioid receptor by an ...
*  Opioid receptor
This receptor is known as the nociceptin receptor or ORL1 (opiate receptor-like 1). The opioid receptor types are nearly 70% ... Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are ... This receptor is now most commonly referred to as the opioid growth factor receptor (OGFr). Another postulated opioid receptor ... The opioid receptors are ~40% identical to somatostatin receptors (SSTRs). Opioid receptors are distributed widely in the brain ...
*  Κ-opioid receptor
δ-opioid receptor μ-opioid receptor GRCh38: Ensembl release 89: ENSG00000082556 - Ensembl, May 2017 GRCm38: Ensembl release 89 ... "Heterologous mu-opioid receptor adaptation by repeated stimulation of kappa-opioid receptor: up-regulation of G-protein ... The κ-opioid receptor (KOR) is a G protein-coupled receptor that in humans is encoded by the OPRK1 gene. The KOR is coupled to ... "Opioid Receptors: κ". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. ...
*  Δ-opioid receptor
... opioid receptors have been shown to interact with β2 adrenergic receptors, arrestin β1 and GPRASP1. K-opioid receptor μ-opioid ... The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR, is an inhibitory 7- ... It is also suggested however that the pain modulated by the mu-opioid receptor and that modulated by the δ-opioid receptor are ... Another interesting aspect of δ-opioid receptor function is the suggestion of mu/delta opioid receptor interactions. At the ...
*  Opioid peptide
... s are peptides that bind to opioid receptors in the brain; opiates and opioids mimic the effect of these peptides ... The opioid food peptides have lengths of typically 4-8 amino acids. The body's own opioids are generally much longer. Opioid ... They mimic the actions of endorphines because they bind to the same opioid receptors in the brain. These are the most common ... The apparently serendipitous finding of an opiate alkaloid-sensitive, opioid peptide-insensitive, µ3 opiate receptor subtype ...
*  Nociceptin receptor
... receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the OPRL1 (opioid receptor-like 1) gene. ... μ-opioid and δ-opioid receptors, partial agonist at κ-opioid receptor) Etorphine MCOPPB (full agonist) MT-7716 Nociceptin ... also partial agonist of µ-opioid and δ-opioid receptors, and competitive antagonist of κ-opioid receptors) BU08028 (Analogue of ... "Orphanin FQ/nociceptin-mediated desensitization of opioid receptor-like 1 receptor and mu opioid receptors involves protein ...
*  Eletriptan
... or opioid receptors. Eletriptan could be efficiently co-administrated with nitric oxide synthase (NOS's) inhibitors for the ... Eletriptan is a serotonin receptor agonist, specifically an agonist of certain 5-HT1 family receptors. Eletriptan binds with ... It has a modest affinity to the 5-HT[1A, 1E, 2B, 7] receptors, and little to no affinity at the 5-HT[2A, 2C, 3, 4, 5A, 6] ... The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in ...
*  Zenazocine
... and δ-opioid receptors, with less intrinsic activity at the former receptor and more at the latter receptor (hence, it behaves ... Cotton, R.; James, R. (1985). "Chapter 3. Analgesics, Opioids and Opioid Receptors". In Bailey, D. M. Annual Reports in ... Zenazocine (INN; WIN-42,964) is an opioid analgesic of the benzomorphan family which made it to phase II clinical trials before ...
*  Dihydromorphine
... δ-opioid (delta) and κ-opioid (kappa) receptors. Agonist of the μ-opioid and δ-opioid receptors is largely responsible for the ... 216 Costantino CM, Gomes I, Stockton SD, Lim MP, Devi LA (2012). "Opioid receptor heteromers in analgesia". Expert Rev Mol Med ... is used in scientific research to study binding of the opioid receptors in the nervous system. Dihydromorphine is slightly ... "Agonist-specific regulation of the delta-opioid receptor". Life Sci. 76 (6): 599-612. doi:10.1016/j.lfs.2004.07.020. PMID ...
*  Timeline of United States discoveries
1972 Opiate receptors Opioid receptors are a group of G protein-coupled receptors with opioids as ligands. The endogenous ... The opioid receptors are ~40% identical to somatostatin receptors (SSTRs). Opiate receptors were discovered in 1972 by the ... opioids are dynorphins, enkephalins, endorphins, endomorphins, and nociceptin. ...
*  Brigitte Kieffer
"Cloning Opioid Receptors to Better Understand Our Brain." Cloning Opioid Receptors to Better Understand Our Brain. For Women in ... "Opioid receptors: distinct roles in mood disorders." Trends in neurosciences 36.3 (2013): 195-206. - "Opioid Systems and Brain ... Study of brain opioid receptors that deal with depression and happiness are often a focus of her research. In many post-mortem ... In 1992, Kieffer succeeded in "first to clone and isolate the gene for an opioid receptor in the brain that plays a key role in ...
*  Outcomes Research Consortium
"Selective postoperative inhibition of gastrointestinal opioid receptors". N Engl J Med. 345: 935-40. doi:10.1056/nejmoa010564. ... Red hair results from a mutation of the melanocortin-1 receptor. The Consortium's results thus indicate that something about ... this receptor influences anesthetic action. Red hair was the first phenotype (physically apparent characteristics linked to a ...
*  Norbinaltorphimine
It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor ... "Participation of dorsal periaqueductal gray 5-HT1A receptors in the panicolytic-like effect of the κ-opioid receptor antagonist ... Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. Journal of ... Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. Life Sciences. 1987 Mar 30;40( ...
*  Butyrfentanyl
The opioid receptor affinity of fentanyl and its analogs was determined from their inhibitory potency in a binding assay with [ ... During the studies of in vitro inhibition of specific [3H] fentanyl binding to the opioid receptor, the order of analogues was ... It is an agonist for the μ-opioid receptors. Butyrfentanyl has no current legitimate clinical applications; however, it is ... This document also states that the article describing its clinical effects (analgesic studies, μ-, δ-, κ-opioid receptor ...
*  Hibernation
"Further studies on opioids and hibernation: delta opioid receptor ligand selectively induced hibernation in summer-active ... This supposed HIT is a mixture derived from serum, including at least one opioid-like substance. DADLE is an opioid that in ...
*  BU09059
... and δ-opioid receptors (Ki = 1.72 nM, 26.5 nM, and 1060 nM, respectively). κ-Opioid receptor § Antagonists List of ... BU09059 is a potent, selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor (KOR). It was derived ... Urbano, Mariangela; Guerrero, Miguel; Rosen, Hugh; Roberts, Edward (May 2014). "Antagonists of the kappa opioid receptor". ... M.; Bailey, Sarah J. (March 2014). "Characterization of BU09059: A Novel Potent Selective κ-Receptor Antagonist". ACS Chemical ...