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Class of opioid receptors found in humans
The μ-opioid receptors (using the Greek letter mu, abbreviated MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin
Mu-opioid_receptor
Group of biological receptors
example, activation of mu-opioid receptors activates (not inhibits) dopamine release, and activation of kappa-opioid receptors can lead to noradrenaline
Opioid_receptor
affinity for the mu opioid receptor and instead act as ligands for the non-psychoactive nociceptin receptor. List of benzimidazole opioids List of fentanyl
List_of_orphine_opioids
Receptor antagonist that acts on one or more of the opioid receptors
An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors. Opioid antagonists can
Opioid_antagonist
used for scientific research as model kappa opioid receptor agonists. In the mid-2010s, one mu opioid receptor selective compound from this class, U-47700
Utopioid_(drug_class)
Protein-coding gene in the species Homo sapiens, named for ketazocine
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP for its ligand ketazocine, is a G protein-coupled receptor that is encoded by the
Κ-opioid_receptor
Opioid receptor
The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein
Δ-opioid_receptor
Atypical opioid drug
is an atypical opioid receptor modulator with unusual actions and effects. It acts as a biased partial agonist of the μ-opioid receptor (MOR), showing
SR-17018
Opioid analgesic
and 10 nM for the mu, delta, and the total opioid receptor population, respectively. Cychlorphine R6372 List of orphine opioids Leysen JE, Gommeren
R6890
Class of analgesic drug
Opioids are a class of drugs that derive from, or mimic, natural substances found in the opium poppy plant. Opioids work on opioid receptors in the brain
Opioid
Toxicity due to excessive consumption of opiates
coupled receptors distributed throughout the body—including the brain, skin and spinal cord. Three of the major opioid receptors include mu, kappa, delta
Opioid_overdose
Opioid used to treat pain and opioid use disorder
the treatment of opioid use disorder. [1] [2] Buprenorphine versus naltrexone Naltrexone is a full antagonist to the mu-opioid receptor, while buprenorphine
Buprenorphine
Chemical compound
Ohmecarfentanil (RTI-4614-38), also known as Ohlofentanil, is a mu-opioid receptor agonist from the class of fentanyl analogues which was found to be 30
Ohmecarfentanil
Synthetic opioid analgesic
opioids. It acts as an ultrapotent and highly selective agonist of the μ-opioid receptor. Carfentanil was first synthesized in 1974 by a team of chemists at
Carfentanil
Opioid antagonist peptide selective for the mu receptor
being a mu-selective opioid antagonist. In other words, when blocking opioid receptors, it is much more selective for the mu-opioid receptors than the
CTAP_(peptide)
Class of drugs
pain-relieving agents. They are important as centrally active, selective μ-opioid receptor agonists. The high potency of fentanyl (in humans) is matched by a
Nitazenes
Chemical compound
SR-14968 is a drug which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin
SR-14968
Chemical compound
functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy". Nature Communications. 12 (1) 3858. Bibcode:2021NatCo
MGM-16
Atypical opioid analgesic
μ-opioid receptors (MOR) than mitragynine. It acts primarily as a partial agonist at μ-opioid receptors while antagonizing δ- and κ-opioid receptors; unlike
7-Hydroxymitragynine
Type of drug
are opioids. Examples of such opioids are: pentazocine, agonist at the kappa (κ) and sigma (σ) with weak antagonist action at the mu opioid receptor (μ)
Agonist-antagonist
Combination pain relief drug
with alcohol is not recommended. Hydrocodone works by binding to the mu-opioid receptor. How paracetamol works is unclear but may involve blocking the creation
Hydrocodone/paracetamol
Opioid analgesic
agonist of the κ-opioid receptor (KOR), whereas it has relatively low affinity for the δ-opioid receptor (DOR) and sigma receptors. Nalbuphine was patented
Nalbuphine
Opioid analgesic
p-fluorofentanyl on cloned human opioid receptors and exploration of the role of Trp-318 and His-319 in μ-opioid receptor selectivity" (PDF). The Journal
Parafluorofentanyl
Drug class
acting μ-opioid receptor antagonists (PAMORAs) are a class of chemical compounds that are used to reverse adverse effects caused by opioids interacting
Peripherally acting μ-opioid receptor antagonist
Peripherally_acting_μ-opioid_receptor_antagonist
Opioid analgesic drug
non-selective opioid receptor agonist, including as a dual μ-opioid receptor and nociceptin receptor full agonist and to a lesser extent as a κ-opioid receptor partial
Cebranopadol
Opioid analgesic compound
symptoms of opioid withdrawal. It is a partial agonist of the μ-opioid receptors; and as such can produce effects similar to those of classic opioids such as
Mitragynine
Pharmaceutical compound
Deuterated mitragynine (developmental code name KUR-101) is an atypical μ-opioid receptor agonist and deuterated analogue of mitragynine (found in kratom) which
Deuterated_mitragynine
Semi-synthetic opioid
through affinity to predominantly μ-opioid receptor and to lesser extent to κ-opioid receptor and δ-opioid receptor. A 1956 source states that 30 mg of
Dihydrocodeine
Chemical compound
7-hydroxymitragynine and shows higher potency as an agonist of the μ-opioid receptor and δ-opioid receptor compared to 7-hydroxymitragynine itself. MGM-15 has been
MGM-15
Drugs used to achieve relief from pain
delivers analgesia by not only delivering "opioid-like" effects (through mild agonism of the μ-opioid receptor) but also by acting as a weak but fast-acting
Analgesic
Treatment for opioid use disorder
An opioid is considered a ligand, which is an ion or a molecule. An opioid ligand travels to the brain and attaches itself to an opioid receptor, which
Opioid_agonist_therapy
Chemical compound
(-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist". Journal of Medicinal Chemistry. 32 (2): 418–21. doi:10
Cyprodime
Opioid drug used in pain relief
opioid withdrawal. Use during pregnancy or breastfeeding is generally not recommended. Hydrocodone is believed to work by activating opioid receptors
Hydrocodone
Chemical compound
kappa opioid receptor agonist with only moderate affinity at the mu opioid receptor. Nevertheless, it has still appeared on the recreational drug market
U-48800
Opioid medication
be allergic to oxycodone. Opioid withdrawal may occur if rapidly stopped. Oxycodone acts by activating the μ-opioid receptor. When taken by mouth, it has
Oxycodone
Protein-coding gene in the species Homo sapiens
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
Nociceptin_receptor
Chemical compound
H, Pasternak GW (January 2003). "14-Methoxymetopon, a very potent mu-opioid receptor-selective analgesic with an unusual pharmacological profile". European
14-Methoxymetopon
Semi-synthetic opioid
immobilise elephants and other large mammals. Diprenorphine (Revivon) is an opioid receptor antagonist that can be administered in proportion to the amount of
Etorphine
Pharmaceutical compound
literature by Laura M. Bohn and colleagues by 2017. List of orphine opioids μ-Opioid receptor § Biased agonists Acevedo-Canabal A, Grim TW, Schmid CL, McFague
SR-15099
Opioid treatment
an abuse-deterrent is that buprenorphine binds more tightly to the mu-opioid receptor than naloxone. There are small differences in the pharmacokinetics
Buprenorphine/naloxone
Chemical compound
peripherally acting μ-opioid receptor antagonist. With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central nervous
Alvimopan
Pain caused by opioid addiction
The mu opioid receptor is targeted most often by opioids to relieve pain. Two of the most commonly used opioid antagonists at the mu receptor are naltrexone
Opioid-induced_hyperalgesia
Medicine used to reduce diarrhea
under the brand name Imodium, among others, is a medication of the opioid receptor agonist class used to decrease the frequency of diarrhea. It is often
Loperamide
Opioid analgesic
μ-opioid receptor (Ki 11.1 ± 0.4 nM) and possesses significantly lower affinity for the κ-opioid receptor (Ki = 287 ± 24 nM) and δ-opioid receptor (Ki
U-47700
Investigational antidepressant compound
developmental codes JNJ-67953964, CERC-501, and LY-2456302, is a κ-opioid receptor (KOR) antagonist which was under development for the treatment of major
Aticaprant
Withdrawn opioid medication
Dextropropoxyphene acts as a μ-opioid receptor agonist. It also acts as a potent, noncompetitive α3β4 neuronal nicotinic acetylcholine receptor antagonist, as well
Dextropropoxyphene
Side effect of opioids during anesthesia
Wooden Chest Syndrome (WCS) is rooted in the binding of fentanyl to mu-opioid receptors in the central nervous system. This interaction triggers a cascade
Wooden_chest_syndrome
Pharmaceutical compound
opioid receptor modulator which is under development for the treatment of pain and opioid use disorder. It is a highly biased agonist of the μ-opioid
MEB-1170
Opioid medication
Fentanyl has a short duration of action. Fentanyl works by activating μ-opioid receptors. Brand names include Actiq, Duragesic, and Sublimaze, among others
Fentanyl
Opioid analgesic
and RTI-4614-4) is an extremely potent opioid analgesic drug which selectively binds to the μ-opioid receptor. There are eight possible stereoisomers
Ohmefentanyl
Cough suppressant and dissociative drug
affinity for the mu-opioid receptor activity typical of morphinan compounds and exerts its therapeutic effects through several other receptors. In its pure
Dextromethorphan
Chemical compound
2011). "Truncated G protein-coupled mu opioid receptor MOR-1 splice variants are targets for highly potent opioid analgesics lacking side effects". Proc
IBNtxA
Opioid analgesic
metabolite, norpethidine. Pethidine has weak binding affinity for the mu-opioid receptor in humans at 450.1 nM (Morphine 1.168). Pethidine is quickly hydrolysed
Pethidine
Opioid medication used for pain relief
"Molecular determinants of non-specific recognition of delta, mu, and kappa opioid receptors". Bioorganic & Medicinal Chemistry. 9 (1): 69–76. doi:10
Hydromorphone
Pharmaceutical compound
selective agonist of the mu opioid receptor. It is a metabolically stable analogue of dermorphin, a naturally occurring opioid peptide secreted by some
DALDA
Agent in biochemistry
e., negative) efficacy. Receptors for which inverse agonists have been identified include the GABAA, melanocortin, mu opioid, histamine, serotonin, and
Inverse_agonist
Pain medication of the opiate family
the benchmark to which all other opioids are compared. It interacts predominantly with the μ–δ-opioid (mu–delta) receptor heteromer. The μ-binding sites
Morphine
Chemical compound
morphine, the unnatural enantiomer has no affinity or efficacy for the mu opioid receptor and therefore has no analgesic effects. To the contrary, in rats,
(+)-Morphine
Medication in the treatment for Opioid-Induced Constipation
that acts as a peripherally acting μ-opioid receptor antagonist that acts to reverse some of the side effects of opioid drugs such as constipation without
Methylnaltrexone
Opioid receptor antagonist
competitive opioid receptor antagonist. It reverses the depression of the central nervous system and respiratory system caused by opioids. Naloxone was
Naloxone
Opioid antagonist
Juhakoski A, Karhuvaara S, et al. (December 2005). "Prolonged central mu-opioid receptor occupancy after single and repeated nalmefene dosing". Neuropsychopharmacology
Nalmefene
Chemical compound
responsible for this activity. Akuammine is an opioid agonist with low affinity, selective for the mu-opioid receptor, when tested in vitro. Merck Index (12th ed
Akuammine
Chemical compound
G, Archambeau A, et al. (April 2013). "Orvinols with mixed kappa/mu opioid receptor agonist activity". Journal of Medicinal Chemistry. 56 (8): 3207–3216
M320_(opioid)
Opioid analgesic compound
7-hydroxymitragynine. Mitragynine pseudoindoxyl is a μ-opioid receptor agonist and δ-opioid receptor antagonist. Animal studies have shown it causes reduced
Mitragynine_pseudoindoxyl
Chemical compound
μ2-opioid receptor and antagonist of the μ1-opioid receptor. It produces analgesia in animals that differs from that of conventional μ-opioid receptor agonists
TRIMU_5
Opioid analgesic and recreational drug
third opioid type is the mu-3 receptor, which may be a commonality to other six-position monoesters of morphine. The contribution of these receptors to the
Heroin
Chemical compound
pharmacological profile of the 5-benzyl analogue of 14-methoxymetopon, a novel mu opioid analgesic with reduced propensity to alter motor function". Eur J Pharm
14-Methoxydihydromorphinone
Chemical compound
Yue Z, Chen YT, et al. (October 2018). "Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias". Journal of Medicinal
Brorphine
Opioid antagonist
Methocinnamox (MCAM) is an opioid receptor antagonist. It is a pseudo-irreversible non-competitive antagonist of the μ-opioid receptor and a competitive antagonist
Methocinnamox
Chemical compound
selective pseudo-irreversible partial agonist of the μ-opioid receptor (MOR). It shows a mixture of opioid agonist- and antagonist-like effects. The drug has
Methoclocinnamox
Combination drug formulation
antidepressants in treatment-resistant depression (TRD). It is a κ-opioid receptor (KOR) antagonist and was being developed by Alkermes. ALKS-5461 failed
Buprenorphine/samidorphan
Opioid analgesic
"Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor". Journal of Medicinal Chemistry. 43 (3): 381–91. doi:10.1021/jm9903702
R-30490
Opioid analgesic
effects due to their long metabolic half-life and strong receptor affinity at the mu-opioid receptor sites. Therefore, they impart much of the satiating and
Methadone
Chemical compound
Endomorphins belong to the opioid class of neuropeptides (protein neurotransmitters). Opioids are ligands that bind to opioid receptors and exist both as endogenous
Endomorphin
Chemical compound
IC-26 (WIN 1161-3, Methiodone) is an analogue of the opioid analgesic methadone, where the carbonyl group has been replaced by the bioisosteric sulfone
IC-26
Medication
Sadee W (May 2007). "Different effects of opioid antagonists on mu-, delta-, and kappa-opioid receptors with and without agonist pretreatment". The
Naltrexone
Opioid analgesic drug
selective agonists of μ-opioid receptor (MOR) with relatively low affinity for the δ-opioid receptor and the κ-opioid receptor. In accordance with these
Bucinnazine
Opioid analgesic compound
a selective κ-opioid receptor agonist with no significant μ-opioid receptor affinity, herkinorin is predominantly a μ-opioid receptor agonist. Compared
Herkinorin
Peptide hormone in humans
types of G protein–coupled receptors (GPCRs), most notably to the mu and kappa opioid receptors. Binding to these receptors prevents the release of Substance
Β-Endorphin
Drug
1]nonan-9-yl)piperidin-4-yl)indolin-2-one], a novel mixed nociceptin/orphanin FQ/mu-opioid receptor partial agonist: analgesic and rewarding properties in mice". The
SR-16435
Pleasurable phenomenon elicited via direct stimulation of specific brain regions
Generally speaking, high potency mu-opioid receptor (MOR) agonists have high abuse potential, while kappa-opioid receptor (KOR) agonists generally produce
Brain_stimulation_reward
Atypical antidepressant
mu-opioid agonist but not delta-opioid agonist, with EC50 at the mu-opioid receptor of 0.545 μM (vs 0.194 μM for tianeptine). MC3 is a very weak mu-opioid
Tianeptine
Chemical compound
capability of illicit labs. Benzylfentanyl has a Ki of 213 nM at the mu opioid receptor, binding around 1/200 as strong as fentanyl itself, though it is
Benzylfentanyl
Chemical compound
"AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies". Neuropharmacology.
Rimonabant
Chemical compound
the First Small-Molecule Opioid Pan Antagonist with Nanomolar Affinity at Mu, Delta, Kappa, and Nociceptin Opioid Receptors". ACS Chemical Neuroscience
AT-076
Chemical compound
It is selective for antagonism of the MOR over the δ-opioid receptor (DOR) and κ-opioid receptor (KOR). Chemically, it is a naltrexone derivative with
Β-Funaltrexamine
Opioid analgesic drug
to and activating the μ-opioid receptor (MOR) and, to a much lesser extent, the δ-opioid receptor (DOR) and κ-opioid receptor (KOR). Its activity at the
Oxymorphone
Opioid analgesic drug
(December 2020). "Uncovering the analgesic effects of a pH-dependent mu-opioid receptor agonist using a model of nonevoked ongoing pain". Pain. 161 (12):
NFEPP
Chemical compound
"SUMMIT-07: a randomized trial of NKTR-181, a new molecular entity, full mu-opioid receptor agonist for chronic low-back pain". PAIN. 160 (6): 1374–1382. doi:10
Oxycodegol
Opioid analgesic
into opioid receptors. In addition to acting on the μ-opioid receptor, lofentanil has also been found to act as a full agonist of the κ-opioid receptor (Ki
Lofentanil
Pharmaceutical compound
antidotes such as naloxone due to its high binding affinity at the mu opioid receptor. AT-076 Diprenorphine LY-255582 Takeuchi K, Holloway WG, McKinzie
Compound 9 (opioid antagonist)
Compound_9_(opioid_antagonist)
Chemical compound
antagonists such as naltrexone and others. It is a potent agonist of the μ-opioid receptor, but is poorly able to cross the blood–brain barrier into the central
Noroxymorphone
Opioid analgesic of benzenoid class
others, is a synthetic opioid analgesic with a dual mode of action as a highly selective full agonist of the μ-opioid receptor and as a norepinephrine
Tapentadol
Semi-synthetic opioid, morphine analogue
Desomorphine (or in some formulations known as Krokodil) is a semi-synthetic opioid commercialized by Roche, with powerful, fast-acting effects, such as sedation
Desomorphine
Synthetic opioid peptide
synthetic opioid peptide with high μ-opioid receptor specificity. It was synthesized as a biologically stable analog of δ-opioid receptor-preferring
DAMGO
Chemical compound
(August 2018). "A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates". Science Translational
AT-121
Medication used in the treatment for Opioid-Induced Constipation
peripherally acting μ-opioid receptor antagonist developed by AstraZeneca, licensed from Nektar Therapeutics, for the treatment of opioid-induced constipation
Naloxegol
Opioid receptor antagonist
"Inverse agonists and neutral antagonists at mu opioid receptor (MOR): possible role of basal receptor signaling in narcotic dependence". J Neurochem
Β-Naltrexamine
Opiate and prodrug of morphine used to treat pain
"Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors". Molecular Pharmacology. 45 (2): 330–334. doi:10.1016/S0026-895X(25)09932-8
Codeine
Relay center of the thalamus for nociceptive stimuli
Daniel Humberto Pozza et al. Nociceptive behaviour upon modulation of mu-opioid receptors in the ventrobasal complex of the thalamus of rats. Pain 148 (2010)
Ventrobasal_complex
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MU OPIOID-RECEPTOR
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MU OPIOID-RECEPTOR
MU OPIOID-RECEPTOR
MU OPIOID-RECEPTOR
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