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*  Buprenorphine/samidorphan
Robinson SA, Erickson RL, Browne CA, Lucki I (2016). "A role for the mu opioid receptor in the antidepressant effects of ... a weak partial agonist of the μ-opioid receptor (MOR), antagonist/very weak partial agonist of the κ-opioid receptor (KOR), and ... June 2014). "BU08073 a Buprenorphine Analog with Partial Agonist Activity at mu Receptors in vitro but Long-Lasting Opioid ... to a lesser extent, antagonist of the δ-opioid receptor (DOR) and weak partial agonist of the nociceptin receptor (NOP); and (2 ...
*  DAMGO
"Endocytosis of the Mu Opioid Receptor Reduces Tolerance And a Cellular Hallmark of Opiate Withdrawal". Neuron. 32 (5): 829-839 ... 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 ...
*  Μ-opioid receptor
IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. mu Opioid Receptor at ... 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 ...
*  Dextrorphan
"Characterization of the cloned human mu opioid receptor". J. Pharmacol. Exp. Ther. 272 (1): 423-8. PMID 7815359. Pechnick, R. N ... dextrorphan is much more potent as an NMDA receptor antagonist as well much less active as a serotonin reuptake inhibitor, but ...
*  Levacetylmethadol
Levacetylmethadyl acts as a mu-opioid receptor agonist. It also acts as a potent, noncompetitive α3β4 neuronal nicotinic ... It was approved in 1993 by the U.S. Food and Drug Administration for use in the treatment of opioid dependence. In 2001, ... LAAM is indicated as a second-line treatment for the treatment and management of opioid dependence if patients fail to respond ... Levacetylmethadol (INN), levomethadyl acetate (USAN), OrLAAM (trade name) or levo-α-acetylmethadol (LAAM) is a synthetic opioid ...
*  Alfentanil
It is an agonist at mu opioid receptors. While alfentanil tends to cause fewer cardiovascular complications than other similar ... Alfentanil (R-39209, trade name Alfenta, Rapifen in Australia) is a potent but short-acting synthetic opioid analgesic drug, ...
*  Freeman-Sheldon syndrome
Liberzon I, Zubieta JK, Fig LM, Phan KL, Koeppe RA, Taylor SF (May 2002). "mu-Opioid receptors and limbic responses to aversive ... "Behavioral stress modifies hippocampal plasticity through N-methyl-D-aspartate receptor activation". Proc. Natl. Acad. Sci. U.S ...
*  Arylcyclohexylamine
Itzhak, Y.; Simon (1984). "A novel phencyclidine analog interacts selectively with mu opioid receptors". The Journal of ... and μ-opioid receptor agonistic properties. Additionally, σ receptor agonistic, nACh receptor antagonistic, and D2 receptor ... and activation of the μ-opioid receptor causes analgesic and euphoriant effects. Stimulation of the σ and D2 receptors may also ... and BDPC is a superpotent μ-opioid agonist, while PRE-084 is a selective sigma receptor agonist. Thus, radically different ...
*  Gaseous signaling molecules
Gillman MA, Lichtigfeld FJ (March 1985). "Nitrous oxide acts directly at the mu opioid receptor". Anesthesiology. 62 (3): 375- ... "Effects of nitrous oxide and halothane on mu and kappa opioid receptors in guinea-pig brain". Anesthesiology. 70: 541-544. doi: ... Apart from its direct and indirect actions at opioid recepters, it was also shown that N2O inhibits NMDA receptor-mediated ... 3H)Naloxone displacement: evidence for nitrous oxide as opioid receptor agonist". Eur J Pharmacol. 89: 177-178. doi:10.1016/ ...
*  Doxpicomine
... (Doxpicodin, Doxpizodine) is a mild opioid analgesic drug. The drug acts as a mu-opioid receptor agonist. It is of ... although all compounds in this family are comparatively weak mu agonists. US patent 3905987, Booher, R. N., "m-Dioxane-5- ...
*  Xorphanol
"Activity of opioid ligands in cells expressing cloned mu opioid receptors". BMC Pharmacol. 3: 1. doi:10.1186/1471-2210-3-1. PMC ... "Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors". BMC Neuroscience. 3 (1): 19. doi:10.1186/ ... "Pharmacological profiles of opioid ligands at Kappa opioid receptors". BMC Pharmacology. 6 (1): 3. doi:10.1186/1471-2210-6-3. ... ISBN 978-0-89766-441-7. Gmerek, Debra E.; Cowan, A. (1988). "Role of Opioid Receptors in Bombesin-induced Grooming". Annals of ...
*  Dezocine
... as it acts as a partial agonist primarily on mu-opioid receptors. At kappa-opioid receptors, it acts as an antagonist. Overall ... "Activity of opioid ligands in cells expressing cloned mu opioid receptors". BMC Pharmacology. 3: 1. PMC 140036 . PMID 12513698 ... and kappa-opioid receptors. Dezocine is a mixed agonist/antagonist of opioid receptors. It is related to other benzomorphans ... Because decozine has mixed agonist/antagonist effects on mu-, delta-, and kappa-opioid receptors, it has a lowered dependence ...
*  Lofentanil
Bot, G; Blake, AD; Li, S; Reisine, T (Jun 1998). "Fentanyl and its analogs desensitize the cloned mu opioid receptor". Journal ... "Study on mechanism of interaction of nociceptin and opioids binding with opioid receptor-like 1 receptor". Acta Pharmacologica ... In addition to acting on the μ-opioid receptor, lofentanil has also been found to act as a full agonist of the κ-opioid ... "Pharmacological profiles of opioid ligands at Kappa opioid receptors". BMC Pharmacology. 6 (1): 3. doi:10.1186/1471-2210-6-3. ...
*  Salvinorin A
"Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands". Journal of Medicinal Chemistry. 48 (15): 4765-71. ... It acts as a kappa opioid receptor agonist and is the first known compound acting on this receptor that is not an alkaloid. ... A few derivatives such as herkinorin have reduced kappa opioid action and instead act as mu opioid agonists. 2-Methoxymethyl ... Unlike other known opioid-receptor ligands, salvinorin A is not an alkaloid as it does not contain a basic nitrogen atom. ...
*  RGS9
... -2 is of particular interest as the most important RGS protein involved in terminating signalling by the mu opioid receptor ... Garzón J, Rodríguez-Muñoz M, López-Fando A, Sánchez-Blázquez P (March 2005). "Activation of mu-opioid receptors transfers ... "RGS9-2 is a negative modulator of mu-opioid receptor function". Journal of Neurochemistry. 103 (2): 617-25. doi:10.1111/j.1471- ... "RGS-Rz and RGS9-2 proteins control mu-opioid receptor desensitisation in CNS: the role of activated Galphaz subunits". ...
*  Cinobufagin
It is thought to trigger increased synthesis of β-END and the up-regulation of the mu opioid receptor in mouse tumor tissue ... β-END binds the mu opioid receptor to cause the analgesic effect. C. elegans can catabolize cinobufagin into five distinct ...
*  Ventral tegmental area
Indeed, tVTA/RMTg cells express high levels of mu-opioid receptors (Jhou et al., 2009a, 2012; Jalabert et al., 2011), and in ... The tVTA is rich in inhibitory GABA neurons expressing μ-opioid receptors and sends extensive projections toward midbrain ... Lu, XY; Ghasemzadeh, MB; Kalivas, PW (Feb 1998). "Expression of D-1 receptor, D-2 receptor, substance P and enkephalin ... Sziráki I, Sershen H, Hashim A, Lajtha A (2002). "Receptors in the ventral tegmental area mediating nicotine-induced dopamine ...
*  Rostromedial tegmental nucleus
Indeed, tVTA/RMTg cells express high levels of mu-opioid receptors (Jhou et al., 2009a, 2012; Jalabert et al., 2011), and in ... The tVTA is rich in inhibitory GABA neurons expressing μ-opioid receptors and sends extensive projections toward midbrain ... express μ-opioid receptors. Current evidence suggests that exogenous opiates (e.g., morphine and heroin) excite the dopamine ... pathways originating in the VTA by activating the μ-opioid receptors in neurons projecting from the RMTg; opioid activation of ...
*  TRIMU 5
... is a selective agonist of the mu opioid receptor type 2. Eisenberg RM (1994). "TRIMU-5, a mu 2-opioid receptor agonist ...
*  Tricyclic antidepressant
"Effects of imipramine administration on mu-opioid receptor immunostaining in the rat forebrain". Arzneimittel-Forschung. 48 (7 ... σ receptor agonist Tianeptine‡ (Stablon, Coaxil, Tatinol) - atypical μ-opioid receptor agonist Legend: † indicates products ... March 2008). "Delta-opioid receptors are critical for tricyclic antidepressant treatment of neuropathic allodynia". Biological ... Nonetheless due to their atypical MOA, amineptine and tianeptine (dopamine reuptake inhibition and μ-opioid receptor agonism, ...
*  Trevena Inc
The company has disclosed specific interests in the mu Opioid receptor and kappa Opioid receptor. The company raised an ... This avoids the addiction potential of drugs that activate the mu opioid receptor. Other delta opioid-targeting drugs are known ... TRV734 is an oral follow-up to the injected TRV130 mu-opioid biased ligand program. While it binds to the same receptors as ... Trevena's leading drug candidate is Oliceridine (TRV130), a G protein-biased ligand binding to the mu opioid receptor for the ...
*  N-Phenethylnormorphine
"Molecular Docking Reveals a Novel Binding Site Model for Fentanyl at the mu-Opioid Receptor". Journal of Medicinal Chemistry. ... showing that the phenethyl group extends out to reach an additional binding point deeper inside the μ-opioid receptor cleft, ... "Molecular Modeling of Opioid Receptor-Ligand Complexes". Progress in Medicinal Chemistry. Progress in Medicinal Chemistry. 40: ... N-Phenethylnormorphine is an opioid analgesic drug derived from morphine by replacing the N-methyl group with β-phenethyl. It ...
*  Inverse agonist
The opioid antagonists naloxone and naltrexone are also partial inverse agonists at mu opioid receptors.[citation needed] ... Agonist Receptor antagonist Kenakin T (April 2004). "Principles: receptor theory in pharmacology". Trends in Pharmacological ... In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a ... A prerequisite for an inverse agonist response is that the receptor must have a constitutive (also known as intrinsic or basal ...
*  Cyprodime
2. (−)-N- (cyclopropylmethyl)- 4,14-dimethoxymorphinan- 6-one, a selective mu opioid receptor antagonist. Journal of Medicinal ... Cyprodime is a selective opioid antagonist which blocks the μ-opioid receptor, but without affecting the δ-opioid or κ-opioid ... Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays. ... in contrast to better known opioid antagonists such as naloxone which block all three opioid receptor subtypes. Samidorphan ...
*  GPM6A
"Membrane glycoprotein M6A promotes mu-opioid receptor endocytosis and facilitates receptor sorting into the recycling pathway ...
*  Animal psychopathology
Mu and Kappa receptors are associated with aversion behaviors and Mu receptor density is greater in tethered sows than sows ... 1996). "Brain opioid receptors in relation to stereotypies, inactivity, and housing in sows". Physiol Behav. 59 (4-5): 769-75. ... experienced a decrease both in Mu and Kappa receptor density in the brain suggesting that inactivity increases Mu receptor ... Tasty food can activate opioid receptors in the ventral tegmental area and thereby stimulate cells that release dopamine in the ...
*  Enkephalin
The receptors for enkephalin are the delta opioid receptors and mu opioid receptors. Opioid receptors are a group of G-protein- ... mu receptors), endomorphins, and nociceptin/orphanin FQ. The opioid receptors are ~40% identical to somatostatin receptors ( ... coupled receptors, with other opioids as ligands as well. The other endogenous opioids are dynorphins (that bind to kappa ... The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. ...