"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 ...
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 ...
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, ...
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 ...
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 ...
... mu- and delta-opioid receptors correspondingly; AdrR - adrenergic receptors. Clark, L.A., Watson, D., & Mineka, S. (1994). ... whereas the three emotionality-related traits emerge as a dysregulation of opioid receptors systems that have direct control ... It became clear that an impressive diversity of neurotransmitters and their receptors is necessary to meet a wide range of ...
It is an allosteric modulator of the μ- and δ-opioid receptors as well. Cannabidiol's pharmacological effects have additionally ... Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E (February 2006). "Cannabidiol is an allosteric modulator at mu- and delta- ... It may potentiate THC's effects by increasing CB1 receptor density or through another CB1 receptor-related mechanism. ... opioid receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 372 (5): 354-61. doi:10.1007/s00210-006-0033-x. PMID ...
Méndez M, Morales-Mulia M (2008). "Role of mu and delta opioid receptors in alcohol drinking behaviour". Curr Drug Abuse Rev. 1 ... and NMDA receptors, the glycine receptor, the nicotinic acetylcholine receptors, the serotonin 5-HT3 receptor, voltage-gated ... NMDA receptor negative allosteric modulator Increased levels of dopamine and endogenous opioids in the mesolimbic pathway, ... to other actions AMPA receptor negative allosteric modulator Kainate receptor negative allosteric modulator Glycine receptor ...
... and δ-opioid receptors. Due to its partial agonistic activity, THC appears to result in greater downregulation of cannabinoid ... Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E (February 2006). "Cannabidiol is an allosteric modulator at mu- and delta- ... In populations of low cannabinoid receptor density, THC may act to antagonize endogenous agonists that possess greater receptor ... opioid receptors". Naunyn Schmiedebergs Arch. Pharmacol. 372 (5): 354-61. doi:10.1007/s00210-006-0033-x. PMID 16489449. ...
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/ ...
... (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- ...
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. ...
Evidence which suggests that mu and delta opioid receptors possess different stereochemical requirements". Journal of Medicinal ... It binds to and activates both the μ- and δ-opioid receptors, with the (S)-isomer being the more potent of its two enantiomers ... Isomethadone (INN, BAN; Liden), also known as isoamidone, is a synthetic opioid analgesic and antitussive related to methadone ... June 1982). "Synthesis, X-ray crystallographic determination, and opioid activity of erythro-5-methylmethadone enantiomers. ...
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. ...
... 1-8 is an agonist at the mu-, kappa-, and delta-opioid receptors; it has the highest binding affinity for the kappa- ... opioid receptor. Dynorphin 1-13 - Compound Summary, PubChem. "Dynorphin A 1-8". HMDB Version 4.0. Human Metabolome Database. 27 ... Dynorphin A is a form of dynorphin and an endogenous opioid peptide with the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg- ...
9-diazabicyclo3.3.1nonanes as mu-opioid receptor agonists. Effects on mu-affinity of arylalkenyl chain modifications". ... Barlocco, D; Cignarella, G; Vianello, P; Villa, S; Pinna, G. A.; Fadda, P; Fratta, W (1998). "Synthesis and mu-opioid receptor ... and mu-opioid receptor affinity of N-3(9)-arylpropenyl-N-9(3)-propionyl-3,9-diazabicycl". Farmaco. 55 (8): 553-62. doi:10.1016/ ... octanes with mu and delta opioid receptors". Pharmacological research communications. 20 (5): 383-94. doi:10.1016/s0031-6989(88 ...
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 ...
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 ...
"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. ...
... -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". ...
"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 ...
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 ...
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 ...
Three known kinds of opioid receptors have been identified: mu (μ), kappa (κ) and delta (δ). Synthetic opioid and opioid- ... endogenous opioid neurotransmitters), which bind to mu opioid receptors on the axons of incoming C and A-delta fibers carrying ... The activation of the mu-opioid receptor inhibits the release of substance P from these incoming first-order neurons and, in ... derivative drugs activate these receptors (possibly by acting on the PAG directly, where these receptors are densely expressed ...
"Membrane glycoprotein M6A promotes mu-opioid receptor endocytosis and facilitates receptor sorting into the recycling pathway ...
D2 receptor,[15][16] reuptake transporter), serotonin receptors (5HT1A, 5HT2A, reuptake transporter) opioid receptors (mu) and ... "Imaging cortical dopamine D1 receptors using 11C NNC112 and ketanserin blockade of the 5-HT 2A receptors". J Cereb Blood Flow ... Mefway for serotonin 5HT1A receptors, [18F] Nifene for nicotinic acetylcholine receptors or enzyme substrates (e.g. 6-FDOPA for ... Studies have been performed examining the state of these receptors in patients compared to healthy controls in schizophrenia, ...