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Topic: Opioid receptor

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In the News (Sun 21 Jul 19)

 Molecular Modeling of Opioid Analgesics
Furthermore, ligands that are recognized and bound by all three types of opioid receptors can have differential efficacy in activating each receptor, acting as agonists for one type of receptor and as antagonists for another.
An example of an extension point is the position of a proton donor in the receptor expressed as an extension of a carbonyl group acting as the hydrogen-bond acceptor in the ligand.
The possible modes of receptor activation were investigated by comparing the structures of the computer-generated agonist- and antagonist-receptor complexes and the ligand-free receptor.
pubs.acs.org /hotartcl/mdd/99/dec/loew.html   (2021 words)

 Opioid Review   (Site not responding. Last check: 2007-10-12)
receptor was accepted as a member of the “family” of opioid receptors on the basis of its structural homology towards the classical types, there is no corresponding pharmacological homology.
However, different responses evoked in different cell types in response to activation of different opioid receptors or even in response to activation of the same receptor are likely to reflect changes in the expression of G proteins and effector systems between cell types rather than any inherent differences in the properties of the receptors themselves.
Among the receptors for the many neuropeptides that exist in the nervous system, the opioid receptors are unique in that there existed before the discovery of the natural agonists, an abundance of non-peptide ligands with which the pharmacology of the receptors was already defined.
www.tocris.com /opioidrev.htm   (4913 words)

 5-HT4 receptor agonists and delta -opioid receptor antagonists act synergistically to stimulate colonic propulsion -- ...
Increase in velocity of propulsion induced by opioid receptor antagonists.
Inhibition of cholinergic transmission by opiates in ileal myenteric plexus is mediated by kappa receptor.
Regulatory role of enteric mu and kappa opioid receptors in the release of acetylcholine and norepinephrine from guinea pig ileum.
ajpgi.physiology.org /cgi/content/full/275/5/G979   (3096 words)

 Dopamine's effect on opioids
A wide-range of opioid agonists (drugs that activate a receptor by binding to it), including opium, heroin, morphine, percodan, and codeine, have addictive properties and are commonly abused.
Opioid receptors are distributed throughout the brain and spinal cord and are known to mediate a number of activities including analgesia, species-typical behavior, and reward.
Cloning demonstrates that the receptors are usually G protein-linked receptors imbedded in the plasma membrane of neurons (Satoh and Minami, 1995).
www.macalester.edu /psychology/whathap/UBNRP/Dopamine/opioids.html   (2062 words)

 Pain Medicine & Palliative Care: Pain Medicine
These receptors are the sites of action for the endorphins, compounds that already exist in the body and are chemically related to the opioid drugs that are prescribed for pain.
Opioids are typically first-line if the pain is severe and is expected to be short-lived, like post-surgical pain, and if the pain is associated with a progressive incurable illness.
Although opioids can make people sleepy and cloud their thinking, this side effect is usually temporary and long-term therapy is usually associated with normal thinking.
www.stoppain.org /pain_medicine/content/medication/opioids.asp   (2273 words)

 Kappa Opioid Receptors   (Site not responding. Last check: 2007-10-12)
Three different opioid receptor subtypes - kappa (k), delta (d), and mu (m)- were first identified by their different selectivities for various naturally occurring alkaloid opioid ligands, and subsequently confirmed by molecular cloning.
The amino acid sequences of the opioid receptor subtypes are ~70% homologous.
The kappa opioid receptor is widely distributed throughout the brain, the spinal cord and other organs, as well as in lymphocytes.
www.unet.univie.ac.at /~a0001355/kappa   (1481 words)

 Volume X   (Site not responding. Last check: 2007-10-12)
By the end of the 1960s, it was clear that the receptors activated by opioids are of several types, distinguishable on the basis of their selective binding of prototype reagents, and could be fully or partially activated.
Receptor studies using synthetic enkephalins led to recognition of another opioid receptor, termed the “delta” opioid receptor on the basis of its discovery in vas deferens tissue of the mouse.
Although a metabolite of tramadol expresses higher affinity for mu opioid receptors than does the parent compound, a major reason for tramadol’s effectiveness is its additional ability to inhibit the reuptake of serotonin and norepinephrine.
www.iasp-pain.org /PCU02-4.html   (2703 words)

 Probing the role of the delta opioid receptor in alcohol consumption
The body's endogenous opioid system has traditionally been linked with peptides such as enkephalins and endorphins, which influence the brain's reward pathway to act as the body's natural response to pain.
Opioids are known to moderate the activity of dopamine pathways, and it is possible that alcohol addiction is partly associated with alterations in opiate receptor-mediated processes.
"Because this drug influences all three of the known opioid receptor subtypes, mu, delta and kappa," she said, "a worthwhile endeavor is to examine the specific roles that each of the opiate receptor subtypes might play in alcohol addiction.
www.eurekalert.org /pub_releases/2001-09/ace-ptr091001.php   (927 words)

 Heterodimeric Opioid G-Protein Coupled Receptor
Other types of opioid receptors have been postulated but are less well characterized and have not been cloned.
Their current research relates to the discovery that the opioid receptors are capable of forming functional heterodimers.
Understanding possible differences in the affinity and efficacy of various agonists and antagonists for the various forms of these receptors and their differential ability to transmit signals will help explain the differences in the physiological responses induced and will be instrumental in identifying and developing novel therapeutic compounds and formulations.
www.med.nyu.edu /oil/tech/therapeutics/topioid.html   (316 words)

 Neuropharmacology of Endogenous Opioid Peptides
The binding of ligands to all of the three well-accepted types of opioid receptors (mu, delta, and kappa) is modulated by the addition of GTP to radioligand binding assays.
The distinction between the effects of exogenously applied opioids and effects of endogenously released opioid peptides is important, because it is not necessarily true that a given population of receptors occupied by bath-applied drug are relevant targets for opioid peptides released from endogenous stores.
Less well defined is the modulatory role of opioids in the neural circuit where questions about the physical dimensions of the "opioid peptide synapse" and the kinetics of endogenous opioid action should be resolved to provide a clearer insight to the role of these neuropeptides in synaptic function.
www.acnp.org /g4/GN401000050/CH050.html   (6459 words)

 Chronic {micro}-Opioid Receptor Stimulation in Humans Decreases Muscle Sympathetic Nerve Activity -- Kienbaum et al. ...
Chronic µ-opioid receptor stimulation was associated with a marked parallel decrease in both MSA and norepinephrine plasma concentration.
Acute detoxification of opioid addicted patients during propofol or methohexital anesthesia: a comparison of withdrawal symptoms, neuroendocrine, metabolic, and cardiovascular patterns.
Kimura T, Katoh M, Satoh S. Inhibition by opioid agonists and enhancement by antagonists of the release of catecholamines from the dog adrenal gland in response to splanchnic nerve stimulation: evidence for the functional role of opioid receptors.
circ.ahajournals.org /cgi/content/full/103/6/850   (3310 words)

 In vivo activation of a mutant {micro}-opioid receptor by antagonist: Future direction for opiate pain treatment ...
expression of the µ-opioid receptor and the ligand-binding characteristics
The ability of opioid agonists to elicit antinociceptive responses seems to be dependent on the µ-opioid receptor level.
-opioid receptors in the inhibition of the chronic morphine
www.pnas.org /cgi/content/full/100/4/2117   (4138 words)

 Mechanisms of Agonist-Induced Down-Regulation of the Human kappa -Opioid Receptor: Internalization Is Required for ...
the receptors are trafficked to lysosomes for degradation.
Jin W, Terman GW and Chavkin C (1997) Kappa opioid receptor tolerance in the guinea pig hippocampus.
Krupnick JG and Benovic JL (1998) The role of receptor kinases and arrestins in G protein-coupled receptor regulation.
molpharm.aspetjournals.org /cgi/content/full/58/4/795   (5064 words)

 Role of delta -opioid receptor agonists on infarct size reduction in swine -- Sigg et al. 282 (6): 1953 -- AJP - Heart ...
Opposing effects on infarction of delta and kappa opioid receptor activation in the isolated rat heart: implications for ischemic preconditioning.
Opioids confer myocardial tolerance to ischemia: interaction of delta agonists and antagonists.
Opioid receptor contributes to ischemic preconditioning through protein kinase C activation in rabbits.
ajpheart.physiology.org /cgi/content/full/282/6/H1953   (4584 words)

 Cloning, heterologous expression and pharmacological characterization of a kappa opioid receptor from the brain of the ...
Cloning, heterologous expression and pharmacological characterization of a kappa opioid receptor from the brain of the rough-skinned newt, Taricha granulosa -- Bradford et al.
Articles by Bradford, C S. Articles by Moore, F. Cloning, heterologous expression and pharmacological characterization of a kappa opioid receptor from the brain of the rough-skinned newt, Taricha granulosa
opioid receptor is expressed in amphibians and that the pharmacology
jme.endocrinology-journals.org /cgi/content/abstract/34/3/809   (249 words)

 Orphanin FQ/Nociceptin-Mediated Desensitization of Opioid Receptor-Like 1 Receptor and {micro} Opioid Receptors ...
Chen Y and Yu L (1994) Differential regulation by cAMP-dependent protein kinase and protein kinase C of the µ opioid receptor coupling to a G protein-activated K+ channel.
opioid receptors are differentially desensitized by the coexpression of
Li AH and Wang H-L (2001) G protein-coupled receptor kinase 2 mediates µ opioid receptor desensitization in GABAergic neurons of the nucleus raphe magnus.
jpet.aspetjournals.org /cgi/content/full/302/2/502   (5417 words)

 Erowid Salvia Divinorum Vault : Salvinorin Activity at Kappa Opioid Receptor
By using cloned cells which expressed a variety of neurotransmitter receptor types, bathing them in a solution with salvinorin A in it, and then using radio-labeled chemicals known to bind to the given receptor, they were able to see if the salvinorin kept the other chemical from 'sticking'.
Dr Roth's lab is one of the most active in doing this type of neuropharmalogical receptor screening and more info about this type of work can be found at http://pdsp.cwru.edu/nimh/5ht.html.
Interestingly, the kappa opioid receptor was previously known for its ability to cause strange psychoactive effects which have been called 'hallucinogenic'.
www.erowid.org /plants/salvia/salvia_info5.shtml   (487 words)

 Methods of screening modulators of opioid receptor activity (US6432652)
Genes encoding opioid receptors (including opioid-like receptor (ORL) proteins) can be retrieved from vertebrate libraries using the murine probe disclosed herein under low-stringency conditions.
(a) incubating cells displaying opioid receptor in the presence and absence of the candidate substance under conditions suitable for detection of activation of said opioid receptor, and
wherein said opioid receptor is a mammalian opioid receptor which is able to transduce a signal when contacted with an opioid agonist and is encoded by a nucleotide sequence which hybridizes under conditions of high stringency to the nucleotide sequence of SEQ.
www.delphion.com /details?pn=US06432652__   (618 words)

 Discovery of the First Potent and Selective Small Molecule Opioid Receptor-like (ORL1) Antagonist: ...
ORL1 is a member of the G-protein coupled receptor superfamily with a high degree of amino acid sequence homology to the classical opioid receptors.
The amino acid sequence of NC/OFQ has notable homology to that of opioid peptide dynorphin A; however, this new peptide does not show significant affinity to the other opioid receptors.
]nociceptin(1-13)-NH is an agonist of the nociceptin (ORL1) receptor.
pubs.acs.org /cgi-bin/jtextd?jmcmar/42/i25/html/jm990517p.html   (1890 words)

 CD28 Costimulation Induces {delta} Opioid Receptor Expression During Anti-CD3 Activation of T Cells -- Nguyen and ...
Opioid modulation of immune responses: effects on phagocyte and lymphoid cell populations.
opioid receptors by splenocytes from SEB-treated mice and effects on phosphorylation of MAP kinase.
Opioid receptor gene: cytokine response element and the effect of cytokines.
www.jimmunol.org /cgi/content/full/168/9/4440   (3917 words)

 CORD Structural Models   (Site not responding. Last check: 2007-10-12)
On this page we have made available three-dimensional models of the delta, kappa, and mu opioid receptor transmembrane regions in PDB format.
Metzger, T.G., Paterlini, M.G., Portoghese, P.S., Ferguson, D.M. Application of the Message-Address Concept to the Docking of Naltrexone and Selective Naltrexone-Derived Opioid Antagonists into Opioid Receptor Models.
(7) Liu, J.; Schoneberg, T.; van Rhee, M.; Wess, J. Mutational Analysis of the Relative Orientation of Transmembrane Helices I and VII in G Protein-coupled Receptors.
www.opioid.umn.edu /strumod.html   (488 words)

 Medical Dictionary: Opioid receptor - WrongDiagnosis.com
Opioid receptor : family of cell surface receptors which mediate opiate drug effects on neurons, lymphocytes, macrophages, and other cells; may or may not coincide with neuropeptide receptors; some are G protein coupled to calcium channel inhibition.
The term Opioid receptor can be used for:
Other terms that may be related to Opioid receptor:
www.wrongdiagnosis.com /medical/opioid_receptor.htm   (209 words)

 The molecular basis of opioid receptor function -- Simonds 9 (2): 200 -- Endocrine Reviews
least three opioid receptor subtypes mediating the diverse effects of
and kappa-opioid receptors represent recent discrete molecular entities.
Purification and affinity labeling of receptor subunits are beginning to
edrv.endojournals.org /cgi/content/abstract/9/2/200   (508 words)

 GM1 Ganglioside-induced Modulation of Opioid Receptor-mediated Functions -- CRAIN and SHEN 845 (1): 106 -- Annals of ...
GM1 Ganglioside-induced Modulation of Opioid Receptor-mediated Functions -- CRAIN and SHEN 845 (1): 106 -- Annals of the New York Academy of Sciences
opioid agonists for eliciting excitatory effects is markedly
opioid supersensitivity of GM1-treated DRG neurons is due primarily
www.annalsnyas.org /cgi/content/abstract/845/1/106   (361 words)

 Mosberg Lab - Opioid receptor-ligand complexes
Our complementary studies elucidating the bioactive conformations of opioid ligands at delta and mu receptors and the development of accurate structural models for these receptors have allowed us to propose models of the ligand-receptor complexes.
Complementarity of delta opioid ligand pharmacophore and receptor models.
Synthesis of Biologically Active Opioids for in vivo Studies
mosberglab.phar.umich.edu /projects/proj3.php   (107 words)

 Opioid receptor genes (US6265563)
    Genes encoding opioid receptors can be retrieved from vertebrate libraries using the murine probe disclosed herein under low-stringency conditions.
, pH 7.2; 1% SDS; and 1 mM EDTA for one hour at 68° C. and specifically identifies a mammalian kappa opioid receptor clone in a cDNA library.
Show 1 U.S. patent(s) that reference this one
www.delphion.com /details?pn=US06265563__   (444 words)

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