Genomes and Genes
Summary: A narcotic antagonist similar in action to NALOXONE. It is used to remobilize animals after ETORPHINE neuroleptanalgesia and is considered a specific antagonist to etorphine.
Publications156 found, 100 shown here
- The role of opioids in restless legs syndrome: an [11C]diprenorphine PET studySarah von Spiczak
Division of Neuroscience and MRC Clinical Sciences Centre, Faculty of Medicine, Imperial College, London, UK
Brain 128:906-17. 2005..receptor availability in 15 patients with primary RLS and 12 age-matched healthy volunteers using PET and [11C]diprenorphine, a non-selective opioid receptor radioligand...
- A combined [11C]diprenorphine PET study and fMRI study of acupuncture analgesiaDarin D Dougherty
Psychiatric Neuroimaging Research Program, Department of Psychiatry, Massachusetts General Hospital MGH, Harvard Medical School, MA 02129, USA
Behav Brain Res 193:63-8. 2008..functional magnetic resonance imaging signal changes in the orbitofrontal cortex, insula, and pons and [11C]diprenorphine positron emission tomography signal changes in the orbitofrontal cortex, medial prefrontal cortex, insula, ..
- Differential involvement of P-glycoprotein (ABCB1) in permeability, tissue distribution, and antinociceptive activity of methadone, buprenorphine, and diprenorphine: in vitro and in vivo evaluationHazem E Hassan
Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, Maryland, USA
J Pharm Sci 98:4928-40. 2009..The objective of this study was to evaluate the P-gp affinity status of methadone, buprenorphine and diprenorphine to predict P-gp-mediated drug-drug interactions and to determine a better candidate for management of opioid ..
- Using [11C]diprenorphine to image opioid receptor occupancy by methadone in opioid addiction: clinical and preclinical studiesJan K Melichar
Psychopharmacology Unit, University of Bristol, Whitson St, Bristol, BS1 3NY, UK
J Pharmacol Exp Ther 312:309-15. 2005..and occupation of opioid receptors in brain using the positron emission tomography (PET) radioligand [(11)C]diprenorphine in humans and rats...
- Opiate receptors in the human spinal cord: a detailed anatomical study comparing the autoradiographic localization of [3H]diprenorphine binding sites with the laminar pattern of substance P, myelin and nissl stainingR L Faull
Neuroscience 20:395-407. 1987..quantitative autoradiographic methods following the incubation of fresh, unfixed cryostat sections with [3H]diprenorphine. In order to precisely localize the distribution of receptors in the spinal cord, the laminar anatomy of the ..
- Central poststroke pain and reduced opioid receptor binding within pain processing circuitries: a [11C]diprenorphine PET studyFrode Willoch
Department of Neurology, Technische Universitat Munchen, Klinikum rechts der Isar, Ismaningerstr 22, 81675 Munich, Germany
Pain 108:213-20. 2004..after lesions in the brain stem, thalamus or parietal cortex and twelve healthy volunteers underwent a [11C]diprenorphine positron emission tomography study...
- Functional complementation and the analysis of opioid receptor homodimerizationGeraldine Pascal
Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
Mol Pharmacol 68:905-15. 2005..Because the amino acids modified in the opioid receptors are highly conserved in most rhodopsin-like receptors, this approach should be widely applicable to study the existence and molecular basis of receptor dimerization...
- Opioid binding in DYT1 primary torsion dystonia: an 11C-diprenorphine PET studyAlan L Whone
Division of Neuroscience and MRC Clinical Sciences Centre, Faculty of Medicine, Imperial College, Hammersmith Hospital, London, United Kingdom
Mov Disord 19:1498-503. 2004..Moreover, a previous 11C-diprenorphine PET study investigating levodopa-induced dyskinesias found reduced opioid receptor availability in PD with but ..
- Low sensitivity of the positron emission tomography ligand [11C]diprenorphine to agonist opiatesSusan P Hume
Hammersmith Imanet Ltd, Hammersmith Hospital, London, United Kingdom
J Pharmacol Exp Ther 322:661-7. 2007..of the micro-opioid agonist, methadone, measured in vivo using positron emission tomography (PET) with [(11)C]diprenorphine and subsequently used rats to obtain experimental data in support of a high receptor reserve hypothesis (..
- Brain opioid receptor binding in early abstinence from alcohol dependence and relationship to craving: an [11C]diprenorphine PET studyTim M Williams
Psychopharmacology Unit, Dorothy Hodgkin Building, University of Bristol, Whitson Street, Bristol, UK
Eur Neuropsychopharmacol 19:740-8. 2009..We used PET with the non-selective tracer [11C]diprenorphine to examine opioid receptor binding in early abstinence from alcohol dependence and the relationship to craving...
- Cerebral decreases in opioid receptor binding in patients with central neuropathic pain measured by [11C]diprenorphine binding and PETAnthony K P Jones
Human Pain Research Laboratory, University of Manchester Rheumatic Diseases Centre, Clinical Sciences Building, Hope Hospital, Eccles Old Road, Salford M6 8HD, UK
Eur J Pain 8:479-85. 2004..If confirmed, these findings may explain why certain patients with CNP require high doses of synthetic opiates to achieve optimum analgesia. The findings also raise the possibility of new pharmacological approaches to treatment...
- Antagonist efficacy in MORS196L mutant is affected by the interaction between transmembrane domains of the opioid receptorPatricia A Claude-Geppert
Department of Pharmacology, Medical School, University of Minnesota, Minneapolis, MN 55455 0217, USA
J Pharmacol Exp Ther 313:216-26. 2005..These data suggest that the efficacy of opioid antagonists in the Ser196 mutant can be affected by the interaction between TM1 and TM7...
- Quantification of [18F]diprenorphine kinetics in the human brain with compartmental and non-compartmental modeling approachesMary E Spilker
Nuklearmedizinische Klinik und Poliklinik, Klinikum rechts der Isar, Technische Universitat Munchen, Munchen, Germany
Neuroimage 22:1523-33. 2004..BP values were also found to correlate with DV values; however, these results should be interpreted with the understanding that specific binding in the reference region (occipital region) may exist...
- Characterization of specific opioid binding sites in neural membranes from the myenteric plexus of porcine small intestineDeWayne Townsend
Department of Veterinary Pathobiology, College of Veterinary Medicine, University of Minnesota, St Paul, Minnesota 55108 6010, USA
J Pharmacol Exp Ther 308:385-93. 2004..The nonselective OPR antagonist [3H]diprenorphine bound to a single, high-affinity site in myenteric neural membrane homogenates...
- [Binding characteristics of new synthesized opioid receptor ligands to cloned mu opioid receptors stably expressed in CHO cell]Ping Hu
Department of Pharmacology, Institute of Basic Medical Sciences, CAMS, PUMC, Beijing 100005, China
Zhongguo Yi Xue Ke Xue Yuan Xue Bao 25:79-82. 2003..To determine the affinity of new opioid receptor ligands to cloned mu opioid receptors stably expressed in CHO cell...
- Long-term interactions between opioid and cannabinoid agonists at the cellular level: cross-desensitization and downregulationMa anit Shapira
Department of Physiology and Pharmacology, Sackler Faculty of Medicine, Tel Aviv University, Tel Aviv 69978, Israel
Brain Res 960:190-200. 2003..of the cannabinoid ligand [3H]CP55,940, while DALN failed to reduce the binding of the opioid ligand [3H]diprenorphine. In contrast to the asymmetric desensitization in HEK-293 cells, COS-7 cells presented a two-way cross-..
- (-)U50,488H [(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide] induces internalization and down-regulation of the human, but not the rat, kappa-opioid receptor: structural basis for the differential regulationFengqin Zhang
Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, USA
J Pharmacol Exp Ther 302:1184-92. 2002..In addition, the trafficking of the FLAG-rkorN358S mutant seems to be more complex than the rkor and the hkor...
- Changes in respiratory function following the intramuscular administration of etorphine to boer goats (Capra hircus)P E Buss
Department of Companion Animal Surgery, Faculty of Veterinary Science, University of Pretoria, Onderstepoort, South Africa
J S Afr Vet Assoc 72:137-42. 2001..The effectiveness of diprenorphine (M5050, Logos Agvet) (3 mg/l mg etorphine) as an antagonist of the physiological changes induced by the ..
- Inverse agonist up-regulates the constitutively active D3.49(164)Q mutant of the rat mu-opioid receptor by stabilizing the structure and blocking constitutive internalization and down-regulationJ Li
Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
Mol Pharmacol 60:1064-75. 2001..49(164)Q mutant and the mechanisms underlying the effect of naloxone. Naloxone pretreatment up-regulated [(3)H]diprenorphine binding and protein expression of the D3...
- Comparison of the amino acid residues in the sixth transmembrane domains accessible in the binding-site crevices of mu, delta, and kappa opioid receptorsW Xu
Department of Pharmacology and Center for Substance Abuse Research and Fels Institute for Molecular Biology and Cancer Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
Biochemistry 40:8018-29. 2001..47) of each receptor were mutated to cysteine, 1 at a time. Most mutants retained binding affinities for [3H]diprenorphine, a nonselective opioid antagonist, similar to that of the template receptors...
- Alterations in cortical and basal ganglia levels of opioid receptor binding in a rat model of l-DOPA-induced dyskinesiaP A Johansson
Department of Physiological Sciences, Neurobiology Division, Wallenberg Neuroscience Centre, University of Lund, , Lund, S-223 62, Sweden
Neurobiol Dis 8:220-39. 2001....
- Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligandsWen Lian Wu
Schering Plough Research Institute, 2015 Galloping Hill Road, MS 2800, Kenilworth, NJ 07033 0539, USA
Bioorg Med Chem Lett 12:3157-60. 2002..Structure-activity relationships have been investigated at the azetidine N and the alkyl side chain sites. Several potent and selective analogues have been identified...
- Binding profile of the endogenous novel heptapeptide Met-enkephalin-Gly-tyr in zebrafish and rat brainV Gonzalez-Nunez
Department of Biochemistry and Molecular Biology, Faculty of Medicine, University of Salamanca, Avda Alfonso X El Sabio, s n 37007 Salamanca, Spain
J Pharmacol Exp Ther 314:862-7. 2005..Therefore, we can deduct that some of the MEGY binding sites should not be considered classical opioid sites...
- Opioid antagonists differ according to negative intrinsic efficacy in a mouse model of acute dependenceEllen A Walker
Department of Pharmaceutical Sciences, Temple University School of Pharmacy, 3307 North Broad Street, Philadelphia, PA 19140, USA
Br J Pharmacol 145:975-83. 2005..g) were acutely treated with 56 or 180 mg kg(-1) morphine 4 h prior to injection with naloxone, naltrexone, diprenorphine, nalorphine, or naloxonazine. Vertical jumping, paw tremors, and weight loss were recorded...
- Opioid receptor PET reveals the psychobiologic correlates of reward processingMathias Schreckenberger
Department of Nuclear Medicine, Johannes Gutenberg University, Mainz, Germany
J Nucl Med 49:1257-61. 2008....
- Agonist treatment did not affect association of mu opioid receptors with lipid rafts and cholesterol reduction had opposite effects on the receptor-mediated signaling in rat brain and CHO cellsPeng Huang
Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, USA
Brain Res 1184:46-56. 2007..5 M Na(2)CO(3) buffer and fractionated through sucrose density gradients. Western blot and [(3)H]diprenorphine binding showed that approximately 70% of MOR in CHO-HA-rMOR was present in low-density (5-20% sucrose) ..
- Balancing bias, reliability, noise properties and the need for parametric maps in quantitative ligand PET: [(11)C]diprenorphine test-retest dataAlexander Hammers
MRC Clinical Sciences Centre and Division of Neuroscience, Faculty of Medicine, Imperial College, Hammersmith Hospital, DuCane Road, London, UK
Neuroimage 38:82-94. 200711)C]diprenorphine (DPN) is a non-subtype selective opioid receptor PET ligand with slow kinetics and no region devoid of specific binding. Parametric maps are desirable but have to overcome high noise at the voxel level...
- A select set of opioid ligands induce up-regulation by promoting the maturation and stability of the rat kappa-opioid receptor in human embryonic kidney 293 cellsKENNETH M WANNEMACHER
Graduate School of Biomedical Science, University of Medicine and Dentistry of New Jersey New Jersey Medical School, Newark, New Jersey, USA
J Pharmacol Exp Ther 323:614-25. 2007..of rKOR cells with naltrexone for 24 h increased the B(max) >3-fold, with no change in the affinity of [(3)H]diprenorphine. Two immunoreactive receptor species were present in cell lysates: naltrexone treatment caused a >3-fold ..
- Membrane partitioning of various delta-opioid receptor forms before and after agonist activations: the effect of cholesterolAurore André
IPBS, MR5089 CNRS UPS, Toulouse Cedex 4, France
Biochim Biophys Acta 1778:1483-92. 2008..iv) An increase in the quantity of DOR* was observed upon agonist addition. (v) This DRM relocation is prevented by uncoupling the receptor-G-protein interaction...
- Upregulation of opioid receptor binding following spontaneous epileptic seizuresAlexander Hammers
MRC Clinical Sciences Centre and Division of Neuroscience, Faculty of Medicine, Imperial College, Hammersmith Hospital, London, UK
Brain 130:1009-16. 2007..and compared their postictal binding of the non-subtype selective opioid receptor PET radioligand [11C]diprenorphine (DPN), quantified as a volume-of-distribution (VD), with interictal binding and with binding changes in 14 ..
- Differential brain opioid receptor availability in central and peripheral neuropathic painJoseph Maarrawi
INSERM EMI 342 Central Integration of pain, 59 Bd Pinel, 69394 Lyon and St Etienne, France
Pain 127:183-94. 2007This study used positron emission tomography (PET) and [11C]diprenorphine to compare the in vivo distribution abnormalities of brain opioid receptors (OR) in patients with peripheral (n=7) and central post-stroke pain (CPSP, n=8), ..
- The opioid ligand binding of human mu-opioid receptor is modulated by novel splice variants of the receptorHack Sun Choi
Department of Pharmacology, Medical School, University of Minnesota, Minneapolis, MN 55455, USA
Biochem Biophys Res Commun 343:1132-40. 2006..In a receptor binding assay, cells expressing the SV1 and SV2 do not exhibit binding to [(3)H]diprenorphine. The formations of MOR.SV1 and MOR...
- Molecular cloning, tissue distribution and chromosomal localization of a novel member of the opioid receptor gene familyY Chen
Department of Medical and Molecular Genetics, Indiana University School of Medicine, Indianapolis 46202
FEBS Lett 347:279-83. 1994..and the other opioid receptors, expression studies of this clone in COS-7 cells did not show binding to [3H]diprenorphine, a ligand that binds to the other three opioid receptors...
- Direct measurements of in situ interactions of rat brain opioid receptors with the guanine nucleotide-binding protein GoZ Georgoussi
Institute of Biology, National Center for Scientific Research, Demokritos, Athens, Greece
Mol Pharmacol 44:62-9. 1993..interacts with delta and mu but not significantly with kappa receptors) to displace specific binding of [3H] diprenorphine (which binds to all of these sites), demonstrating a clear interaction of the mu and delta receptors with one ..
- Optimal duration of PET studies with 18F-fluoroethyl-diprenorphineHenning Boecker
Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universitat Munchen, Munich, Germany
J Nucl Med 46:2092-6. 2005..18F-FDPN) provides enhanced flexibility to PET studies of the opioidergic system because the label has a longer half-life than the label of 11C-diprenorphine. Here we evaluated the ideal length of PET studies with 18F-FDPN.
- What to learn from in vivo opioidergic brain imaging?Till Sprenger
Department of Neurology, Technical University, Moehlstr 28, 81675 Munich, Germany
Eur J Pain 9:117-21. 2005..mainly the mu-opioidergic agonist [(11)C]-carfentanil and the unspecific opioid receptor antagonist [(11)C]-diprenorphine are applied...
- Cholesterol reduction by methyl-beta-cyclodextrin attenuates the delta opioid receptor-mediated signaling in neuronal cells but enhances it in non-neuronal cellsPeng Huang
Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, United States
Biochem Pharmacol 73:534-49. 2007..Cholesterol-dependent association of caveolin-1 with and the resulting inhibition of G proteins may be a contributing factor...
- Discrimination of a single dose of morphine followed by naltrexone: substitution of other agonists for morphine and other antagonists for naltrexone in a rat model of acute dependenceStephen G Holtzman
Department of Pharmacology, Emory University School of Medicine, Atlanta, Georgia 30322, USA
J Pharmacol Exp Ther 304:1033-41. 2003..Antagonists with no intrinsic efficacy at mu-opioid receptors (naloxone and diprenorphine) substituted completely for naltrexone, whereas those with some efficacy (nalorphine and levallorphan) ..
- The effects of sigma, PCP, and opiate receptor ligands in rats trained with ibogaine as a discriminative stimulusS Helsley
Department of Pharmacology and Toxicology, School of Medicine and Biomedical Sciences, State University of New York at Buffalo, 14214 3000, USA
Pharmacol Biochem Behav 59:495-503. 1998..9%), (+/-)-pentazocine (73.9%), nalorphine (70.4%), and diprenorphine (75.0%) indicating a potential role for opiate receptors in the ibogaine stimulus...
- The antiproliferative effect of opioid receptor agonists on the T47D human breast cancer cell line, is partially mediated through opioid receptorsA Hatzoglou
Laboratory of Experimental Endocrinology, University of Crete, Greece
Eur J Pharmacol 296:199-207. 1996..The opioid receptor antagonist diprenorphine had no significant effect per se, but it was able to reverse the action of all opioid receptor agonists except ..
- Acute and chronic morphine administration: effects of mixed-action opioids in rats and squirrel monkeys responding under a schedule of food presentationA H Oliveto
Department of Psychology, University of North Carolina, Chapel Hill 27599 3270
J Pharmacol Exp Ther 257:8-18. 1991..In morphine-pretreated rats, dose-effect curves for the opioid antagonists naloxone, naltrexone and diprenorphine shifted to the left of those determined when rats were not morphine-pretreated; whereas those for the mu-..
- Neuroleptanalgesia in wild Asian elephants (Elephas maximus maximus)Ashoka Dangolla
Department of Veterinary Clinical Studies, Faculty of Veterinary Medicine and Animal Science, University of Peradeniya, Sri Lanka
Vet Anaesth Analg 31:276-9. 2004..To evaluate the suitability of etorphine with acepromazine for producing prolonged neuroleptanalgesia in wild Asian elephants...
- Overdose during chemical restraint in a black rhinoceros (Diceros bicornis)Wendy A Adams
Department of Anaesthesia, University Clinical Department, Liverpool, UK
Vet Anaesth Analg 32:53-7. 2005..The trachea was intubated, inspired breath was enriched with oxygen and the lungs ventilated manually. Diprenorphine (1.5 mg) was given intravenously and spontaneous breathing resumed 11 minutes later...
- Opiate binding differentially associated with oxytocin and vasopressin nerve endings from porcine neurohypophysesN Falke
Sektion Elektronenmikroskopie, , Federal Republic of Germany
Exp Brain Res 70:145-54. 1988..Specific (= displaceable) binding was observed with 3H-etorphine and with 3H-diprenorphine, two ligands with low selectivity for distinct opiate receptor subclasses...
- Comparison of stably expressed rat UGT1.1 and UGT2B1 in the glucuronidation of opioid compoundsC D King
Department of Pharmacology, University of Iowa, Iowa City 52242, USA
Drug Metab Dispos 25:251-5. 1997..1. Comparably high glucuronidation rates and efficiencies were found for buprenorphine and diprenorphine with both UGT isoforms...
- Development of displacement binding and GTPgammaS scintillation proximity assays for the identification of antagonists of the micro-opioid receptorGeorge Rodgers
Eli Lilly and Company Lilly RTP, Research Triangle Park, NC 27709, USA
Assay Drug Dev Technol 1:627-36. 2003..report describes the development of a MOR displacement binding SPA using the radiolabeled antagonist [(3)H]diprenorphine ((3)H-DPN)...
- Monoclonal anti-idiotypic antibodies to opioid receptorsC Gramsch
Department of Neuropharmacology, Max Planck Institut fur Psychiatrie, Planegg Martinsried, Federal Republic of Germany
J Biol Chem 263:5853-9. 1988..The anti-idiotypic antibodies were able to precipitate [3H] diprenorphine binding sites from solubilized opioid receptor preparations...
- Molecular cloning and functional expression of a mu-opioid receptor from rat brainY Chen
Department of Medical and Molecular Genetics, Indiana University School of Medicine, Indianapolis 46202
Mol Pharmacol 44:8-12. 1993..When transfected into COS-7 cells, the cDNA conferred a binding site with subnanomolar affinity for [3H]diprenorphine, a high affinity ligand for all three types of opioid receptors...
- The orvinols and related opioids--high affinity ligands with diverse efficacy profilesJohn W Lewis
Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
Curr Pharm Des 10:717-32. 2004..b>Diprenorphine is primarily a mu antagonist though it also has some kappa-partial agonist effects...
- Plasma lactate concentrations in free-ranging moose (Alces alces) immobilized with etorphineHenning A Haga
Department of Companion Animal Clinical Sciences, Norwegian School of Veterinary Science, Oslo, Norway
Vet Anaesth Analg 36:555-61. 2009..To investigate plasma lactate concentrations of etorphine-immobilized moose in relation to environmental, temporal and physiological parameters...
- Respiratory and circulatory parameters of African elephants (Loxodonta africana) anaesthetised with etorphine and azaperoneJ Still
Department of Companion Animal Medicine and Surgery, Medical University of Southern Africa, Medunsa, South Africa
J S Afr Vet Assoc 67:123-7. 1996..Individual elephants spent 35-150 minutes under anaesthesia and all recovered uneventfully after reversal of etorphine with diprenorphine.
- Receptor selectivity of Met-enkephalin-Arg6-Phe7, an endogenous opioid peptide, in cerebral cortex of human and ratK W Kim
Dept of Pharmacology, Chonbuk University Medical School, Chonju, Republic of Korea
Life Sci 67:61-71. 2000..However, MERF had little influence on the specific binding of [3H]DPDPE, [3H]U69 and [3H]diprenorphine ([3H]DIP) in the presence of 1 microM each of DAMGO, DPDPE and U69...
- Haemodynamic, metabolic and physical responses to a neuroleptanalgesic-glyceryl guaiacolate combination in the horseF Gasthuys
Large Animal Surgical Clinic, Faculty of Veterinary Medicine, State University, Gent, Belgium
Vet Res Commun 13:113-26. 1989..No electrolyte changes were found. After reversal of the action of etorphine with diprenorphine, there was a prolonged decrease in the calcium and phosphorus serum concentrations and decreases in the packed ..
- Opioid agonists modify breast cancer cell proliferation by blocking cells to the G2/M phase of the cycle: involvement of cytoskeletal elementsS Panagiotou
Laboratory of Experimental Cancerology, CJF 93 11, Marseille, France
J Cell Biochem 73:204-11. 1999..a clear redistribution at the periphery of the cell, reversed by the addition of the general opioid antagonist diprenorphine. Furthermore, differences between the two opioids were obvious, attributed to the different receptor affinity ..
- Effects of chronic opioid exposure on guinea pig mu opioid receptor in Chinese hamster ovary cells: comparison with human and rat receptorMichael Wallisch
Department of Physiology and Pharmacology, School of Medicine, 3181 SW Sam Jackson Park Road, Oregon Health and Science University, Portland, OR 97239, USA
Biochem Pharmacol 73:1818-28. 2007..MOP expressing CHO cells were treated in culture with methadone or morphine for up to 48 h. Radioligand diprenorphine and [D-AIa(2),N-Me-Phe(4),Gly(5)-ol]-enkephalin (DAMGO)-stimulated GTP gamma S binding assays were carried out ..
- The seventh transmembrane domains of the delta and kappa opioid receptors have different accessibility patterns and interhelical interactionsWei Xu
Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, PA 19140, USA
Biochemistry 44:16014-25. 2005..Most mutants displayed similar binding affinity for [(3)H]diprenorphine, an antagonist, as the wild types...
- Mu-opioid receptor expression in High Five insect cells is regulated by 5' untranslated region (5'UTR)G F Belke-Louis
Institute of Pharmacology, Toxicology and Pharmacy, Ludwig Maximilians University, Muenchen, Germany
Life Sci 64:913-21. 1999..expressed opioid receptors displayed identical high affinity binding characteristics for the opioid antagonist diprenorphine and similar EC50 values to inhibit forskolin (10(-5) M) stimulated cAMP synthesis...
- New kappa opioid receptor from zebrafish Danio rerioFranscisco Alvar Alvarez
Department of Biochemistry and Molecular Biology, Faculty of Medicine, Instituto de Neurociencias de Castilla y Leon, University of Salamanca, Avda Alfonso X El Sabio s n, 37007 Salamanca, Spain
Neurosci Lett 405:94-9. 2006..When ZFOR3 is stably expressed in HEK293 cells, [(3)H]-diprenorphine binds with high affinity (K(D)=1.05+/-0...
- Evidence for endogenous opioid release in the amygdala during positive emotionM J Koepp
Institute of Neurology, University College London, Queen Square, London WC1, UK
Neuroimage 44:252-6. 2009..However, this theory remains controversial. Using positron emission tomography and [(11)C]diprenorphine (DPN) in healthy volunteers, we found significantly reduced DPN binding to opioid receptor in the hippocampus ..
- Kappa2 opioid receptor subtype binding requires the presence of the DOR-1 geneMichael A Ansonoff
Department of Neuroscience and Cell Biology, University of Medicine and Dentistry of New Jersey Robert Wood Johnson Medical School, 675 Hoes Lane, Piscataway, NJ 08854, USA
Front Biosci (Schol Ed) 2:772-80. 2010..Using displacement of the general opioid ligand diprenorphine, we observed that occupancy or knockout of the DOR-1 gene increases the binding density of kappa1 receptors ..
- What has positron emission tomography told us about the epileptogenic zone?A Hammers
MRC Clinical Sciences Centre, Imperial College London, South Kensington, Hammersmith Hospital, United Kingdom
Rev Neurol (Paris) 165:739-41. 2009..FDG, flumazenil (FMZ), alpha-methyl-tryptophan (AMT), the 5-HT1A ligands, and diprenorphine are discussed.
- Post-endocytic fates of delta-opioid receptor are regulated by GRK2-mediated receptor phosphorylation and distinct beta-arrestin isoformsXiaoqing Zhang
Pharmacology Research Center and National Laboratory of Medical Neurobiology, Shanghai Medical College and Institutes of Brain Science, Fudan University, Shanghai, China
J Neurochem 106:781-92. 2008..Thus, the post-endocytic fate of internalized DOR can be regulated by GRK2-catalyzed receptor phosphorylation as well as distinct beta-arrestin isoforms...
- Characterization of delta, kappa, and mu human opioid receptors overexpressed in baculovirus-infected insect cellsD Massotte
Département des Récepteurs et Protéines Membranaires, CNRS Unité Propre de Recherche 9050, F 64700 Illkirch Graffenstaden, France
J Biol Chem 272:19987-92. 1997..The pharmacological profile was similar to the one obtained when the receptor was expressed in Sf9 cells. Our results show that the baculovirus expression system is suitable for large scale production of human opioid receptors...
- The runner's high: opioidergic mechanisms in the human brainHenning Boecker
Nuklearmedizinische Klinik, Klinikum rechts der Isar, Technische Universitat Munchen, 81675 Munchen, Germany
Cereb Cortex 18:2523-31. 2008..These findings support the "opioid theory" of the runner's high and suggest region-specific effects in frontolimbic brain areas that are involved in the processing of affective states and mood...
- Characterization of a new duplicate delta-opioid receptor from zebrafishNoelia Pinal-Seoane
Department of Biochemistry and Molecular Biology, Faculty of Medicine, Instituto de Neurociencias de Castilla y Leon INCYL, University of Salamanca, Avda Alfonso X El Sabio s n, 37007 Salamanca, Spain
J Mol Endocrinol 37:391-403. 2006..Pharmacological analysis of ZFOR4 shows specific and saturable binding with [(3)H] diprenorphine, displaying one binding site with K(D) = 3.42 +/- 0...
- Adenylyl cyclase superactivation induced by long-term treatment with opioid agonist is dependent on receptor localized within lipid rafts and is independent of receptor internalizationHui Zhao
Department of Pharmacology, 6 120 Jackson Hall, Medical School, University of Minnesota, 321 Church St S E, Minneapolis, MN 55455 0217, USA
Mol Pharmacol 69:1421-32. 2006..In the presence of diprenorphine, the magnitude of adenylyl cyclase superactivation after etorphine treatment was identical to that observed ..
- Opioid alkaloids and casomorphin peptides decrease the proliferation of prostatic cancer cell lines (LNCaP, PC3 and DU145) through a partial interaction with opioid receptorsM Kampa
Laboratory of Experimental Endocrinology, University of Crete, School of Medicine and University Hospital, Heraklion, Greece
Eur J Pharmacol 335:255-65. 1997..In many cases, this effect was antagonized by the general opioid antagonist, diprenorphine, indicating the existence of specific opioid binding sites...
- Imaging endogenous opioid peptide release with [11C]carfentanil and [3H]diprenorphine: influence of agonist-induced internalizationDarren R Quelch
Centre for Neuropsychopharmacology, Division of Brain Sciences, Imperial College London, London, UK
J Cereb Blood Flow Metab 34:1604-12. 2014..We compared the sensitivities of opioid receptor radioligands, carfentanil, and diprenorphine, to amphetamine-induced endogenous opioid peptide (EOP) release and methadone administration in the rat...
- Opioidergic activation in the medial pain system after heat painTill Sprenger
Department of Neurology, Technische Universitaet Muenchen, Germany
Pain 122:63-7. 2006..Pain stimulation led to significant reduction of diprenorphine binding in limbic and paralimbic brain areas including the rostral ACC and insula...
- Identification and characterization of opioid-binding sites present in the Ishikawa human endometrial adenocarcinoma cell lineA Hatzoglou
Department of Experimental Endocrinology, Medical School, University of Crete, Greece
J Clin Endocrinol Metab 80:418-23. 1995..kappa 2-sites with high affinity for ethylketocyclazocine (Kd, approximately 1 nmol/L) and low affinity for diprenorphine (Kd, approximately 8 nmol/L) at a concentration of 93,000 sites/cell, and high affinity kappa 3-sites (Kd, 3...
- Electron density analyses of opioids: a comparative studyStephan Scheins
Institute for Chemistry and Biochemistry Crystallography, Free University of Berlin, Fabeckstrasse 36a, 14195 Berlin, Germany
J Phys Chem A 111:5499-508. 2007The electron densities of five morphine related molecules (codeine, diprenorphine, naltrexone in the neutral and protonated states, and dextromethorphan) were determined from high-resolution X-ray diffraction experiments (Mo Kalpha and ..
- Cloning of a human kappa opioid receptor from the brainJ Zhu
Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140
Life Sci 56:PL201-7. 1995..Hkor had high affinity for [3H] diprenorphine, a nonselective opioid antagonist, and displayed stereospecific binding to naloxone...
- Brain opioid receptor binding in early abstinence from opioid dependence: positron emission tomography studyTim M Williams
Psychopharmacology Unit, University of Bristol, and Bristol Specialist Drug Service, Blackberry Hill Hospital, UK
Br J Psychiatry 191:63-9. 2007..Although opioid receptor function in humans is clearly reduced during opioid dependence, what happens to the receptor in early abstinence is not understood...
- The inhibitory effect of opioids on HepG2 cells is mediated via interaction with somatostatin receptorsGeorge Notas
Laboratory of Gastroenterology and Hepatology, School of Medicine, University of Crete, Heraklion, Crete, Greece
Eur J Pharmacol 555:1-7. 2007..This inhibitory effect is not exerted via opioids receptors since it was not reversed by the opioid antagonist diprenorphine and functional opioid receptors were not found on HepG2 cells...
- Differential agonist regulation of the human kappa-opioid receptorA D Blake
Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104, U S A
J Neurochem 68:1846-52. 1997..l)-1-oxaspiro [4,5] dec-8-yl] benzeneacetamide ([3H]U69,593), and a nonselective opioid antagonist, [3H]diprenorphine. Pretreatment with pertussis toxin or guanosine 5'-O-(3-thiotriphosphate) reduced [3H]69,593 binding, ..
- Expression of two variants of the human mu opioid receptor mRNA in SK-N-SH cells and human brainL A Bare
Ohmeda PPD, Murray Hill, NJ 07974
FEBS Lett 354:213-6. 1994..Both receptors show similar ligand binding and coupling to cAMP in CHO-K1 cells. The C-terminal differences between MOR1 and MOR1A could have effects on receptor coupling or receptor transport and localization...
- Antagonism of the discriminative stimulus effects of the kappa-opioid agonist spiradolineS G Holtzman
Department of Pharmacology, Emory University School of Medicine, Atlanta, GA 30322 3090
Psychopharmacology (Berl) 116:243-8. 1994..They spanned a 150-fold potency range from diprenorphine (5 times as potent as naloxone) to nalbuphine (0.03 times as potent as naloxone)...
- DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and phKenneth J Valenzano
Department of Molecular Pharmacology, Purdue Pharma Discovery Research, 6 Cedarbrook Drive, Cranbury, NJ 08512, USA
J Pharmacol Exp Ther 310:783-92. 2004..5]dec-3-yl]-acetic acid (DiPOA). In a radioligand binding assay, DiPOA inhibited [(3)H]-diprenorphine binding to recombinant human mu receptors with a K(i) value of approximately 0.8 nM...
- Structural basis for μ-opioid receptor binding and activationAdrian W R Serohijos
Biochemistry and Biophysics Department, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Structure 19:1683-90. 2011..In summary, the MOR1 model provides a tool for elucidating the structural mechanism of ligand-initiated cell signaling and for screening novel analgesics...
- Synthesis and evaluation of three structurally related ¹⁸F-labeled orvinols of different intrinsic activities: 6-O-[¹⁸F]fluoroethyl-diprenorphine ([¹⁸F]FDPN), 6-O-[¹⁸F]fluoroethyl-buprenorphine ([¹⁸F]FBPN), and 6-O-[¹⁸F]fluoroethyl-phenethyl-orvinol ([¹⁸FBent W Schoultz
Department of Chemistry, University of Oslo, P O Box 1033, Blindern, N 0315 Oslo, Norway
J Med Chem 57:5464-9. 2014..of structurally related orvinols that span across the full range of intrinsic activities, the antagonist diprenorphine, the partial agonist buprenorphine, and the full agonist phenethyl-orvinol...
- Characterization of nociceptin/orphanin FQ binding sites in dog brain membranesEmma E Johnson
University Department of Anaesthesia, Critical Care and Pain Management, Leicester Royal Infirmary, Leicester, United Kingdom
Anesth Analg 97:741-7. 2003..The density of classic opioid receptors was determined by using [(3)H]diprenorphine. Leucyl-[(3)H]N/OFQ(1-17)OH binding was concentration dependent and saturable in dog (maximum binding capacity ..
- Functional role of a conserved motif in TM6 of the rat mu opioid receptor: constitutively active and inactive receptors result from substitutions of Thr6.34(279) with Lys and AspP Huang
Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
Biochemistry 40:13501-9. 2001..state of the wild type, which was not altered by GTPgammaS, while having unchanged affinity for the antagonist diprenorphine. The T6.34(279)K mutant displayed a higher intracellular receptor pool than the wild type...
- Divers pathways mediate delta-opioid receptor down regulation within the same cellM Shapira
The Mauerberger Chair in Neuropharmacology, Department of Physiology and Pharmacology, Sackler Faculty of Medicine, Tel Aviv University, 69978, Tel Aviv, Israel
Brain Res Mol Brain Res 96:142-50. 2001..the absence or presence of various pharmacological agents and measured the binding of the opioid ligand [(3)H]diprenorphine to either isolated cell membranes or whole cells...
- Tramadol reduces the 5-HTP-induced head-twitch response in mice via the activation of mu and kappa opioid receptorsHong Lei Sun
National Institute on Drug Dependence, Peking University, Xue Yuan Road 38, Haidian District, Beijing 100083, PR China
Life Sci 72:1221-30. 2003..Furthermore, the nonselective opioid receptor antagonists, naloxone and diprenorphine (M5050), reversed the effect of tramadol on 5-HTP-induced HTR dose-dependently...
- Positron emission tomography radioligands for the opioid systemRobert F Dannals
Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University School of Medicine, Baltimore, Maryland, USA, 21287
J Labelled Comp Radiopharm 56:187-95. 2013..This review looks at the history of positron emission tomography radioligands for probing this receptor system. ..
- Molecular details of the activation of the μ opioid receptorJihyun Shim
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, Maryland 21201, USA
J Phys Chem B 117:7907-17. 2013..With the orvinols, the increased size of the C19 substituent in buprenorphine over diprenorphine leads to increased interactions with residues adjacent to Asp147, partially overcoming the presence of the ..
- Human exposures to immobilising agents: results of an online surveyA Haymerle
Research Institute of Wildlife Ecology, University of Veterinary Medicine, A 1160 Vienna, Austria
Vet Rec 167:327-32. 2010..such as naloxone, nalmefene or naltrexone, and not with antagonists with agonistic properties, such as diprenorphine. With regard to the alpha(2)-agonists xylazine, detomidine, medetomidine and romifidine, no antagonist is ..
- Expression of EGFP-amino-tagged human mu opioid receptor in Drosophila Schneider 2 cells: a potential expression system for large-scale production of G-protein coupled receptorsBénédicte G Perret
Récepteurs et Protéines Membranaires, UPR CNRS 9050, Ecole Superieure de Biotechnologie de Strasbourg, Bld Sébastien Brant, B P 10413, F 67400, Illkirch, France
Protein Expr Purif 31:123-32. 2003..expressing EGFPhMOR display high-affinity, saturable, and specific binding sites for the opioid antagonist diprenorphine. Competition studies with opioid agonists and antagonists defined the pharmacological profile of a mu opioid ..
- The human delta opioid receptor activates G(i1)alpha more efficiently than G(o1)alphaH E Moon
Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK
J Neurochem 76:1805-13. 2001....
- In rats, acute morphine dependence results in antagonist-induced response suppression of intracranial self-stimulationKeith W Easterling
Department of Pharmacology, School of Medicine, Emory University, Atlanta, GA, USA
Psychopharmacology (Berl) 175:287-95. 2004..Lower (0.001-1.0 mg/kg) doses of the opioid antagonist naltrexone produce few behavioral effects in otherwise drug-free rats responding for ICSS, but reduce response rates by up to 75% after a single dose of morphine...
- Delta9-tetrahydrocannabinol releases and facilitates the effects of endogenous enkephalins: reduction in morphine withdrawal syndrome without change in rewarding effectO Valverde
, U266 INSERM, UMR 8600 CNRS, UFR des Sciences Pharmaceutiques et Biologiques, avenue de l'Observatoire, 75270 Paris Cedex 06, France
Eur J Neurosci 13:1816-24. 2001..In addition, this cannabinoid agonist displaced the in vivo [3H]diprenorphine binding to opioid receptors in total mouse brain...
- Comparison of etorphine-detomidine and medetomidine-ketamine anesthesia in captive addax (Addax nasomaculatus)Timothy J Portas
Victoria s Open Range Zoo, K Road, Werribee, Victoria 3030, Australia
J Zoo Wildl Med 34:269-73. 2003..Etorphine-detomidine anesthesia was antagonized with diprenorphine (107.1 +/- 16.4 microg/kg) and atipamezole (100.9 +/- 42.4 microg/kg)...
- Agonist Activity of the delta-antagonists TIPP and TIPP-psi in cellular models expressing endogenous or transfected delta-opioid receptorsN A Martin
Department of Pharmacology and Toxicology, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, USA
J Pharmacol Exp Ther 298:240-8. 2001..12 to 6.67 pmol/mg. These results suggest that compounds previously thought to be purely delta-opioid receptor antagonists also demonstrate agonist activity in several in vitro models...
- Identification of a novel opioid peptide (Tyr-Val-Pro-Phe-Pro) derived from human alpha S1 casein (alpha S1-casomorphin, and alpha S1-casomorphin amide)M Kampa
Laboratory of Experimental Endocrinology, University of Crete School of Medicine and University Hospital, Heraklion, Greece
Biochem J 319:903-8. 1996..In T47D breast cancer cells, other casomorphins have been found to bind to somatostatin receptors in addition to opioid sites. In contrast, alpha S1-casomorphin and its amide do not interact with somatostatin receptors in our system...
- Evidence for modulation of opioidergic activity in central vestibular processing: A [(18)F] diprenorphine PET studyBernhard Baier
Department of Neurology, University of Mainz, Langenbeckstr 1, 55131 Mainz, Germany
Hum Brain Mapp 31:550-5. 2010..receptor availability during caloric air stimulation of the right ear were studied with [(18)F] Fluoroethyl-diprenorphine ([(18)F]FEDPN) PET scans in 10 right-handed healthy volunteers and compared to a control condition...
- Thienorphine is a potent long-acting partial opioid agonist: a comparative study with buprenorphineGang Yu
Department of Pharmacology, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, Beijing, China
J Pharmacol Exp Ther 318:282-7. 2006..In vitro, thienorphine was more potent than buprenorphine in inhibiting [3H]diprenorphine and stimulating guanosine 5'-O-(3-[35S]thio)triphosphate binding to rat mu-opioid receptor stably expressed in ..
- Interaction of bivalent ligand KDN21 with heterodimeric delta-kappa opioid receptors in human embryonic kidney 293 cellsZhihua Xie
Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN, USA
Mol Pharmacol 68:1079-86. 2005..We have shown previously that when using [(3)H]diprenorphine as radioligand, KDN21 displayed greatly enhanced affinity in this series for coexpressed delta and kappa ..
- Autoradiography in opioid triple knockout mice reveals opioid and opioid receptor like binding of naloxone benzoylhydrazoneVeronica Cox
Pharmacology Group, School of Biomedical and Molecular Sciences, University of Surrey, Guildford, Surrey, GU2 7XH, UK
Neuropharmacology 48:228-35. 2005..As competing ligands we have used diprenorphine and nociceptin at 1 microM, alone or in combination, to determine the contribution of opioid and ORL1 receptor ..
- Transient overexpression of kappa and mu opioid receptors using recombinant adenovirus vectorsZhu Zhen
Department of Microbiology and Immunology, University of Rochester Medical Center, Rochester, NY 14642, USA
J Neurosci Methods 136:133-9. 2004..U69,593), respectively, and a nonselective antagonist, [3H]diprenorphine, revealed that rAd5-transduced cells expressed MOR and KOR for at least 3 days, at levels which exceeded those ..
- Characterization of specific delta-opioid binding sites in the distal small intestine of swineDeWayne Townsend
Department of Veterinary Pathobiology, College of Veterinary Medicine, University of Minnesota, 1988 Fitch Avenue, St Paul, MN 55108 6010, USA
Eur J Pharmacol 482:111-6. 2003..In both preparations, the delta-opioid receptor antagonist naltrindole displaced [3H]diprenorphine from two binding sites...
- Human peripheral blood mononuclear cells express nociceptin/orphanin FQ, but not mu, delta, or kappa opioid receptorsJohn P Williams
Department of Cardiovascular Sciences, Pharmacology and Therapeutics Group, Division of Anaesthesia, Critical Care and Pain Management, University of Leicester, Leicester Royal Infirmary, Leicester, United Kingdom
Anesth Analg 105:998-1005, table of contents. 2007..These receptors are currently classified as classical (MOP/mu/mu, DOP/delta/delta and KOP/kappa/kappa) and nonclassical NOP (nociceptin/orphanin FQ; N/OFQ)...
- CHARACTERIZATION & REGULATION OF BETA-ENDORPHIN RECEPTORNancy Lee; Fiscal Year: 1992..The antisense-transfected cells exhibit reduced 3H-diprenorphine binding, relative to non-transfected and sense- transfected NG108-15 cells; in contrast, muscarinic and alpha2-..
- OPIOID RECEPTOR SIGNAL TRANSDUCTION MECHANISMSKELLY STANDIFER; Fiscal Year: 2000..agonist naloxone benzoylhydrazone (NalBzoH) is antagonized by nonselective opioid antagonists (Win44,441, diprenorphine, Mr2266), but not by subtype selective antagonists (naloxone, naltrindole, norbinaltorphimine)...
- AUTONOMIC FUNCTION IN RENOVASCULAR HYPERTENSIONBARBARA BARRON; Fiscal Year: 2000..be tested by repeating baroreflex challenges in the presence of the non-selective opioid receptor antagonist, diprenorphine. 3) Measurement of tissue enkephalinase activity, proenkephalin products and catecholamine content in ..
- CHARACTERIZATION AND REGULATION OF BETA-ENDORPHIN RECEPTNancy Lee; Fiscal Year: 2001..The antisense-transfected cells exhibit reduced 3H-diprenorphine binding, relative to non-transfected and sense- transfected NG108-15 cells; in contrast, muscarinic and alpha2-..
- fMRI and Opioid Neuroimaging of Acupuncture AnalgesiaRandy Gollub; Fiscal Year: 2003..We will utilize PET and [11C]diprenorphine at baseline and during acupuncture to quantitate opioid receptor binding and thus indirectly measure ..
- DRUGS OF ABUSE AND THE MEDIAL FOREBRAIN BUNDLELARRY REID; Fiscal Year: 1990..The possibility of a specific receptor became apparent by studying diprenorphine, a mixed agonist-antagonist which antagonizes many events of morphine but which shows signs of having ..
- BEHAVIORAL PHARMACOLOGY OF OPIATE-LIKE PEPTIDESKAREN BRITTON; Fiscal Year: 1990..will be characterized in the RACs as will the relatively pure opiate antagonists naloxone, naltrexone, and diprenorphine. Under identical experimental conditions, the effects of restraint, noise, and exposure to a novel environment ..
- Behavioral Pharmacology of Serotonin Inverse AgoinstsEllen Walker; Fiscal Year: 2006..Taken together, these experiments will provide a novel pharmacological and/or behavioral profile for 5-HT2C inverse agonists and neutral antagonists while testing hypotheses generated from in vitro data. ..
- Society for the Stimulus Properties of Drugs SatelliteEllen Walker; Fiscal Year: 2005..The SSPD Satellite to the EBPS 2005 Conference promises to coordinate, exchange, and disseminate information to further our understanding of drug abuse. ..
- BEHAVIORAL PHARMACOLOGY OF OPIOIDSSTEPHEN HOLTZMAN; Fiscal Year: 2004....
- PHYSIOLOGIC STUDIES OF ANGER IN DEPRESSED PATIENTSDarin Dougherty; Fiscal Year: 2002..abstract_text> ..
- BEHAVIORAL PHARMACOLOGY OF NARCOTIC ANTAGONISTSSTEPHEN HOLTZMAN; Fiscal Year: 2002..Acute agonist-induced sensitization to opioid antagonists appears to be an exquisite example of neuronal plasticity, reflecting the first hours of the drug-receptor interactions that lead to chronic physical dependence upon opioids. ..
- Maternal Separation: Rat Model of Opioid VulnerabilitySTEPHEN HOLTZMAN; Fiscal Year: 2006..abstract_text> ..