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1. Full Text Mice Lacking GPR88 Show Motor Deficit, Improved Spatial Learning, and Low Anxiety Reversed by Delta Opioid Antagonist
by Meirsman, Aura C and Le Merrer, Julie and Pellissier, Lucie P and Diaz, Jorge and Clesse, Daniel and Kieffer, Brigitte L and Becker, Jérôme A.J
Biological Psychiatry, ISSN 0006-3223, 2015, Volume 79, Issue 11, pp. 917 - 927
Abstract Background GPR88 is an orphan G protein coupled receptor highly enriched in the striatum, and previous studies have focused on GPR88 function in... 
Psychiatry | Ethological scoring of anxiety | GPR88 agonist-induced GTPγS binding | Gene clustering | Medium spiny neurons | Psychiatric disorders | Spatial learning | CENTRAL EXTENDED AMYGDALA | PSYCHIATRY | DEPENDENT BEHAVIORS | PROTRACTED ABSTINENCE | NEUROSCIENCES | ADENOSINE A(2A) RECEPTORS | GPR88 agonist-induced GTP gamma S binding | C-TERMINAL DOMAINS | STRIATOPALLIDAL NEURONS | DORSAL STRIATUM | SELECTIVE INTERACTIONS | OBJECT RECOGNITION | PARKINSON-DISEASE | Naltrexone - analogs & derivatives | Receptors, Opioid, delta - metabolism | Dendrites - pathology | Male | Anxiety - drug therapy | Corpus Striatum - metabolism | Spatial Learning - physiology | Naltrexone - pharmacology | Female | Anxiety - metabolism | Corpus Striatum - pathology | Dopamine - metabolism | Dendrites - drug effects | Dendrites - metabolism | Movement Disorders - pathology | Receptors, Opioid, mu - metabolism | Mice, Inbred C57BL | Spatial Learning - drug effects | Amygdala - metabolism | Hippocampus - pathology | Amygdala - pathology | Anxiety - pathology | Mice, Knockout | Hippocampus - metabolism | Movement Disorders - metabolism | Animals | Receptors, G-Protein-Coupled - deficiency | Narcotic Antagonists - pharmacology | Serotonin - metabolism | Receptors, G-Protein-Coupled - genetics | Movement Disorders - drug therapy | Neurosciences | G proteins | Anxiety | Brain research | Genetic transcription | Neurons | Life Sciences | Human health and pathology | Other | Psychiatrics and mental health | medium spiny neurons | spatial learning | gene clustering | ethological scoring of anxiety | psychiatric disorders
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2. Full Text 14-Alkoxy- and 14-Acyloxypyridomorphinans: mu Agonist/delta Antagonist Opioid Analgesics with Diminished Tolerance and Dependence Side Effects
by Ananthan, S and Saini, SK and Dersch, CM and Xu, H and McGlinchey, N and Giuvelis, D and Bilsky, EJ and Rothman, RB
JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0022-2623, 10/2012, Volume 55, Issue 19, pp. 8350 - 8363
In the search for opioid ligands with mixed functional activity, a series of 5'-(4-chlorophenyl)-4,5 alpha-epoxypyridomorphinans possessing alkoxy or acyloxy... 
14-ALKOXYMORPHINANS | CHEMISTRY, MEDICINAL | LIGANDS | MORPHINE-TOLERANCE | DELTA | BIOLOGICAL EVALUATION | SELECTIVE MU | MICE | RECEPTOR INTERACTIONS | BINDING | ANTINOCICEPTIVE TOLERANCE
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3. Full Text Molecular control of δ-opioid receptor signalling
by Fenalti, Gustavo and Giguere, Patrick M and Katritch, Vsevolod and Huang, Xi-Ping and Thompson, Aaron A and Cherezov, Vadim and Roth, Bryan L and Stevens, Raymond C
Nature, ISSN 0028-0836, 2014, Volume 506, Issue 7487, pp. 191 - 196
Opioids represent widely prescribed and abused medications, although their signal transduction mechanisms are not well understood. Here we present the 1.8... 
CRYSTALLIZING MEMBRANE | ALLOSTERIC REGULATION | INVERSE AGONISTS | SODIUM | DESIGN | PROTEIN | MULTIDISCIPLINARY SCIENCES | ANTAGONISTS | BINDING | SELECTIVITY | DISCOVERY | Naltrexone - analogs & derivatives | Receptors, Opioid, delta - metabolism | Humans | Naltrexone - chemistry | Crystallography, X-Ray | Structure-Activity Relationship | Sodium - metabolism | Arrestins - metabolism | Narcotic Antagonists - chemistry | Naltrexone - pharmacology | Narcotic Antagonists - metabolism | Receptors, Opioid, delta - genetics | Receptors, Opioid, delta - antagonists & inhibitors | Asparagine - genetics | Naltrexone - metabolism | Allosteric Regulation - drug effects | Allosteric Site - genetics | Sodium - pharmacology | Allosteric Regulation - genetics | Mutagenesis, Site-Directed | Receptors, Opioid, delta - chemistry | Allosteric Site - drug effects | Models, Molecular | Signal Transduction - drug effects | beta-Arrestins | Asparagine - metabolism | Narcotic Antagonists - pharmacology | Ligands | Receptors, Opioid, delta - agonists | Index Medicus | sodium regulation | constitutive activity | human opioid receptor | arrestin | functional selectivity | GPCR signaling | allostery
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4. Full Text Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives
by Kutsumura, Noriki and Koyama, Yasuaki and Nagumo, Yasuyuki and Nakajima, Ryo and Miyata, Yoshiyuki and Yamamoto, Naoshi and Saitoh, Tsuyoshi and Yoshida, Naoko and Iwata, Satoshi and Nagase, Hiroshi
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 08/2017, Volume 25, Issue 16, pp. 4375 - 4383
The 7-benzylidenenaltrexone (BNTX) derivatives , , , and were synthesized from naltrexone ( ) and evaluated for their antitrichomonal activity. The... 
Antitrichomonal activity | Trichomonas | Morphinan | Opioid receptor | BNTX | CHEMISTRY, MEDICINAL | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | RESISTANT TRICHOMONAS-VAGINALIS | DRUG-RESISTANT | NITROIMIDAZOLE DERIVATIVES | PLASMODIUM-CHABAUDI | BIVALENT LIGANDS | PROSTATE-CANCER | TRITRICHOMONAS-MOBILENSIS | BINDING-SITES | METRONIDAZOLE | AGONIST | Naltrexone - analogs & derivatives | Cricetulus | Naltrexone - chemistry | Naltrexone - chemical synthesis | Benzylidene Compounds - chemical synthesis | Structure-Activity Relationship | Benzylidene Compounds - chemistry | Dose-Response Relationship, Drug | Naltrexone - pharmacology | Animals | Benzylidene Compounds - pharmacology | Trichomonas vaginalis - drug effects | Receptors, Opioid, delta - antagonists & inhibitors | Molecular Structure | Antitrichomonal Agents - chemical synthesis | Antitrichomonal Agents - chemistry | Antitrichomonal Agents - pharmacology | CHO Cells | Index Medicus
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5. Full Text Structure of the δ-opioid receptor bound to naltrindole
by Granier, Sébastien and Manglik, Aashish and Kruse, Andrew C and Kobilka, Tong Sun and Thian, Foon Sun and Weis, William I and Kobilka, Brian K
Nature, ISSN 0028-0836, 05/2012, Volume 485, Issue 7398, pp. 400 - 404
The opioid receptor family comprises three members, the mu-, delta- and kappa-opioid receptors, which respond to classical opioid alkaloids such as morphine... 
SITE | MUTAGENESIS | LIGANDS | SELECTIVITY | MULTIDISCIPLINARY SCIENCES | PEPTIDE | Naltrexone - analogs & derivatives | Protein Structure, Tertiary | Receptors, Opioid, delta - metabolism | Amino Acid Sequence | Reproducibility of Results | Receptors, Opioid, delta - chemistry | Models, Molecular | Molecular Sequence Data | Naltrexone - chemistry | Substrate Specificity | Crystallography, X-Ray | Structure-Activity Relationship | Naltrexone - pharmacology | Animals | Conserved Sequence | Receptors, Opioid, delta - antagonists & inhibitors | Mice | Binding Sites | Naltrexone - metabolism
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6. Full Text Development and in Vitro Characterization of a Novel Bifunctional mu-Agonist/delta-Antagonist Opioid Tetrapeptide
by Purington, LC and Sobczyk-Kojiro, K and Pogozheva, ID and Traynor, JR and Mosberg, HI
ACS CHEMICAL BIOLOGY, ISSN 1554-8929, 12/2011, Volume 6, Issue 12, pp. 1375 - 1381
The development of tolerance to and dependence on opioid analgesics greatly reduces their long-term usefulness. Previous studies have demonstrated that... 
RECEPTOR SELECTIVE TETRAPEPTIDE | MULTIPLE LIGANDS | POTENT | MORPHINE-TOLERANCE | SENSITIZATION | DELTA | BIOCHEMISTRY & MOLECULAR BIOLOGY | KNOCKOUT MICE | BINDING | DMT-TIC PHARMACOPHORE | DEPENDENCE
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7. Full Text Synthesis, Modeling, and Pharmacological Evaluation of UMB 425, a Mixed mu Agonist/delta Antagonist Opioid Analgesic with Reduced Tolerance Liabilities
by Healy, JR and Bezawada, P and Shim, J and Jones, JW and Kane, MA and MacKerell, AD and Coop, A and Matsumoto, RR
ACS CHEMICAL NEUROSCIENCE, ISSN 1948-7193, 09/2013, Volume 4, Issue 9, pp. 1256 - 1266
Opioid narcotics are used for the treatment of moderate-to-severe pain and primarily exert their analgesic effects through mu receptors. Although traditional... 
conformationally sampled pharmacophore | CHEMISTRY, MEDICINAL | RECEPTOR ANTAGONISTS | EFFICACY | BIOCHEMISTRY & MOLECULAR BIOLOGY | PHYSICAL-DEPENDENCE | Antinociception | FORCE-FIELDS | mu agonist | NEUROSCIENCES | opioid receptor | delta antagonist | PAIN | LIGANDS | MORPHINE-TOLERANCE | MICE | tolerance
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8. Full Text Structural basis for bifunctional peptide recognition at human δ-opioid receptor
by Fenalti, Gustavo and Zatsepin, Nadia A and Betti, Cecilia and Giguere, Patrick and Han, Gye Won and Ishchenko, Andrii and Liu, Wei and Guillemyn, Karel and Zhang, Haitao and James, Daniel and Wang, Dingjie and Weierstall, Uwe and Spence, John C.H and Boutet, Sébastien and Messerschmidt, Marc and Williams, Garth J and Gati, Cornelius and Yefanov, Oleksandr M and White, Thomas A and Oberthuer, Dominik and Metz, Markus and Yoon, Chun Hong and Barty, Anton and Chapman, Henry N and Basu, Shibom and Coe, Jesse and Conrad, Chelsie E and Fromme, Raimund and Fromme, Petra and Tourwé, Dirk and Schiller, Peter W and Roth, Bryan L and Ballet, Steven and Katritch, Vsevolod and Stevens, Raymond C and Cherezov, Vadim and Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Nature Structural and Molecular Biology, ISSN 1545-9993, 03/2015, Volume 22, Issue 3, pp. 265 - 268
Bifunctional mu- and delta-opioid receptor (OR) ligands are potential therapeutic alternatives, with diminished side effects, to alkaloid opiate analgesics. We... 
POTENT | BIOPHYSICS | MORPHINE | TOLERANCE | BIOCHEMISTRY & MOLECULAR BIOLOGY | SERIAL FEMTOSECOND CRYSTALLOGRAPHY | DMT | MU AGONIST/DELTA ANTAGONIST | BOND | DEPENDENCE | CELL BIOLOGY | Protein Structure, Tertiary | Tetrahydroisoquinolines - chemistry | Receptors, Opioid, delta - chemistry | Humans | HEK293 Cells | Models, Molecular | Crystallography, X-Ray | Receptors, Opioid, delta - antagonists & inhibitors | Binding Sites | Oligopeptides - chemistry | X-ray crystallography | G protein-coupled receptors | Peptides | 60 APPLIED LIFE SCIENCES | opioid receptor | G protein-coupled receptor | protein structure | Bi-functional peptide | X-ray free electron laser | ligand binding | serial femtosecond crystallography
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9. Full Text Delta-opioid receptor antagonist naltrindole reduces oxycodone addiction and constipation in mice
by Yang, Pao-Pao and Yeh, Teng-Kuang and Loh, Horace H and Law, Ping-Yee and Wang, Yun and Tao, Pao-Luh
European Journal of Pharmacology, ISSN 0014-2999, 06/2019, Volume 852, pp. 265 - 273
Oxycodone, a widely prescribed and very potent oral opioid analgesic agent, is highly addictive and has many side effects, including troublesome constipation.... 
Tolerance | Naltrindole | Conditioned place preference | Delta-opioid receptor | Oxycodone | Dependence | UNITED-STATES | DOPAMINE RELEASE | ANALGESIC ABUSE | MORPHINE | MU | NUCLEUS-ACCUMBENS | GASTROINTESTINAL TRANSIT | PAIN | RELAPSE VULNERABILITY | PHARMACOLOGY & PHARMACY | Drug abuse | Liability (Law) | Constipation | Opioids
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10. Full Text Delta-Opioid Receptor Antagonists Prevent Sensitization to the Conditioned Rewarding Effects of Morphine
by Shippenberg, Toni S and Chefer, Vladimir I and Thompson, Alexis C
Biological Psychiatry, ISSN 0006-3223, 2009, Volume 65, Issue 2, pp. 169 - 174
Background Functional interactions between μ- and δ-opioid receptors (MOPr and DOPr, respectively) are implicated in morphine tolerance and dependence. The... 
Psychiatry | naltrindole | δ opioid receptor | sensitization | Conditioned place preference | naltriben | morphine | SUBTYPES | PSYCHIATRY | PLACE PREFERENCE | TOLERANCE | delta opioid receptor | KNOCKOUT MICE | DELTA-OPIOID RECEPTOR | NEUROSCIENCES | DEPENDENCE | MEDIATED ANTINOCICEPTION | KAPPA | Naltrexone - analogs & derivatives | Conditioning, Classical - drug effects | Receptors, Opioid, mu - drug effects | Reinforcement (Psychology) | Rats | Male | Rats, Sprague-Dawley | Association Learning - drug effects | Morphine Dependence - physiopathology | Naltrexone - pharmacology | Animals | Benzylidene Compounds - pharmacology | Analysis of Variance | Narcotic Antagonists - pharmacology | Statistics, Nonparametric | Behavior, Animal - drug effects | Receptors, Opioid, delta - antagonists & inhibitors | Disease Models, Animal | Receptor Cross-Talk - drug effects | Morphine | Index Medicus | conditioned place preference
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11. Full Text Pyrrolo- and pyridomorphinans: Non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists
by Kumar, V and Clark, M.J and Traynor, J.R and Lewis, J.W and Husbands, S.M
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 08/2014, Volume 22, Issue 15, pp. 4067 - 4072
Opioid ligands have found use in a number of therapeutic areas, including for the treatment of pain and opiate addiction (using agonists) and alcohol addiction... 
Opioid | Partial agonist | Antagonist | Non-selective | Naltrexone | DESIGN | CHEMISTRY, MEDICINAL | LIGANDS | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | Receptors, Opioid, delta - metabolism | Morphinans - chemistry | Cricetinae | Analgesics, Opioid - chemical synthesis | Cricetulus | Pyridines - chemistry | Receptors, Opioid, mu - metabolism | Humans | Morphinans - chemical synthesis | Structure-Activity Relationship | Receptors, Opioid, mu - agonists | Animals | Morphinans - metabolism | Receptors, Opioid, delta - genetics | Analgesics, Opioid - chemistry | Protein Binding | Pyrroles - chemistry | Analgesics, Opioid - metabolism | Kinetics | Receptors, Opioid, mu - genetics | Receptors, Opioid, delta - agonists | CHO Cells
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12. Full Text Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2
by Váradi, András and Marrone, Gina F and Palmer, Travis C and Narayan, Ankita and Szabó, Márton R and Le Rouzic, Valerie and Grinnell, Steven G and Subrath, Joan J and Warner, Evelyn and Kalra, Sanjay and Hunkele, Amanda and Pagirsky, Jeremy and Eans, Shainnel O and Medina, Jessica M and Xu, Jin and Pan, Ying-Xian and Borics, Attila and Pasternak, Gavril W and McLaughlin, Jay P and Majumdar, Susruta
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2016, Volume 59, Issue 18, pp. 8381 - 8397
Natural products found in Mitragyna speciosa, commonly known as kratom, represent diverse scaffolds (indole, indolenine, and spiro pseudoindoxyl) with opioid... 
HERB MITRAGYNA-SPECIOSA | KNOCK-OUT MICE | CHEMISTRY, MEDICINAL | MORPHINE-TOLERANCE | PHYSICAL-DEPENDENCE | DRUG DISCOVERY | ANTISENSE OLIGODEOXYNUCLEOTIDES | RECEPTOR AGONIST | G-PROTEIN | MOR-1 SPLICE VARIANTS | AGONIST/DELTA ANTAGONIST | Mitragyna - chemistry | Receptors, Opioid, delta - metabolism | Cell Line | Secologanin Tryptamine Alkaloids - chemistry | Secologanin Tryptamine Alkaloids - pharmacology | Receptors, Opioid, mu - metabolism | Humans | Analgesics, Opioid - pharmacology | Male | beta-Arrestin 2 - metabolism | Receptors, Opioid, mu - agonists | Animals | Analgesics, Opioid - chemistry | Receptors, Opioid, delta - antagonists & inhibitors | Mice | Molecular Docking Simulation
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13. Full Text Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties
by Fujita, Y and Tsuda, Y and Li, TY and Motoyama, T and Takahashi, M and Shimizu, Y and Yokoi, T and Sasaki, Y and Ambo, A and Kita, A and Jinsmaa, Y and Bryant, SD and Lazarus, LH and Okada, Y
JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0022-2623, 07/2004, Volume 47, Issue 14, pp. 3591 - 3599
The C terminus of endomorphin-2 (EM-2) analogues (Tyr-Pro-Phe-NH-X) was modified with aromatic, heteroaromatic, or aliphatic groups (X = phenethyl,benzyl,... 
PRO AMIDE BOND | CHEMISTRY, MEDICINAL | PEPTIDES | ACID | MORPHINE-TOLERANCE | RECEPTOR AGONISTS | MOUSE VAS-DEFERENS | HUMAN BRAIN CORTEX | OPIATE RECEPTORS | DMT-TIC PHARMACOPHORE | DEPENDENCE | Analgesics - pharmacology | Neuromuscular Junction - drug effects | Stereoisomerism | Male | Receptors, Opioid, mu - agonists | Muscle, Smooth - drug effects | Ileum - drug effects | Analgesics - chemical synthesis | Muscle, Smooth - physiology | Receptors, Opioid, delta - antagonists & inhibitors | Oligopeptides - chemistry | Vas Deferens - drug effects | Ileum - innervation | Oligopeptides - chemical synthesis | Guinea Pigs | Muscle, Smooth - innervation | Models, Molecular | Rats | Rats, Sprague-Dawley | Animals | Analgesics - chemistry | Muscle Contraction - drug effects | Ileum - physiology | Mice | In Vitro Techniques | Oligopeptides - pharmacology | Pain Measurement | Receptors, Opioid, delta - agonists | Vas Deferens - physiology | Neuromuscular Junction - physiology
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14. Full Text δ Opioid Receptor Antagonists: Do They Buy Time for Traumatic Hemorrhagic Shock Patients?
by Duranteau, Jacques and Le Manach, Yannick
Anesthesiology, ISSN 0003-3022, 08/2013, Volume 119, Issue 2, pp. 253 - 255
SURVIVAL | ANESTHESIOLOGY | OPIATE ANTAGONISTS | NALOXONE | Receptors, Opioid, delta - antagonists & inhibitors | Animals | Enkephalin, Leucine - analogs & derivatives | Shock, Hemorrhagic - drug therapy | Narcotic Antagonists - therapeutic use | Enkephalin, Leucine - therapeutic use
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15. Full Text Bi- or multifunctional opioid peptide drugs
by Schiller, Peter W
Life Sciences, ISSN 0024-3205, 2010, Volume 86, Issue 15, pp. 598 - 603
Strategies for the design of bi- or multifunctional drugs are reviewed. A distinction is made between bifunctional drugs interacting in a monovalent fashion... 
Opioid tolerance and dependence | Mixed agonist/antagonists | Bifunctional drugs | Opioid analgesics | MEDICINE, RESEARCH & EXPERIMENTAL | MU-AGONIST/DELTA-ANTAGONIST | PHARMACOLOGICAL CHARACTERIZATION | NEUROKININ-1 RECEPTOR ANTAGONISTS | PHYSICAL-DEPENDENCE | DESIGNED MULTIPLE LIGAND | MORPHINE-TOLERANCE | DELTA-ANTAGONIST | IN-VIVO | PHARMACOLOGY & PHARMACY | LINKED BIFUNCTIONAL PEPTIDES | DMT-TIC PHARMACOPHORE | Humans | Analgesics, Opioid - pharmacology | Narcotic Antagonists - adverse effects | Receptors, Opioid, mu - agonists | Analgesics, Opioid - adverse effects | Animals | Pain - drug therapy | Pain - physiopathology | Narcotic Antagonists - pharmacology | Drug Design | Ligands | Receptors, Opioid, delta - antagonists & inhibitors | Binding Sites
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