217 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.
Clinical Research Institute Of Montreal
[Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.
Nanjing Medical University
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.
Vrije Universiteit Brussel
Evaluation of N-substituent structural variations in opioid receptor profile of LP1.
University Of Catania
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.
Vrije Universiteit Brussel
Multitarget opioid ligands in pain relief: New players in an old game.
University Of Catania
Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands.
University Of Arizona
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective¿-opioid receptor agonists.
Harvard Medical School
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.
University Of Arizona
Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.
University Of Arizona
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
University Of Tsukuba
Design, synthesis, and structure-activity relationship of novel opioid¿ receptor selective agonists:a-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
Kitasato University
Synthesis and Pharmacology of a Novel¿ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton.
Kitasato University
'Carba'-carfentanil (trans isomer): aµ opioid receptor (MOR) partial agonist with a distinct binding mode.
Clinical Research Institute Of Montreal
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.
Vrije Universiteit Brussel
Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6a-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
Virginia Commonwealth University
Methoxyflavones from Stachys glutinosa with binding affinity to opioid receptors: in silico, in vitro, and in vivo studies.
National Research Council
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.
Kitasato University
Novel delta opioid receptor agonists with oxazatricyclodecane structure.
Kitasato University
In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt
Vrije Universiteit Brussel
Endomorphin analogues with mixedµ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lackingß-arrestin2 recruitment activity.
Nanjing Medical University
[Dmt(1)]DALDA analogues with enhancedµ opioid agonist potency and with a mixedµ/¿ opioid activity profile.
Nanjing Medical University
Biological active analogues of the opioid peptide biphalin: mixeda/ß(3)-peptides.
Universit£
The effect of 17-N substituents on the activity of the opioid¿ receptor in nalfurafine derivatives.
Kitasato University
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.
Pfizer
A quantitative structure-activity relationship study of the inhibitory action of a series of enkephalin-like peptides in the guinea pig ileum and mouse vas deferens bioassays.
TBA
Assessment of substitution in the second pharmacophore of Dmt-Tic analogues.
University Of Naples
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 3: synthesis of novel triplet drugs with the bis(epoxymethano) or bis(dimethylepoxymethano) structure (double-capped triplet).
Kitasato University
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: part 3, novel propellane derivatives with pentacyclic skeletons.
Kitasato University
Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
Kitasato University
Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at thed opioid receptor. Discovery of two highly potent and selectived opioid agonists.
Clinical Research Institute Of Montreal
Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
Vrije Universiteit Brussel
cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2.
Universit£
Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associatedµ opioid receptor (MOR-1) splice variants.
Memorial Sloan-Kettering Cancer Center
A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).
Lanzhou University
Tuned-Affinity Bivalent Ligands for the Characterization of Opioid Receptor Heteromers.
TBA
Synthesis of quinolinomorphinan derivatives as highly selectived opioid receptor ligands.
Kitasato University
Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
Kitasato University
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
Kitasato University
Development of potent µ and d opioid agonists with high lipophilicity.
University Of Arizona
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
University Of Arizona
"Carba"-analogues of fentanyl are opioid receptor agonists.
Clinical Research Institute Of Montreal
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
University Of Arizona
Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A.
Harvard Medical School
Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology.
Kitasato University
Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies.
Kitasato University
Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
Vrije Universiteit Brussel
Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.
Stanford University School Of Medicine
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
University Of Ferrara
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Harvard Medical School
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Mclean Hospital
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.
University Of Minnesota
Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors.
University Of Missouri-Columbia
Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
University Of Cagliari
New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
Vrije Universiteit Brussels
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
University Of Arizona
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.
Sapienza University Of Rome
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.
University Of Arizona
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
Southern Research Institute
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University Of Arizona
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
University Of Cagliari
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
National Institute Of Diabetes And Digestive And Kidney Diseases
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the"address" recognition locus.
University Of Minnesota
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
Clinical Research Institute Of Montreal
Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole.
University Of Minnesota
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.
University Of Maryland
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Southern Research Institute
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.
Southern Research Institute
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid r
National Institute Of Diabetes And Digestive And Kidney Diseases
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.
University Of Arizona
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
Smithkline Beecham
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.
University Of Ferrara
Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity.
University Of Minnesota
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.
University Of Minnesota
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
National Institute Of Diabetes And Digestive And Kidney Diseases
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
National Institute Of Diabetes And Digestive And Kidney Diseases
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.
University Of Minnesota
Newly discovered stereochemical requirements in the side-chain conformation of delta opioid agonists for recognizing opioid delta receptors.
University Of Arizona
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.
University Of Arizona
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
University Of Arizona
Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity.
University Of Minnesota
Synthesis and structure-activity relationships of deltorphin analogues.
University Of Ferrara
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
University Of Minnesota
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
TBA
Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
TBA
Oral bioavailability of a new class of micro-opioid receptor agonists containing 3,6-bis[Dmt-NH(CH(2))(n)]-2(1H)-pyrazinone with central-mediated analgesia.
National Institutes Of Environmental Health Sciences
Synthesis and biological activities of YkFA analogues: effects of position 4 substitutions and altered ring size on in vitro opioid activity.
University Of Louisville
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
Research Triangle Institute
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
Research Triangle Institute
Pyrrolooctahydroisoquinolines as potent and selective opioid receptor ligands: SAR analysis and docking studies
TBA
Synthesis of quinolinomorphinan-4-ol derivatives asd opioid receptor agonists.
Kitasato University
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.
University Of Arizona
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
Kitasato University
Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.
Vrije Universiteit Brussel
Discovery of a potent and efficacious peptide derivative ford/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
University Of Arizona
Design and synthesis of KNT-127, ad-opioid receptor agonist effective by systemic administration.
Kitasato University
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.
Sapienza University Of Rome
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
University Of Cagliari
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
University Of Arizona
Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues.
Universit£
Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.
Vrije Universiteit Brussel
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
University Of Arizona
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj
Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain.
University Of Arizona
Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).
Clinical Research Institute Of Montreal
The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
University Of Kansas
Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
The University Of Kansas
Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.
University Of Cagliari
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.
Universit£
Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin I
TBA
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.
Mclean Hospital
Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.
Vrije Universiteit Brussel
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
University Of Arizona
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
National University Of Singapore
Design and synthesis of a metabolically stable and potent antitussive agent, a novel delta opioid receptor antagonist, TRK-851.
Toray Industries
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
University Of Cagliari
Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Lanzhou University
Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.
Kobe Gakuin University
Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Kobe Gakuin University
Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
Clinical Research Institute Of Montreal
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
Medical University
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
University Of Arizona
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
Lanzhou University
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
Kobe Gakuin University
Synthesis of 3,6-bis[H-Tyr/H-Dmt-NH(CH2)m,n]-2(1H)pyrazinone derivatives: function of alkyl chain length on opioid activity.
Kobe Gakuin University
Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.
University Of Arizona
6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
Universidad De Santiago De Compostela
Identification of potent phenyl imidazoles as opioid receptor agonists.
Johnson & Johnson Pharmaceutical Research & Development
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
University Of Cagliari
Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Kobe Gakuin University
Synthesis and biological activity of the first cyclic biphalin analogues.
University Of Arizona
New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Kobe Gakuin University
From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.
University Of Cagliari
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
TBA
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
Lanzhou University
Modulating ?-arrestin 2 recruitment at the ?- and ?-opioid receptors using peptidomimetic ligands.
The Ohio State University
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.
Kobe Gakuin University
A novel cyclic enkephalin analogue with potent opioid antagonist activity.
Clinical Research Institute Of Montreal
Design of a Stable Cyclic Peptide Analgesic Derived from Sunflower Seeds that Targets the ?-Opioid Receptor for the Treatment of Chronic Abdominal Pain.
Medical University Of Vienna
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
University Of Maryland
Isolation and Pharmacological Characterization of Six Opioidergic
University Of Illinois At Chicago
Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.
University Of Maryland
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.
Kobe Gakuin University
Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.
University Of Sydney
Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities.
Tohoku Pharmaceutical University
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University Of Nebraska Medical Center
Synthesis and structure-activity relationships of an orally available and long-acting analgesic peptide, N(alpha)-amidino-Tyr-D-Arg-Phe-MebetaAla-OH (ADAMB).
Daiichi Fine Chemical
Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.
University Of Maryland
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.
University Of California
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
Tohoku Pharmaceutical University
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
Tohoku Pharmaceutical University
Synthesis and evaluation of isothiocyanate-containing derivatives of the delta-opioid receptor antagonist Tyr-Tic-Phe-Phe (TIPP) as potential affinity labels for delta-opioid receptors.
University Of Maryland
Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues.
Virginia Commonwealth University
Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit ?-Arrestin-2.
Memorial Sloan Kettering Cancer Center
Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.
Hungarian Academy Of Sciences
Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.
University Of Louisville
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
Sapienza University Of Rome
Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.
University Of Arizona
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.
The University Of Arizona
Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as ?/? Opioid Receptor Dual Selective Ligands.
Virginia Commonwealth University
7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands.
University Of Minnesota
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.
National Institute Of Environmental Health Sciences
Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators.
Virginia Commonwealth University
Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
University Of Arizona
Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.
University Of Arizona
Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides.
University Of Ferrara
Discovery of Novel Multifunctional Ligands with ?/? Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.
University Of Arizona
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.
University Of Arizona
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
University Of Arizona
The most effective influence of 17-(3-ethoxypropyl) substituent on the binding affinity and the agonistic activity in KNT-127 derivatives, ? opioid receptor agonists.
Kitasato University
N-Alkyl dien- and trienamides from the roots of Otanthus maritimus with binding affinity for opioid and cannabinoid receptors.
Uos Of Cagliari
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
University Of Arizona
Synthesis and biological evaluation of novel delta (?) opioid receptor ligands with diazatricyclodecane skeletons.
C.N.R. Istituto Di Farmacologia Traslazionale
Systematic replacement of amides by 1,4-disubstituted[1,2,3]triazoles in Leu-enkephalin and the impact on the delta opioid receptor activity.
Universit£
Structure activity relationship studies of 17-cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affinity and function.
Virginia Commonwealth University
N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.
Clinical Research Institute Of Montreal
Development of a model for the delta opioid receptor pharmacophore. 2. Conformationally restricted Phe3 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).
University Of Michigan
Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).
University Of Michigan
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.
Universit£
Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group.
Smithkline Beecham Farmaceutici
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton having a 7-amide side chain and their pharmacologies.
Kitasato University
Stereoisomers of N-[1-hydroxy-(2-phenylethyl)-3-methyl-4-piperidyl]- N-phenylpropanamide: synthesis, stereochemistry, analgesic activity, and opioid receptor binding characteristics.
Institute Of Materia Medica
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.
University Of Minnesota
Structure-activity relationships of cyclic opioid peptide analogues containing a phenylalanine residue in the 3-position.
Clinical Research Institute Of Montreal
?-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.
Vrije Universiteit Brussel
Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.
Eisai
Novel delta opioid receptor agonists with oxazatricyclodecane structure showing potent agonistic activities.
Kitasato University
Conformationally restricted deltorphin analogues.
Clinical Research Institute Of Montreal
Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity.
University Of Arizona
Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.
Columbia University
Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.
Temple University
Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine.
Memorial Sloan-Kettering Cancer Center
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.
Case Western Reserve University
In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.
WestfÄLische Wilhelms-UniversitÄ
Dynorphin A analogs containing a conformationally constrained phenylalanine derivative in position 4: reversal of preferred stereochemistry for opioid receptor affinity and discrimination of kappa vs. delta receptors.
University Of Maryland
Synthesis and in vitro opioid activity profiles of DALDA analogues.
Clinical Research Institute Of Montreal
Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.
Hungarian Academy Of Sciences
Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group.
Loughborough University
Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity.
University Of Rochester
Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain.
Memorial Sloan-Kettering Cancer Center
Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Sri International
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Janssen Research Foundation