283 articles for thisTarget
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Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective¿-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
Dr. August Wolff Gmbh & Co. Kg Arzneimittel
Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.
West Virginia University School Of Pharmacy
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s
University Of Catania
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
Conformationally restricted¿-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
Mercachem
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
'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
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
University Of Bath
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.
University Of Bath
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
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.
Lanzhou University
Biological active analogues of the opioid peptide biphalin: mixeda/ß(3)-peptides.
Universit£
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.
Pfizer
Assessment of substitution in the second pharmacophore of Dmt-Tic analogues.
University Of Naples
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: part 3, novel propellane derivatives with pentacyclic skeletons.
Kitasato University
Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
Vrije Universiteit Brussel
Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversibleµ opioid receptor antagonist effects.
University Of Bristol
cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2.
Universit£
A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).
Lanzhou University
The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues.
Universit£
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
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
Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Kitasato University
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
University Of Arizona
Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.
Kitasato University
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Adolor
14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
University Of Bath
Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
Kitasato University
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Rensselaer Polytechnic Institute
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.
Toray Industries
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
Synthesis of bridged piperazines with sigma receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie
Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors.
University Of Missouri-Columbia
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
University Of Bristol
Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
University Of Cagliari
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
University Of Bristol
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.
University Of Kentucky
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
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.
Universit£
Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.
University Of Vermont
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
University Of California
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
Research Triangle Institute
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
University Of Cagliari
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
University Of Innsbruck
[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
Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functional studies.
Pharmazeutisches Institut Der Universit£T Freiburg
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Research Triangle Institute
Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.
University Of Bristol
Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.
Rensselaer Polytechnic Institute
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
Harvard Medical School
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.
National Institute Of Diabetes
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
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
Research Triangle Institute
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
University Of Washington
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
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.
University Of Ferrara
Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide"address" recognition at kappa opioid receptors.
University Of Minnesota
Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.
University Of Minnesota
The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid recepto
University Of Arizona
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
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
University Of Washington
7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice.
University Of Minnesota
Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime.
University Of Innsbruck
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
Clinical Research Institute Of Montreal
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
University Of Washington
Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide.
University Of Washington
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
Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor.
University Of Minnesota
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
University Of Arizona
Possible contribution of a glutathione conjugate to the long-duration action of beta-funaltrexamine.
University Of Minnesota
A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists.
University Of Minnesota
Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity.
University Of Minnesota
A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists.
University Of Minnesota
Substitution on the Phe3 aromatic ring in cyclic delta opioid receptor-selective dermorphin/deltorphin tetrapeptide analogues: electronic and lipophilic requirements for receptor affinity.
University Of Michigan
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.
Oregon State University
O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
University Of Washington
Incorporation of a novel conformationally restricted tyrosine analog into a cyclic, delta opioid receptor selective tetrapeptide (JOM-13) enhances delta receptor binding affinity and selectivity.
University Of Michigan
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
University Of Minnesota
Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors.
Zambeletti Research Laboratories
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
University Of Washington
Selective reversible and irreversible ligands for the kappa opioid receptor.
National Taiwan University
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
University Of Minnesota
Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
University Of Minnesota
Synthesis and structure-activity relationships of deltorphin analogues.
University Of Ferrara
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
University Of Minnesota
Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity.
Parke-Davis Research Unit
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
University Of Minnesota
Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.
Ciba-Geigy
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.
Parke-Davis Research Unit
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.
University Of Paris
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
University Of Minnesota
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
TBA
Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides.
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, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.
Southern Research Institute
Synthesis and biological activities of YkFA analogues: effects of position 4 substitutions and altered ring size on in vitro opioid activity.
University Of Louisville
Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.
University Of Bristol
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
Harvard Medical School
3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.
Pharmacia
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.
University Of Bristol
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
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.
University Of Michigan
A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.
University Of Michigan
Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the -selective opioid receptor antagonist cyprodime
TBA
Neurotensin receptor binding and antinociceptive activity for lipophilic N-amido neurotensin(913) analogs
TBA
Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.
University Of Pavia
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.
University Of Arizona
Synthesis, biological evaluation, and automated docking of constrained analogues of the opioid peptide H-Dmt-D-Ala-Phe-Gly-NH2 using the 4- or 5-methyl substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one scaffold.
Vrije Universiteit Brussel
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
Kitasato University
Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
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
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
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
Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
Kitasato University
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
Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
Kitasato University
Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).
University Of Pavia
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
Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain.
University Of Arizona
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
The University Of Kansas
Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).
Clinical Research Institute Of Montreal
Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.
University Of Cagliari
Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative.
Kitasato University
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.
Universit£
6N-Cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions
TBA
Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists
TBA
Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogs
TBA
Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin I
TBA
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
A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
University Of Ferrara
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
Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore.
University Of Cagliari
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.
University Of Arizona
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 and highly selective chiral tri-amine and tetra-amine mu opioid receptors ligands: an example of lead optimization using mixture-based libraries.
Institute For Molecular Studies
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
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
Lanzhou University
Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).
Kobe Gakuin University
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.
Kobe Gakuin University
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
University Of Cagliary
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
Johnson & Johnson Pharmaceutical Research & Development
A novel cyclic enkephalin analogue with potent opioid antagonist activity.
Clinical Research Institute Of Montreal
Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.
University Of Cagliary
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Biological Research Center Of The Hungarian Academy Of Sciences
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
Harvard Medical School
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.
Kobe Gakuin University
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
Rensselaer Polytechnic Institute
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain.
Huazhong University Of Science And Technology
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
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
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
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.
Niddk
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
Tohoku Pharmaceutical University
Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.
Hungarian Academy Of Sciences
Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.
The University Of Arizona
Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.
University Of Louisville
Progress in the development of more effective and safer analgesics for pain management.
University Of Catania
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety.
Universit£T M£Nster
Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic ?-Opioid Receptor (MOR) Agonist/?-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.
University Of Michigan
Development of Novel Quinoxaline-Based ?-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
Universit£T M£Nster
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
Research Triangle Institute
C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.
National Taiwan University
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
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
Research Triangle Institute
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Research Triangle Institute
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.
National Institute Of Environmental Health Sciences
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the"address" sequence.
Oregon State University
Aspartic acid conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1(3-aminophenyl)-2-(1-pyrrolidi nyl) ethyl]acetamide: kappa opioid receptor agonists with limited access to the central nervous system.
University Of Minnesota
Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
University Of Arizona
Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
University Of Arizona
Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.
University Of Arizona
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Universitá
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
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: an opioid receptor affinity label that produces selective and long-lasting kappa antagonism in mice.
University Of Minnesota
Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration.
Medical University Of Lodz
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
University Of Arizona
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.
Eli Lilly
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
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
University Of Arizona
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.
Universit£
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.
National Taiwan University
Orally active opioid compounds from a non-poppy source.
Temple University School Of Pharmacy
Highly kappa receptor-selective dynorphin A analogues with modifications in position 3 of dynorphin A(1-11)-NH2.
University Of Arizona
kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists.
University Of Minnesota
Electrophilic N-benzylnaltrindoles as delta opioid receptor-selective antagonists.
University Of Minnesota
Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids.
Eastern Michigan University
Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
University Of Arizona
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.
University Of Minnesota
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.
TBA
Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands.
Chiba University
Selective kappa opioid antagonists for treatment of addiction, are we there yet?
University Of Science And Technology
Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review.
University Of Catania
Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors.
TBA
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
TBA
Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic ? Receptor Ligands with Exocyclic Amino Moiety.
Universit£T M£Nster
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
Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
University Of Arizona
Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.
Eisai
Modification of the enkephalin"message" with an artificial polycationic C-terminus.
Case Western Reserve University
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.
Anaquest
(2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics.
Zambeletti Research Laboratories
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.
Zambeletti Research Laboratories
Conformationally restricted deltorphin analogues.
Clinical Research Institute Of Montreal
Synthesis and evaluation of a ligand targeting the? and? opioid receptors for drug delivery to lung cancer.
Purdue University
Iminothiazoline-Sulfonamide Hybrids as Jack Bean Urease Inhibitors; Synthesis, Kinetic Mechanism and Computational Molecular Modeling.
Quaid-I-Azam University