88 articles for thisTarget
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Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.
Johns Hopkins Medical Institutions
Irreversible blockage of opioid receptor types by ester homologues of beta-funaltrexamine.
TBA
Synthesis and biological activity of analogues of beta-chlornaltrexamine and beta-funaltrexamine at opioid receptors.
TBA
Replacement of the peptide-backbone amides connecting Tyr-Gly and Gly-Gly in leucine-enkephalin with ketomethylene groups: synthesis and biological activity.
TBA
Diastereomeric 6-desoxy-6-spiro-alpha-methylene-gamma-butyrolactone derivatives of naltrexone and oxymorphone. Selective irreversible inhibition of naltrexone binding in an opioid receptor preparation by a conformationally restricted michael acceptor ligand.
TBA
N-Methylnalorphine: definition of N-allyl conformation for antagonism at the opiate receptor.
TBA
Synthesis and pharmacology of metabolically stable tert-butyl ethers of morphine and levorphanol.
TBA
Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.
University of Arizona
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
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
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.
Lanzhou University
The effect of 17-N substituents on the activity of the opioid¿ receptor in nalfurafine derivatives.
Kitasato University
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
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
Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associatedµ opioid receptor (MOR-1) splice variants.
Memorial Sloan-Kettering Cancer Center
Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixedµ/d opioid receptor agonistic properties.
Vrije Universiteit Brussel
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
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
Kitasato University
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
Kitasato University
Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology.
Kitasato University
Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies.
Kitasato University
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
University of Maryland
Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
Biological Research Center of The Hungarian Academy of Sciences
18F-labeled sufentanil for PET-imaging of mu-opioid receptors.
Technische Universit£T M£Nchen
Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.
University of Northern Colorado
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
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
Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties.
Virginia Commonwealth University
Possible contribution of a glutathione conjugate to the long-duration action of beta-funaltrexamine.
University of Minnesota
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
University of Minnesota
Benzofuro[2,3-c]pyridin-6-ols: synthesis, affinity for opioid-receptor subtypes, and antinociceptive activity.
Ciba-Geigy
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
TBA
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.
Merck
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 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 and synthesis of KNT-127, ad-opioid receptor agonist effective by systemic administration.
Kitasato University
Synthesis and opioid activity of novel 6-substituted-6-demethoxy-ethenomorphinans.
University of Debrecen
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
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.
University of Szeged
Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists.
Johnson and Johnson Pharmaceutical Research and Development
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Biological Research Center of The Hungarian Academy of Sciences
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
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
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
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Synaptic Pharmaceutical
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
Sapienza University of Rome
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
Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators.
Virginia Commonwealth University
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
Solvay Duphar Research Laboratories
Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors.
University of Ferrara
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
Synthesis and biological evaluation of novel delta (?) opioid receptor ligands with diazatricyclodecane skeletons.
C.N.R. Istituto Di Farmacologia Traslazionale
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
Access to 7?-analogs of codeine with mixed ?/? agonist activity via 6,7-?-epoxide opening.
University of Texas At Austin
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
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
A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers.
University of Minnesota
Design and synthesis of naltrexone-derived affinity labels with nonequilibrium opioid agonist and antagonist activities. Evidence for the existence of different mu receptor subtypes in different tissues.
TBA
?-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
Novel delta opioid receptor agonists with oxazatricyclodecane structure showing potent agonistic activities.
Kitasato University
Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide.
University of Notre Dame
Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents.
Hazara University