PMID

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Article Title

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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

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

Novel diazabicycloalkane delta opioid agonists.

Istituto Di Farmacologia Traslazionale

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

Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: part 3, novel propellane derivatives with pentacyclic skeletons.

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

Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.

Toray Industries

Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase.

University Of Washington

Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.

University Of Northern Colorado

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

Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.

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

 

Pyrrolooctahydroisoquinolines as potent and selective opioid receptor ligands: SAR analysis and docking studies

TBA

Synthesis and biological evaluation of dibenz[b,f][1,5]oxazocine derivatives for agonist activity at κ-opioid receptor.

Indian Institute Of Chemical Biology

 

6N-Cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions

TBA

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

7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands.

University Of Minnesota

Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.

Solvay Duphar Research Laboratories

Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group.

Smithkline Beecham Farmaceutici

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

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