Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists. - Wikidata - wikimedia - TriplyDB

Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.

Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.

http://www.wikidata.org/entity/Q33893723

about

Behavioral and cellular pharmacology characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) as a mu opioid receptor selective ligand.Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.N-naphthoyl-beta-naltrexamine (NNTA), a highly selective and potent activator of μ/kappa-opioid heteromers Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associated μ opioid receptor (MOR-1) splice variants.Effects of the novel, selective and low-efficacy mu opioid receptor ligand NAQ on intracranial self-stimulation in rats.Preclinical disposition (in vitro) of novel μ-opioid receptor selective antagonists.Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity Design and synthesis of a bivalent ligand to explore the putative heterodimerization of the mu opioid receptor and the chemokine receptor CCR5.Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands Characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives as novel leads to development of mu opioid receptor selective antagonists.6β-N-heterocyclic substituted naltrexamine derivative NAP as a potential lead to develop peripheral mu opioid receptor selective antagonists.Synthesis and characterization of a dual kappa-delta opioid receptor agonist analgesic blocking cocaine reward behavior Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan derivatives as peripheral selective μ opioid receptor Agents.A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.Antinociceptive Interactions between the Imidazoline I2 Receptor Agonist 2-BFI and Opioids in Rats: Role of Efficacy at the μ-Opioid Receptor.Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of m Novel 6β-acylaminomorphinans with analgesic activity.17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-(4'-pyridylcarboxamido)morphinan (NAP) Modulating the Mu Opioid Receptor in a Biased Fashion Structure selectivity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists.Binding mode analyses of NAP derivatives as mu opioid receptor selective ligands through docking studies and molecular dynamics simulation.Synthesis and evaluation of a ligand targeting the μ and δ opioid receptors for drug delivery to lung cancer.Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.Nanoconjugated NAP as a Potent and Periphery Selective Mu Opioid Receptor Modulator To Treat Opioid-Induced Constipation.Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.Application of receptor theory to the design and use of fixed-proportion mu-opioid agonist and antagonist mixtures in rhesus monkeys.

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P2860

Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.

http://www.wikidata.org/entity/Q33893723

description

2009 nî lūn-bûn

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2009 թուականի Մարտին հրատարակուած գիտական յօդուած

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2009 թվականի մարտին հրատարակված գիտական հոդված

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2009年の論文

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2009年論文

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2009年論文

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2009年論文

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2009年論文

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2009年論文

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2009年论文

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Design, synthesis, and biologi ...... eceptor selective antagonists.

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Design, synthesis, and biologi ...... eceptor selective antagonists.

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Design, synthesis, and biologi ...... eceptor selective antagonists.

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Design, synthesis, and biologi ...... eceptor selective antagonists.

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Design, synthesis, and biologi ...... eceptor selective antagonists.

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Design, synthesis, and biologi ...... eceptor selective antagonists.

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Journal of Medicinal Chemistry

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Design, synthesis, and biologi ...... eceptor selective antagonists.

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P2093

Bichoy H Gabra

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Dana E Selley

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David L Stevens

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Guo Li

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Jianyang Chen

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Lindsey C Aschenbach

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Michael P Cassidy

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Richard B Westkaemper

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William L Dewey

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Yan Zhang

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P2860

High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor

Crystal structure of a photoactivated deprotonated intermediate of rhodopsin

Advances in Determination of a High-Resolution Three-Dimensional Structure of Rhodopsin, a Model of G-Protein-Coupled Receptors (GPCRs)

Crystal structure of the human beta2 adrenergic G-protein-coupled receptor

A Specific Cholesterol Binding Site Is Established by the 2.8 Å Structure of the Human β2-Adrenergic Receptor

Crystal structure of the ligand-free G-protein-coupled receptor opsin

Structure of a beta1-adrenergic G-protein-coupled receptor.

SOME NARCOTIC ANTAGONISTS IN THE BENZOMORPHAN SERIES

GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function

Model structures of alpha-2 adrenoceptors in complex with automatically docked antagonist ligands raise the possibility of interactions dissimilar from agonist ligands.

P304

1416-1427

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10.1021/JM801272C

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