Modulation of opioid receptor ligand affinity and efficacy using active and inactive state receptor models.
about
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.C7β-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.Opioid peptidomimetics: leads for the design of bioavailable mixed efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligandsEffects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) LigandsMolecular Pharmacology of δ-Opioid Receptors.N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.The behavioral effects of a mixed efficacy antinociceptive peptide, VRP26, following chronic administration in mice.Development of a bioavailable μ opioid receptor (MOPr) agonist, δ opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.Translation of structure-activity relationships from cyclic mixed efficacy opioid peptides to linear analoguesAsymmetric synthesis and in vitro and in vivo activity of tetrahydroquinolines featuring a diverse set of polar substitutions at the 6 position as mixed-efficacy μ opioid receptor/δ opioid receptor ligands.Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.Design, synthesis, and biological evaluation of a series of bifunctional ligands of opioids/SSRIs.Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligandsPlacement of Hydroxy Moiety on Pendant of Peptidomimetic Scaffold Modulates Mu and Kappa Opioid Receptor Efficacy.In Vivo Effects of μ Opioid Receptor Agonist/δ Opioid Receptor Antagonist Peptidomimetics Following Acute and Repeated Administration.
P2860
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P2860
Modulation of opioid receptor ligand affinity and efficacy using active and inactive state receptor models.
description
2012 nî lūn-bûn
@nan
2012年の論文
@ja
2012年学术文章
@wuu
2012年学术文章
@zh-cn
2012年学术文章
@zh-hans
2012年学术文章
@zh-my
2012年学术文章
@zh-sg
2012年學術文章
@yue
2012年學術文章
@zh
2012年學術文章
@zh-hant
name
Modulation of opioid receptor ...... nactive state receptor models.
@en
Modulation of opioid receptor ...... nactive state receptor models.
@nl
type
label
Modulation of opioid receptor ...... nactive state receptor models.
@en
Modulation of opioid receptor ...... nactive state receptor models.
@nl
prefLabel
Modulation of opioid receptor ...... nactive state receptor models.
@en
Modulation of opioid receptor ...... nactive state receptor models.
@nl
P2093
P2860
P356
P1476
Modulation of opioid receptor ...... nactive state receptor models.
@en
P2093
Henry I Mosberg
Irina D Pogozheva
Jessica P Anand
John R Traynor
Lauren C Purington
P2860
P304
P356
10.1111/CBDD.12014
P577
2012-09-12T00:00:00Z