Development of functionally selective, small molecule agonists at kappa opioid receptors.
about
Salvinorin A, a kappa-opioid receptor agonist hallucinogen: pharmacology and potential template for novel pharmacotherapeutic agents in neuropsychiatric disordersGaddum Memorial Lecture 2014: receptors as an evolving concept: from switches to biased microprocessorsMolecular switches of the κ opioid receptor triggered by 6'-GNTI and 5'-GNTI.The G protein-biased κ-opioid receptor agonist RB-64 is analgesic with a unique spectrum of activities in vivoCurrent approaches for the discovery of drugs that deter substance and drug abuse.Determination of sites of U50,488H-promoted phosphorylation of the mouse κ opioid receptor (KOPR): disconnect between KOPR phosphorylation and internalizationEffects of kappa opioid receptors on conditioned place aversion and social interaction in males and femalesSelective κ receptor partial agonist HS666 produces potent antinociception without inducing aversion after i.c.v. administration in mice.Putative kappa opioid heteromers as targets for developing analgesics free of adverse effects.Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2.Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.Pharmacology and anti-addiction effects of the novel κ opioid receptor agonist Mesyl Sal B, a potent and long-acting analogue of salvinorin AA novel method for analyzing extremely biased agonism at G protein-coupled receptors.Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motifIntrinsic relative activities of κ opioid agonists in activating Gα proteins and internalizing receptor: Differences between human and mouse receptors.Quantitative Signaling and Structure-Activity Analyses Demonstrate Functional Selectivity at the Nociceptin/Orphanin FQ Opioid Receptor.Fulfilling the Promise of "Biased" G Protein-Coupled Receptor Agonism.Identification of the Kappa-Opioid Receptor as a Therapeutic Target for Oligodendrocyte Remyelination.Opioid receptors: Structural and mechanistic insights into pharmacology and signaling.Investigation of the role of βarrestin2 in kappa opioid receptor modulation in a mouse model of pruritusSupersensitive Kappa Opioid Receptors Promotes Ethanol Withdrawal-Related Behaviors and Reduce Dopamine Signaling in the Nucleus Accumbens.Biased G Protein-Coupled Receptor Signaling: New Player in Modulating Physiology and PathologyBiased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria.Minireview: More than just a hammer: ligand "bias" and pharmaceutical discovery.Synthesis of Kappa Opioid Antagonists Based On Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence.Neuronal extracellular signal-regulated kinase (ERK) activity as marker and mediator of alcohol and opioid dependence.Does the kappa opioid receptor system contribute to pain aversion?Characterization of Structurally Novel G Protein Biased CB1 Agonists: Implications for Drug Development.Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor.Biased agonism: An emerging paradigm in GPCR drug discovery.Approaches to Assess Functional Selectivity in GPCRs: Evaluating G Protein Signaling in an Endogenous Environment.Structure-activity relationship studies of functionally selective kappa opioid receptor agonists that modulate ERK 1/2 phosphorylation while preserving G protein over βarrestin2 signaling bias.Endogenous opioid system: a promising target for future smoking cessation medications.Discovery of G Protein-Biased EP2 Receptor Agonists.The Diverse Roles of Arrestin Scaffolds in G Protein-Coupled Receptor Signaling.Human native kappa opioid receptor functions not predicted by recombinant receptors: Implications for drug designDiscovery of novel brain permeable and G protein-biased beta-1 adrenergic receptor partial agonists for the treatment of neurocognitive disorders.Placement of Hydroxy Moiety on Pendant of Peptidomimetic Scaffold Modulates Mu and Kappa Opioid Receptor Efficacy.Dissociable effects of the kappa opioid receptor agonist nalfurafine on pain/itch-stimulated and pain/itch-depressed behaviors in male rats.Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics.
P2860
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P2860
Development of functionally selective, small molecule agonists at kappa opioid receptors.
description
2013 nî lūn-bûn
@nan
2013年の論文
@ja
2013年学术文章
@wuu
2013年学术文章
@zh-cn
2013年学术文章
@zh-hans
2013年学术文章
@zh-my
2013年学术文章
@zh-sg
2013年學術文章
@yue
2013年學術文章
@zh
2013年學術文章
@zh-hant
name
Development of functionally selective, small molecule agonists at kappa opioid receptors.
@en
Development of functionally selective, small molecule agonists at kappa opioid receptors.
@nl
type
label
Development of functionally selective, small molecule agonists at kappa opioid receptors.
@en
Development of functionally selective, small molecule agonists at kappa opioid receptors.
@nl
prefLabel
Development of functionally selective, small molecule agonists at kappa opioid receptors.
@en
Development of functionally selective, small molecule agonists at kappa opioid receptors.
@nl
P2093
P2860
P50
P356
P1476
Development of functionally selective, small molecule agonists at kappa opioid receptors.
@en
P2093
Angela M Phillips
Cullen L Schmid
Edward Stahl
Franck Madoux
Kevin J Frankowski
Kimberly M Lovell
Laura M Bohn
Michael D Cameron
Peter Hodder
P2860
P304
36703-36716
P356
10.1074/JBC.M113.504381
P407
P577
2013-11-01T00:00:00Z