In a Rat Model of Opioid Maintenance, the G Protein–Biased Mu Opioid Receptor Agonist TRV130 Decreases Relapse to Oxycodone Seeking and Taking and Prevents Oxycodone-Induced Brain Hypoxia
Sign Up to like & getrecommendations! Published in 2020 at "Biological Psychiatry"
DOI: 10.1016/j.biopsych.2020.02.014
Abstract: BACKGROUND Maintenance treatment with opioid agonists (buprenorphine, methadone) is effective for opioid addiction but does not eliminate opioid use in all patients. We modeled maintenance treatment in rats that self-administered the prescription opioid oxycodone. The… read more here.
Keywords: oxycodone seeking; protein biased; maintenance; biased opioid ... See more keywords
Effectiveness comparisons of G-protein biased and unbiased mu opioid receptor ligands in warm water tail-withdrawal and drug discrimination in male and female rats
Sign Up to like & getrecommendations! Published in 2019 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2019.01.020
Abstract: &NA; One emerging strategy to address the opioid crisis is the development of mu opioid receptor (MOR) ligands that preferentially signal the G‐protein vs. &bgr;‐arrestin pathway. The present study compared the relative potency and effectiveness… read more here.
Keywords: tail withdrawal; protein biased; stimulus effects; mor ... See more keywords
G-protein Biased Signaling Agonists of Dopamine D3 Receptor Promote Distinct Activation Patterns of ERK1/2.
Sign Up to like & getrecommendations! Published in 2022 at "Pharmacological research"
DOI: 10.1016/j.phrs.2022.106223
Abstract: Dopamine D3 receptors (D3R) have a causal role in neurological and psychiatric disorders. We have developed a novel class of G-protein biased (GPB) signaling D3R agonists with minimal β-arrestin2 (βarr2) recruitment and demonstrated efficacy in… read more here.
Keywords: activation; protein biased; phosphorylation; gpb agonists ... See more keywords
Discovery of G Protein-Biased Ligands against 5-HT7R.
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DOI: 10.1021/acs.jmedchem.1c00110
Abstract: There has been significant attention concerning the biased agonism of G protein-coupled receptors (GPCRs), and it has resulted in various pharmacological benefits. 5-HT7R belongs to a GPCR, and it is a promising pharmaceutical target for… read more here.
Keywords: protein; biased ligands; ligands ht7r; discovery protein ... See more keywords
Novel glucagon-like peptide-1 analogue exhibits potency-driven G-protein biased agonism with promising effects on diabetes and diabetic dry eye syndrome
Sign Up to like & getrecommendations! Published in 2022 at "Bioengineered"
DOI: 10.1080/21655979.2022.2031418
Abstract: ABSTRACT Glucagon-like peptide-1 receptor agonists (GLP-1RAs) are considered as effective treatments for type 2 diabetes. Here, we describe the in vitro characteristics and in vivo anti-diabetic efficacies of a novel GLP-1RA, termed SM102. The in… read more here.
Keywords: eye syndrome; dry eye; glucagon like; potency driven ... See more keywords
Endothelial‐protective effects of a G‐protein‐biased sphingosine‐1 phosphate receptor‐1 agonist, SAR247799, in type‐2 diabetes rats and a randomized placebo‐controlled patient trial
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DOI: 10.1111/bcp.14632
Abstract: SAR247799 is a G‐protein‐biased sphingosine‐1 phosphate receptor‐1 (S1P1) agonist designed to activate endothelial S1P1 and provide endothelial‐protective properties, while limiting S1P1 desensitization and consequent lymphocyte‐count reduction associated with higher doses. The aim was to show… read more here.
Keywords: endothelial protective; biased sphingosine; sar247799; sphingosine phosphate ... See more keywords
The G‐protein‐biased agents PZM21 and TRV130 are partial agonists of μ‐opioid receptor‐mediated signalling to ion channels
Sign Up to like & getrecommendations! Published in 2019 at "British Journal of Pharmacology"
DOI: 10.1111/bph.14702
Abstract: Opioids remain the most efficient medications against severe pain; they act on receptors that couple to heterotrimeric G‐proteins in the Gαi/o family. Opioids exert many of their acute effects through modulating ion channels via Gβγ… read more here.
Keywords: ion channels; pzm21 trv130; agents pzm21; biased agents ... See more keywords