Terguride stimulates locomotor activity at 2 months but not 10 months after 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine treatment of common marmosets [PDF]
, 1992 The mixed dopamine (DA) agonist/antagonist terguride acts as a DA antagonist on normosensitive receptors but shows DA agonistic properties at supersensitive DA receptors.
Horowski, R. +6 more
core +1 more source
Cannabigerol Action at Cannabinoid CB1 and CB2 Receptors and at CB1–CB2 Heteroreceptor Complexes
Frontiers in Pharmacology, 2018 Cannabigerol (CBG) is one of the major phytocannabinoids present in Cannabis sativa L. that is attracting pharmacological interest because it is non-psychotropic and is abundant in some industrial hemp varieties.
Gemma Navarro +17 more
doaj +1 more source
Agonist-directed desensitization of the β2-adrenergic receptor. [PDF]
PLoS ONE, 2011 The β(2)-adrenergic receptor (β(2)AR) agonists with reduced tachyphylaxis may offer new therapeutic agents with improved tolerance profile. However, receptor desensitization assays are often inferred at the single signaling molecule level, thus ligand ...
Vasiliy Goral +5 more
doaj +1 more source
Ligand-Specific Regulation of the Endogenous Mu-Opioid Receptor by Chronic Treatment with Mu-Opioid Peptide Agonist [PDF]
, 2013 Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors, several analogues have been synthesized to improve their binding and pharmacological profiles.
Birkás, Erika +12 more
core +3 more sources
eLife, 2022 To clarify the determinants of agonist efficacy in pentameric ligand-gated ion channels, we examined a new compound, aminomethanesulfonic acid (AMS), a molecule intermediate in structure between glycine and taurine.
Josip Ivica +4 more
doaj +1 more source
Determining the neurotransmitter concentration profile at active synapses [PDF]
, 2009 Establishing the temporal and concentration profiles of neurotransmitters during synaptic release is an essential step towards understanding the basic properties of inter-neuronal communication in the central nervous system.
A Barberis +144 more
core +2 more sources
Treatment of type 2 diabetes by free fatty acid receptor agonists [PDF]
, 2014 Dietary free fatty acids (FFAs), such as ω-3 fatty acids, regulate metabolic and anti-inflammatory processes, with many of these effects attributed to FFAs interacting with a family of G protein-coupled receptors.
Hudson, Brian D. +3 more
core +2 more sources
TRAF2 binds to TIFA via a novel motif and contributes to its autophagic degradation
FEBS Letters, EarlyView.TRAF family members couple receptor signalling complexes to downstream outputs, but how they interact with these complexes is not always clear. Here, we show that during ADP‐heptose signalling, TRAF2 binding to TIFA requires two short sequence motifs in the C‐terminal tail of TIFA, which are distinct from the TRAF6 binding motif.
Tom Snelling +4 more
wiley +1 more source
Label-free phenotypic profiling identified D-luciferin as a GPR35 agonist. [PDF]
PLoS ONE, 2012 Fluorescent and luminescent probes are essential to both in vitro molecular assays and in vivo imaging techniques, and have been extensively used to measure biological function.
Haibei Hu, Huayun Deng, Ye Fang
doaj +1 more source
Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]
, 2018 The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J. +14 more
core +1 more source