RGS4 regulates partial agonism of the M2 muscarinic receptor-activated K+ currents. [PDF]
, 2014 Partial agonists are used clinically to avoid overstimulation of receptor-mediated signalling, as they produce a submaximal response even at 100% receptor occupancy.
Chen, I-Shan +3 more
core +2 more sources
Novel 2-amino-isoflavones exhibit aryl hydrocarbon receptor agonist or antagonist activity in a species/cell-specific context [PDF]
, 2012 The aryl hydrocarbon receptor (AhR) mediates the induction of a variety of xenobiotic metabolism genes. Activation of the AhR occurs through binding to a group of structurally diverse compounds, most notably dioxins, which are exogenous ligands ...
BALBONI, GIANFRANCO +10 more
core +1 more source
Opioid regulation of Mu receptor internalisation: relevance to the development of tolerance and dependence [PDF]
, 2010 Internalisation of the mu opioid receptor from the surface of cells is generally achieved by receptor occupancy with agonist ligands of high efficacy. However, in many situations the potent analgesic morphine fails to promote internalisation effectively ...
Lopez-Gimenez, J.F., Milligan, G.
core +2 more sources
Cyclic nucleotide-gated channels: structural basis of ligand efficacy and allosteric modulation [PDF]
, 1997 Most working proteins, including metabolic enzymes, transcription regulators, and membrane receptors, transporters, and ion channels, share the property of allosteric coupling. The term 'allosteric' means that these proteins mediate indirect interactions
Lester, Henry A. +2 more
core +1 more source
Pharmaceutical Fronts, 2022 Evidence suggested that the use of partial dopamine D2/D3 receptor agonists may be a better choice for the treatment of Parkinson's disease (PD), and the stimulation of 5-HT1A receptors (mainly via nondopaminergic mechanisms) alleviates motor and ...
Xin-Li Du +7 more
doaj +1 more source
G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease [PDF]
, 2015 G protein-coupled receptor 35 (GPR35) is an orphan receptor, discovered in 1998, that has garnered interest as a potential therapeutic target through its association with a range of diseases.
Amanda E Mackenzie +4 more
core +3 more sources
Differential Effects of D-Cycloserine and ACBC at NMDA Receptors in the Rat Entorhinal Cortex Are Related to Efficacy at the Co-Agonist Binding Site. [PDF]
PLoS ONE, 2015 Partial agonists at the NMDA receptor co-agonist binding site may have potential therapeutic efficacy in a number of cognitive and neurological conditions. The entorhinal cortex is a key brain area in spatial memory and cognitive processing.
Alex M Lench +2 more
doaj +1 more source
Pharmacological Characterization of Dezocine, a Potent Analgesic Acting as a κ Partial Agonist and μ Partial Agonist. [PDF]
Sci Rep, 2018 AbstractDezocine is becoming dominated in China market for relieving moderate to severe pain. It is believed that Dezocine’s clinical efficacy and little chance to provoke adverse events during the therapeutic process are mainly attributed to its partial agonist activity at the μ opioid receptor.
Wang YH +11 more
europepmc +5 more sources
In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]
, 2018 Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta +4 more
core +2 more sources
Partial Agonists for A3 Adenosine Receptors [PDF]
Current Topics in Medicinal Chemistry, 2004 AbstractFor Abstract see ChemInform Abstract in Full Text.
Kenneth A. Jacobson, Zhan-Guo Gao
openaire +4 more sources