Decoding kratom: molecular mechanisms and epigenetic factors in use and dependence. [PDF]
Transl PsychiatryMisnan E +4 more
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Partial agonist antipsychotic drugs differentially interact with a secondary binding site at the dopamine D2 receptor. [PDF]
Int J NeuropsychopharmacolÅgren R, Sahlholm K.
europepmc +1 more source
Recent Advances of Azobenzene-Based Photoresponsive Molecular Switches for Protein-Targeted Photopharmacology. [PDF]
MoleculesJiang J, Yuan X, Hu L.
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Activation of G protein gated inwardly rectifying potassium (GIRK) channels in keratinocytes mediates peripheral kappa opioid receptor-mediated antinociception. [PDF]
NeuropharmacologyPando MM +6 more
europepmc +1 more source
The Relevance of GIRK Channels in Heart Function
Membranes, 2022 Among the large number of potassium-channel families implicated in the control of neuronal excitability, G-protein-gated inwardly rectifying potassium channels (GIRK/Kir3) have been found to be a main factor in heart control. These channels are activated following the modulation of G-protein-coupled receptors and, although they have been implicated in ...
J Antonio Lamas, Campos-Ríos A
exaly +5 more sources
Discovery of ‘molecular switches’ within a GIRK activator scaffold that afford selective GIRK inhibitors [PDF]
Bioorganic and Medicinal Chemistry Letters, 2013 This letter describes a multi-dimensional SAR campaign based on a potent, efficacious and selective GIRK1/2 activator (~10-fold versus GIRK1/4 and inactive on nonGIRK 1-containing GIRKs, GIRK 2 or GIRK2/3). Further chemical optimization through an iterative parallel synthesis effort identified multiple 'molecular switches' that modulated the mode of ...
Gary Sulikowski +2 more
exaly +3 more sources
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Structural characterization of the mouse Girk genes
Gene, 2002Cardiac and neuronal G protein-gated potassium (K(G)) channels are activated by neurotransmitters such as acetylcholine, opioids, and dopamine. K(G) channel activation leads to an inhibition of synaptic transmission. K(G) channels are tetrameric complexes formed by assembly of G protein-gated, inwardly-rectifying potassium (K(+)) channel (GIRK ...
Kevin, Wickman +2 more
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Co‐activation of GPCRs facilitate GIRK‐dependent current
The Journal of Physiology, 2022AbstractThe activity of dopamine neurons is dependent on both intrinsic properties and afferent projections. One potent form of inhibition is mediated by the activation of two inhibitory G protein‐coupled receptors, D2 and GABAB receptors. Each of these receptors activates G protein‐coupled inwardly rectifying potassium (GIRK) channels.
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