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G protein-coupled receptors (GPCRs) are integral membrane proteins forming the fourth largest superfamily in the human genome. Many of these receptors play key physiological roles and several pathologies have been associated with receptor functional abnormalities. GPCRs therefore represent important goals for drug design in pharmaceutical companies since they constitute the target of about one third of the drugs currently on the market. However, endogenous GPCRs are most often difficult to study because of a lack of tools to target them specifically and single out their response to physiological or drug-elicited stimulations. Hence, studies mostly focused on recombinant receptors expressed in a variety of cellular models that do not always closely reflect the receptor natural environment and often deal with levels of expression exceeding by far physiological ranges. Recent technological developments combining for example genetically modified animals and advanced imaging approaches have improved our ability to visualize endogenous GPCRs. To date, trailing receptor activation, subsequent intracellular redistribution, changes in signaling cascade up to integrated response to a drug-elicited stimulation is at hand though the impact of a physiological challenge on receptor dynamics remains a major issue. Data however suggest that the receptor may embrace a different fate depending on the type of stimulation in particular if sustained or repeated. This suggests that current drugs may only partially mimic the genuine response of the receptor and may explain, at least in part, their secondary effects. Commonalities and specificities between physiological and drug-induced activation can thus represent valuable guidelines for the design of future drugs.

opioid receptors --- G protein coupled receptors --- CGamP mice --- FLIM --- fluorescent knock-in mice --- receptor heteromerization --- Endogenous receptors --- cannabinoid receptors --- biased signaling --- Opiate tolerance

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The human genome encompasses ≈ 860 G protein-coupled receptors (GPCRs) including 374 non-chemosensory GPCRs. Half of these latter GPCRs recognize (neuro)peptides as natural ligands. GPCRs thus play a pivotal role in neuroendocrine communication. In particular, GPCRs are involved in the neuroendocrine control of feeding behavior, reproduction, growth, hydromineral homeostasis and stress response. GPCRs are also major drug targets and hence possess a strong potential for the development of innovative pharmaceuticals. The aim of this Research Topic is to assemble a series of review articles and original research papers on neuropeptide GPCRs and their ligands that will illustrate the different facets of the studies currently conducted in this domain.

Neuroendocrinology. --- Neuropharmacology. --- Endocrinology. --- Transduction pathways --- G protein-coupled receptors --- Neuroendocrinology --- Heptahelical receptors --- Neuropeptides --- Signaling mechanisms --- Biologically active peptides --- seven-transmembrane domain receptors

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Since Erspamer and Boretti, 1951 first described the biogenic amine octopamine in the octopus salivary gland as a molecule with “adrenaline-like” action, decades of extensive studies demonstrated the important role octopamine and its precursor tyramine play in invertebrate physiology and behavior. This book contains the latest original research papers on tyramine/octopamine and their receptors in different neuronal and non-neuronal circuits of insects.

octopamine --- Apis mellifera --- olfactory learning and memory --- serotonin --- G-protein coupled receptors (GPCR) --- type I and II synaptic boutons --- Drosophila --- neural circuits --- tyramine --- dopamine

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G proteins --- Receptors. --- G proteins. --- Receptors, G-Protein-Coupled. --- G-Protein-Coupled Receptors --- G Protein Coupled Receptors --- Receptors, G Protein Coupled --- GTP-binding proteins --- GTP regulatory proteins --- Guanine nucleotide-binding proteins --- Guanine nucleotide regulatory proteins --- Membrane proteins --- G Protein Coupled Receptor --- G-Protein-Coupled Receptor --- Receptor, G-Protein-Coupled

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G protein-coupled receptors (GPCRs) are integral membrane proteins forming the fourth largest superfamily in the human genome. Many of these receptors play key physiological roles and several pathologies have been associated with receptor functional abnormalities. GPCRs therefore represent important goals for drug design in pharmaceutical companies since they constitute the target of about one third of the drugs currently on the market. However, endogenous GPCRs are most often difficult to study because of a lack of tools to target them specifically and single out their response to physiological or drug-elicited stimulations. Hence, studies mostly focused on recombinant receptors expressed in a variety of cellular models that do not always closely reflect the receptor natural environment and often deal with levels of expression exceeding by far physiological ranges. Recent technological developments combining for example genetically modified animals and advanced imaging approaches have improved our ability to visualize endogenous GPCRs. To date, trailing receptor activation, subsequent intracellular redistribution, changes in signaling cascade up to integrated response to a drug-elicited stimulation is at hand though the impact of a physiological challenge on receptor dynamics remains a major issue. Data however suggest that the receptor may embrace a different fate depending on the type of stimulation in particular if sustained or repeated. This suggests that current drugs may only partially mimic the genuine response of the receptor and may explain, at least in part, their secondary effects. Commonalities and specificities between physiological and drug-induced activation can thus represent valuable guidelines for the design of future drugs.

opioid receptors --- G protein coupled receptors --- CGamP mice --- FLIM --- fluorescent knock-in mice --- receptor heteromerization --- Endogenous receptors --- cannabinoid receptors --- biased signaling --- Opiate tolerance --- opioid receptors --- G protein coupled receptors --- CGamP mice --- FLIM --- fluorescent knock-in mice --- receptor heteromerization --- Endogenous receptors --- cannabinoid receptors --- biased signaling --- Opiate tolerance