G protein-coupled receptors (GPCRs) have proven to be the most highly favorable class of drug targets in modern pharmacology. Over 90% of nonsensory GPCRs are expressed in the brain, where they play important roles in numerous neuronal functions. GPCRs can be desensitized following activation by agonists by becoming phosphorylated by members of the family of G protein-coupled receptor kinases (GRKs). Phosphorylated receptors are then bound by arrestins, which prevent further stimulation of G proteins and downstream signaling pathways. Discussed in this review are recent progress in understanding basics of GPCR desensitization, novel functional roles, patterns of brain expression, and receptor specificity of GRKs and beta arrestins in major brain functions. In particular, screening of genetically modified mice lacking individual GRKs or beta arrestins for alterations in behavioral and biochemical responses to cocaine and morphine has revealed a functional specificity in dopamine and mu-opioid receptor regulation of locomotion and analgesia. An important and specific role of GRKs and beta arrestins in regulating physiological responsiveness to psychostimulants and morphine suggests potential involvement of these molecules in cert...Continue Reading
Apomorphine-induced stereotypic cage climbing in mice as a model for studying changes in dopamine receptor sensitivity
Increased extracellular serotonin in rat brain after systemic or intraraphe administration of morphine
Chronic morphine administration increases beta-adrenergic receptor kinase (beta ARK) levels in the rat locus coeruleus
Beta-arrestin and arrestin are recognized by autoantibodies in sera from multiple sclerosis patients
Characterization of the G protein-coupled receptor kinase GRK4. Identification of four splice variants.
Differential regulation of dopamine D1A receptor responsiveness by various G protein-coupled receptor kinases.
Members of the G protein-coupled receptor kinase family that phosphorylate the beta2-adrenergic receptor facilitate sequestration
G protein-coupled receptor kinase mediates desensitization of norepinephrine-induced Ca2+ channel inhibition
Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice
Differential desensitization of mu- and delta- opioid receptors in selected neural pathways following chronic morphine treatment
Loss of morphine-induced analgesia, reward effect and withdrawal symptoms in mice lacking the mu-opioid-receptor gene
Regulation of G protein-coupled receptor kinases by calmodulin and localization of the calmodulin binding domain.
G protein-coupled receptor kinase 3 (GRK3) gene disruption leads to loss of odorant receptor desensitization.
Molecular cloning of rat G-protein-coupled receptor kinase 6 (GRK6) from brain tissue, and its mRNA expression in different brain regions and peripheral tissues
beta-Arrestin1 knockout mice appear normal but demonstrate altered cardiac responses to beta-adrenergic stimulation
Regulation of G protein-coupled receptor kinase 2 in brains of opiate-treated rats and human opiate addicts
The G protein-coupled receptor kinase 2 is a microtubule-associated protein kinase that phosphorylates tubulin.
Role for G protein-coupled receptor kinase in agonist-specific regulation of mu-opioid receptor responsiveness
Control of myocardial contractile function by the level of beta-adrenergic receptor kinase 1 in gene-targeted mice.
G protein-coupled receptors. III. New roles for receptor kinases and beta-arrestins in receptor signaling and desensitization.
Selective interference of beta-arrestin 1 with kappa and delta but not mu opioid receptor/G protein coupling.
Sequestration of dopamine D2 receptors depends on coexpression of G-protein-coupled receptor kinases 2 or 5
The beta2-adrenergic receptor/betaarrestin complex recruits the clathrin adaptor AP-2 during endocytosis
The mu opiate receptor as a candidate gene for pain: polymorphisms, variations in expression, nociception, and opiate responses
Functional dissociation of mu opioid receptor signaling and endocytosis: implications for the biology of opiate tolerance and addiction
The GRK4 subfamily of G protein-coupled receptor kinases. Alternative splicing, gene organization, and sequence conservation.
Muscarinic supersensitivity and impaired receptor desensitization in G protein-coupled receptor kinase 5-deficient mice
Differential affinities of visual arrestin, beta arrestin1, and beta arrestin2 for G protein-coupled receptors delineate two major classes of receptors
Expression patterns of the regulatory proteins G protein-coupled receptor kinase 2 and beta-arrestin 1 during rat postnatal brain development: effect of hypothyroidism
Threonine 180 is required for G-protein-coupled receptor kinase 3- and beta-arrestin 2-mediated desensitization of the mu-opioid receptor in Xenopus oocytes
The G-protein-coupled receptor kinase GRK4 mediates homologous desensitization of metabotropic glutamate receptor 1
Mu-opioid receptor desensitization by beta-arrestin-2 determines morphine tolerance but not dependence
The role of phosphorylation/dephosphorylation in agonist-induced desensitization of D1 dopamine receptor function: evidence for a novel pathway for receptor dephosphorylation
G protein-coupled receptor kinase 2 mediates mu-opioid receptor desensitization in GABAergic neurons of the nucleus raphe magnus
Changes in the expression of G protein-coupled receptor kinases and beta-arrestin 2 in rat brain during opioid tolerance and supersensitivity
Differential regulation of the dopamine D2 and D3 receptors by G protein-coupled receptor kinases and beta-arrestins
Distribution of G-protein-coupled receptor kinase (GRK) isoforms 2, 3, 5 and 6 mRNA in the rat brain
Desensitization of endogenously expressed delta-opioid receptors: no evidence for involvement of G protein-coupled receptor kinase 2
Distinct residues in the carboxyl tail mediate agonist-induced desensitization and internalization of the human dopamine D1 receptor
mu-Opioid receptors desensitize less rapidly than delta-opioid receptors due to less efficient activation of arrestin
Endocytosis of G protein-coupled receptors: roles of G protein-coupled receptor kinases and beta-arrestin proteins
Regulation of mu-opioid receptors, G-protein-coupled receptor kinases and beta-arrestin 2 in the rat brain after chronic opioid receptor antagonism
Knockdown of spinal opioid receptors by antisense targeting beta-arrestin reduces morphine tolerance and allodynia in rat
Acute and chronic morphine treatments and morphine withdrawal differentially regulate GRK2 and GRK5 gene expression in rat brain
Up-regulation of neuronal calcium sensor-1 (NCS-1) in the prefrontal cortex of schizophrenic and bipolar patients
Role of G protein-coupled receptor kinase 4 and beta-arrestin 1 in agonist-stimulated metabotropic glutamate receptor 1 internalization and activation of mitogen-activated protein kinases
Acute treatment with the cyclic antidepressant desipramine, but not fluoxetine, increases membrane-associated G protein-coupled receptor kinases 2/3 in rat brain
Differential regulation of beta-arrestin 1 and beta-arrestin 2 gene expression in rat brain by morphine
Regulation of GRK 2 and 6, beta-arrestin-2 and associated proteins in the prefrontal cortex of drug-free and antidepressant drug-treated subjects with major depression
Evidence that a single nucleotide polymorphism in the promoter of the G protein receptor kinase 3 gene is associated with bipolar disorder
Involvement of beta-arrestin-2 in modulation of the spinal antinociception induced by mu-opioid receptor agonists in the mouse
Multifaceted roles of beta-arrestins in the regulation of seven-membrane-spanning receptor trafficking and signalling
G protein-coupled receptor kinase 5 regulates airway responses induced by muscarinic receptor activation
Increased acute inflammation, leukotriene B4-induced chemotaxis, and signaling in mice deficient for G protein-coupled receptor kinase 6
GRK6 deficiency is associated with enhanced CXCR4-mediated neutrophil chemotaxis in vitro and impaired responsiveness to G-CSF in vivo
A new role for monoamine oxidases in the modulation of macrophage-inducible nitric oxide synthase gene expression
Effects of receptor density on Nociceptin/OrphaninFQ peptide receptor desensitisation: studies using the ecdysone inducible expression system
A door opener for future research: agonist-induced β3-adrenoceptor desensitization in HEK cells but not CHO cells
Gβ5-RGS complexes are gatekeepers of hyperactivity involved in control of multiple neurotransmitter systems
Identifying susceptibility loci for nicotine dependence: 2008 update based on recent genome-wide linkage analyses
The 7-transmembrane protein homologue UL78 of the human cytomegalovirus forms oligomers and traffics between the plasma membrane and different intracellular compartments
The fine-structural distribution of G-protein receptor kinase 3, beta-arrestin-2, Ca2+/calmodulin-dependent protein kinase II and phosphodiesterase PDE1C2, and a Cl(-)-cotransporter in rodent olfactory epithelia
Parkinson disease drug screening based on the interaction between D(2) dopamine receptor and beta-arrestin 2 detected by capillary zone electrophoresis
A selective membrane estrogen receptor agonist maintains autonomic functions in hypoestrogenic states
Endogenous Gs-coupled receptors in smooth muscle exhibit differential susceptibility to GRK2/3-mediated desensitization
Rediocide A, an Insecticide, induces G-protein-coupled receptor desensitization via activation of conventional protein kinase C
Repeated cocaine administration decreases 5-HT(2A) receptor-mediated serotonergic enhancement of synaptic activity in rat medial prefrontal cortex
R7BP complexes with RGS9-2 and RGS7 in the striatum differentially control motor learning and locomotor responses to cocaine
A dopamine D1 receptor-dependent β-arrestin signaling complex potentially regulates morphine-induced psychomotor activation but not reward in mice
α-1 Adrenergic receptors are localized on presynaptic elements in the nucleus accumbens and regulate mesolimbic dopamine transmission
Tolerance to repeated morphine administration is associated with increased potency of opioid agonists
beta-Arrestin2, interacting with phosphodiesterase 4, regulates synaptic release probability and presynaptic inhibition by opioids
Dimerization of the thyrotropin-releasing hormone receptor potentiates hormone-dependent receptor phosphorylation
The orphan G protein-coupled receptor, Gpr161, encodes the vacuolated lens locus and controls neurulation and lens development
Agonist-directed signaling of the serotonin 2A receptor depends on beta-arrestin-2 interactions in vivo
G protein-coupled receptor kinase-2 constitutively regulates D2 dopamine receptor expression and signaling independently of receptor phosphorylation
Site-specific phosphorylation of CXCR4 is dynamically regulated by multiple kinases and results in differential modulation of CXCR4 signaling
CK2 phosphorylation of an acidic Ser/Thr di-isoleucine motif in the Na+/H+ exchanger NHE5 isoform promotes association with beta-arrestin2 and endocytosis.
Gi/o signaling and the palmitoyltransferase DHHC2 regulate palmitate cycling and shuttling of RGS7 family-binding protein.
Large putative PEST-like sequence motif at the carboxyl tail of human calcium receptor directs lysosomal degradation and regulates cell surface receptor level.
Involvement of nuclear factor κB (NF-κB) signaling pathway in regulation of cardiac G protein-coupled receptor kinase 5 (GRK5) expression.
Epitope-tagged receptor knock-in mice reveal that differential desensitization of alpha2-adrenergic responses is because of ligand-selective internalization
G protein-coupled receptor kinase-mediated phosphorylation regulates post-endocytic trafficking of the D2 dopamine receptor
Emerging concepts of guanine nucleotide-binding protein-coupled receptor (GPCR) function and implications for high throughput screening
Calcium dysregulation and homeostasis of neural calcium in the molecular mechanisms of neurodegenerative diseases provide multiple targets for neuroprotection
Binding of amyloid beta peptide to beta2 adrenergic receptor induces PKA-dependent AMPA receptor hyperactivity
Association study of the β-arrestin 2 gene (ARRB2) with opioid and cocaine dependence in a European-American population
Desensitization of GSTF8 induction by a prior chemical treatment is long lasting and operates in a tissue-dependent manner
Glutamate receptor subtypes evidenced by differences in desensitization and dependence on the GLR3.3 and GLR3.4 genes
Possible involvement of prolonging spinal µ-opioid receptor desensitization in the development of antihyperalgesic tolerance to µ-opioids under a neuropathic pain-like state
Haloperidol and clozapine differentially affect the expression of arrestins, receptor kinases, and extracellular signal-regulated kinase activation
Identification of RanBP 9/10 as interacting partners for protein kinase C (PKC) gamma/delta and the D1 dopamine receptor: regulation of PKC-mediated receptor phosphorylation
Enhanced hypotensive, bradycardic, and hypnotic responses to alpha2-adrenergic agonists in spinophilin-null mice are accompanied by increased G protein coupling to the alpha2A-adrenergic receptor
Desensitization and trafficking of μ-opioid receptors in locus ceruleus neurons: modulation by kinases
Agonist-driven maturation and plasma membrane insertion of calcium-sensing receptors dynamically control signal amplitude
The complex of G protein regulator RGS9-2 and Gβ(5) controls sensitization and signaling kinetics of type 5 adenylyl cyclase in the striatum
The carboxy-terminal tail of human cytomegalovirus (HCMV) US28 regulates both chemokine-independent and chemokine-dependent signaling in HCMV-infected cells
Suppression of G-protein-coupled receptor kinase 3 expression is a feature of classical GBM that is required for maximal growth
Interaction of the mu-opioid receptor with GPR177 (Wntless) inhibits Wnt secretion: potential implications for opioid dependence.
Growth factor receptor-Src-mediated suppression of GRK6 dysregulates CXCR4 signaling and promotes medulloblastoma migration.
Group I mGluR antagonist rescues the deficit of D1-induced LTP in a mouse model of fragile X syndrome
Receptor downregulation and desensitization enhance the information processing ability of signalling receptors
β-amyloid42 induces desensitization of CXC chemokine receptor-4 via formyl peptide receptor in neural stem/progenitor cells
The rates of protein synthesis and degradation account for the differential response of neurons to spaced and massed training protocols
The recently identified P2Y-like receptor GPR17 is a sensor of brain damage and a new target for brain repair
A high throughput screen identifies Nefopam as targeting cell proliferation in β-catenin driven neoplastic and reactive fibroproliferative disorders
Effects of the dopamine D2 allosteric modulator, PAOPA, on the expression of GRK2, arrestin-3, ERK1/2, and on receptor internalization
The stem cell-expressed receptor Lgr5 possesses canonical and functionally active molecular determinants critical to β-arrestin-2 recruitment
Acute morphine treatments alleviate tremor in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated monkeys
Subcellular sorting of the G-protein coupled mouse somatostatin receptor 5 by a network of PDZ-domain containing proteins
Kaposi's sarcoma-associated herpesvirus K7 induces viral G protein-coupled receptor degradation and reduces its tumorigenicity
A role for Akt and glycogen synthase kinase-3 as integrators of dopamine and serotonin neurotransmission in mental health
Elimination of GRK2 from cholinergic neurons reduces behavioral sensitivity to muscarinic receptor activation
Recovery from mu-opioid receptor desensitization after chronic treatment with morphine and methadone
Differential binding of calmodulin to group I metabotropic glutamate receptors regulates receptor trafficking and signaling
Rapid delivery of internalized signaling receptors to the somatodendritic surface by sequence-specific local insertion
Association of genetic variation in pharmacodynamic factors with methadone dose required for effective treatment of opioid addiction
Smoking but not cocaine use is associated with lower cerebral metabotropic glutamate receptor 5 density in humans
Subcellular and subsynaptic localization of group I metabotropic glutamate receptors in the nucleus accumbens of cocaine-treated rats
Behavioral and cellular pharmacology characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) as a mu opioid receptor selective ligand
PKA and ERK1/2 are involved in dopamine D₁ receptor-induced heterologous desensitization of the δ opioid receptor
Disruption of dopamine D1 receptor phosphorylation at serine 421 attenuates cocaine-induced behaviors in mice
An opioid agonist that does not induce mu-opioid receptor--arrestin interactions or receptor internalization
Cellular mechanisms of nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor regulation and heterologous regulation by N/OFQ
Constitutive internalization of the leucine-rich G protein-coupled receptor-5 (LGR5) to the trans-Golgi network.
Neuromodulation of fast-spiking and non-fast-spiking hippocampal CA1 interneurons by human cerebrospinal fluid
Palmitoylation regulates plasma membrane-nuclear shuttling of R7BP, a novel membrane anchor for the RGS7 family
Beta-Arrestin1 Levels in Mononuclear Leukocytes Support Depression Scores for Women with Premenstrual Dysphoric Disorder.
Endothelin-converting enzyme-1 regulates trafficking and signalling of the neurokinin 1 receptor in endosomes of myenteric neurones
Central HIV-1 Tat exposure elevates anxiety and fear conditioned responses of male mice concurrent with altered mu-opioid receptor-mediated G-protein activation and β-arrestin 2 activity in the forebrain
Target-cell-dependent plasticity within the mossy fibre-CA3 circuit reveals compartmentalized regulation of presynaptic function at divergent release sites
Correlation between endogenous polyamines in human cardiac tissues and clinical parameters in patients with heart failure
Stable G protein-effector complexes in striatal neurons: mechanism of assembly and role in neurotransmitter signaling
Membrane-initiated actions of estradiol that regulate reproduction, energy balance and body temperature
An animal model of female adolescent cannabinoid exposure elicits a long-lasting deficit in presynaptic long-term plasticity.
β-arrestin2 regulates cannabinoid CB1 receptor signaling and adaptation in a central nervous system region-dependent manner
C-terminal peptides of chemokine-like factor 1 signal through chemokine receptor CCR4 to cross-desensitize the CXCR4
Molecular actions and therapeutic potential of lithium in preclinical and clinical studies of CNS disorders
Subcellular plasticity of the corticotropin-releasing factor receptor in dendrites of the mouse bed nucleus of the stria terminalis following chronic opiate exposure
Development of tolerance in D3 dopamine receptor signaling is accompanied by distinct changes in receptor conformation
Identification of brain target neurons using a fluorescent conjugate of corticotropin-releasing factor
Constitutive, agonist-accelerated, recycling and lysosomal degradation of GABA(B) receptors in cortical neurons
Protein kinase C is a common component of CGRP receptor desensitization induced by distinct agonists
Postnatal induction and localization of R7BP, a membrane-anchoring protein for regulator of G protein signaling 7 family-Gbeta5 complexes in brain
Decreased substance P and NK1 receptor immunoreactivity and function in the spinal cord dorsal horn of morphine-treated neonatal rats
The absence of endogenous beta-endorphin selectively blocks phosphorylation and desensitization of mu opioid receptors following partial sciatic nerve ligation
Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from beta-cells through activation of GPR40
Minocycline provides protection against beta-amyloid(25-35)-induced alterations of the somatostatin signaling pathway in the rat temporal cortex
Monitoring of phosphorylated peptides by radioactive assay and matrix-assisted laser desorption-ionization time-of-flight mass spectrometry
Dynorphin activation of kappa opioid receptor reduces neuronal excitability in the paraventricular nucleus of mouse thalamus
Desensitization of endothelial P2Y1 receptors by PKC-dependent mechanisms in pressurized rat small mesenteric arteries
Nicotine sensitization and analysis of brain-derived neurotrophic factor in adolescent beta-arrestin-2 knockout mice
Opposing effects of phorbol-12-myristate-13-acetate, an activator of protein kinase C, on the signaling of structurally related human dopamine D1 and D5 receptors
Activated somatostatin type 2 receptors traffic in vivo in central neurons from dendrites to the trans Golgi before recycling
Regulation of CB1 cannabinoid receptor internalization by a promiscuous phosphorylation-dependent mechanism
Internalization of D2 dopamine receptors is clathrin-dependent and select to dendro-axonic appositions in primate prefrontal cortex
The regulation of M1 muscarinic acetylcholine receptor desensitization by synaptic activity in cultured hippocampal neurons
Repeated cocaine exposure decreases dopamine D₂-like receptor modulation of Ca(2+) homeostasis in rat nucleus accumbens neurons
GABA(B) receptors do not internalize after baclofen treatment, possibly due to a lack of β-arrestin association: study with a real-time visualizing assay
Ligand-induced μ opioid receptor internalization in enteric neurons following chronic treatment with the opiate fentanyl
Nesfatin-1 activates cardiac vagal neurons of nucleus ambiguus and elicits bradycardia in conscious rats
The CB1 cannabinoid receptor C-terminus regulates receptor desensitization in autaptic hippocampal neurones
Possible involvement of β-endorphin in a loss of the coordinated balance of μ-opioid receptors trafficking processes by fentanyl
Potential factors influencing the development of thrombocytopenia and consumptive coagulopathy after genetically modified pig liver xenotransplantation
Arabidopsis transcriptional response to extracellular Ca2+ depletion involves a transient rise in cytosolic Ca2+
Repeated administration of angiotensin II reduces its dipsogenic effect without affecting saline intake
Regulatory mechanisms underlying pheromone biosynthesis activating neuropeptide (PBAN)-induced internalization of the Bombyx mori PBAN receptor
Mu opioid signaling protects against acute murine intestinal injury in a manner involving Stat3 signaling
Association between common genetic variants in the opioid pathway and smoking behaviors in Chinese men
Socially isolated mice exhibit a blunted homeostatic sleep response to acute sleep deprivation compared to socially paired mice
Norepinephrine acts as D1-dopaminergic agonist in the embryonic avian retina: late expression of beta1-adrenergic receptor shifts norepinephrine specificity in the adult tissue
Multi-target strategies for the improved treatment of depressive states: Conceptual foundations and neuronal substrates, drug discovery and therapeutic application
The involvement of G proteins and regulators of receptor-G protein coupling in the pathophysiology, diagnosis and treatment of mood disorders
Delta(9)-Tetrahydrocannabinol-induced desensitization of cannabinoid-mediated inhibition of synaptic transmission between hippocampal neurons in culture.
Dynamics of beta-arrestin1 protein and mRNA levels elevation by antidepressants in mononuclear leukocytes of patients with depression
Expression, stabilization and purification of membrane proteins via diverse protein synthesis systems and detergents involving cell-free associated with self-assembly peptide surfactants
Dexamethasone enhances the norepinephrine-induced ERK/MAPK intracellular pathway possibly via dysregulation of the alpha2-adrenergic receptor: implications for antidepressant drug mechanism of action
Genetic variation in G-protein-coupled receptors--consequences for G-protein-coupled receptors as drug targets
The effects of beta-arrestin1 deletion on acute cannabinoid activity, brain cannabinoid receptors and tolerance to cannabinoids in mice
Sorting nexin 27 regulation of G protein-gated inwardly rectifying K⁺ channels attenuates in vivo cocaine response
Receptor activation involving positive allosteric modulation, unlike full agonism, does not result in GABAB receptor desensitization
Modulation of basal and receptor-induced GIRK potassium channel activity and neuronal excitability by the mammalian PINS homolog LGN
Neurogenesis-dependent and -independent effects of fluoxetine in an animal model of anxiety/depression
The tolerance property of human D3 dopamine receptor is determined by specific amino acid residues in the second cytoplasmic loop
G protein-coupled receptors in the hypothalamic paraventricular and supraoptic nuclei--serpentine gateways to neuroendocrine homeostasis
Perturbation of tyraminergic/octopaminergic function inhibits oviposition in the cattle tick Rhipicephalus (Boophilus) microplus
Rapid CB1 cannabinoid receptor desensitization defines the time course of ERK1/2 MAP kinase signaling
SKF-83959 is not a highly-biased functionally selective D1 dopamine receptor ligand with activity at phospholipase C
Neuropeptides as neuroprotective agents: Oxytocin a forefront developmental player in the mammalian brain
Functional consequences of perturbed CXCL12 signal processing: analyses of immature hematopoiesis in GRK6-deficient mice
Deletion of SHATI/NAT8L increases dopamine D1 receptor on the cell surface in the nucleus accumbens, accelerating methamphetamine dependence
Possible involvement of post-dopamine D2 receptor signalling components in the pathophysiology of schizophrenia
Antidepressants elevate GDNF expression and release from C₆ glioma cells in a β-arrestin1-dependent, CREB interactive pathway
The Identification of Novel Protein-Protein Interactions in Liver that Affect Glucagon Receptor Activity
Heterologous, PKC-Mediated Desensitization of Human Histamine H3 Receptors Expressed in CHO-K1 Cells
Serotonin-reuptake inhibitors act centrally to cause bone loss in mice by counteracting a local anti-resorptive effect
Distinct G protein-coupled receptor recycling pathways allow spatial control of downstream G protein signaling
Role of amino acid residues surrounding the phosphorylation site in peptide substrates of G protein-coupled receptor kinase 2 (GRK2)
Pancreatic Beta Cell G-Protein Coupled Receptors and Second Messenger Interactions: A Systems Biology Computational Analysis
G protein-coupled receptor kinase 2 (GRK2) as an integrative signalling node in the regulation of cardiovascular function and metabolic homeostasis
Heterologous desensitization of cardiac β-adrenergic signal via hormone-induced βAR/arrestin/PDE4 complexes
Purification and identification of G protein-coupled receptor protein complexes under native conditions.
Inhibiting clathrin-mediated endocytosis of the leucine-rich G protein-coupled receptor-5 diminishes cell fitness.
Reciprocal regulation of ARPP-16 by PKA and MAST3 kinases provides a cAMP-regulated switch in protein phosphatase 2A inhibition
Functional N-Formyl Peptide Receptor 2 (FPR2) Antagonists Based on the Ureidopropanamide Scaffold Have Potential To Protect Against Inflammation-Associated Oxidative Stress
Proteolytic degradation of regulator of G protein signaling 2 facilitates temporal regulation of Gq/11 signaling and vascular contraction
Usefulness for the combination of G-protein- and β-arrestin-biased ligands of μ-opioid receptors: Prevention of antinociceptive tolerance
Role of G protein-regulated inducer of neurite outgrowth 3 (GRIN3) in β-arrestin 2-Akt signaling and dopaminergic behaviors
Impact of SNP-SNP interaction among ABCB1, ARRB2, DRD1 and OPRD1 on methadone dosage requirement in Han Chinese patients
Protein kinase D1-dependent phosphorylation of dopamine D1 receptor regulates cocaine-induced behavioral responses
Expression and light-dependent translocation of β-arrestin in the visual system of the terrestrial slug Limax valentianus
Protein kinase C mediates phosphorylation, desensitization, and trafficking of the D2 dopamine receptor
Characterization of EGF-guided MDA-MB-231 cell chemotaxis in vitro using a physiological and highly sensitive assay system
Specific α-arrestins negatively regulate Saccharomyces cerevisiae pheromone response by down-modulating the G-protein-coupled receptor Ste2
β-arrestin-2 regulates NMDA receptor function in spinal lamina II neurons and duration of persistent pain
Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging
Differential regulation of GABAB receptor trafficking by different modes of N-methyl-D-aspartate (NMDA) receptor signaling.
Desensitization of GABA(B) receptor signaling by formation of protein complexes of GABA(B2) subunit with GRK4 or GRK5
Comparative analysis of the subcellular and subsynaptic localization of mGluR1a and mGluR5 metabotropic glutamate receptors in the shell and core of the nucleus accumbens in rat and monkey
A comparison of noninternalizing (herkinorin) and internalizing (DAMGO) mu-opioid agonists on cellular markers related to opioid tolerance and dependence
G protein-coupled receptor kinase regulates dopamine D3 receptor signaling by modulating the stability of a receptor-filamin-beta-arrestin complex. A case of autoreceptor regulation
Prolonged G(q) activity triggers fly rhodopsin endocytosis and degradation, and reduces photoreceptor sensitivity
Inhibition of signal termination-related kinases by membrane-permeant bitter and sweet tastants: potential role in taste signal termination
Eckol as a Potential Therapeutic against Neurodegenerative Diseases Targeting Dopamine D₃/D₄ Receptors
Synergistic actions of diacylglycerol and inositol 1,4,5 trisphosphate for Ca2+-dependent inactivation of TRPC7 channel
Overexpression of the Drosophila vesicular monoamine transporter increases motor activity and courtship but decreases the behavioral response to cocaine
The role of opioid receptor internalization and beta-arrestins in the development of opioid tolerance
The short neuropeptide F-like receptor from the red imported fire ant, Solenopsis invicta Buren (Hymenoptera: Formicidae)
Minireview: the intimate link between calcium sensing receptor trafficking and signaling: implications for disorders of calcium homeostasis
Subcellular targeting of RGS9-2 is controlled by multiple molecular determinants on its membrane anchor, R7BP
Role of beta-adrenergic receptor signaling and desensitization in heart failure: new concepts and prospects for treatment
Cross-regulation of VPAC(2) receptor desensitization by M(3) receptors via PKC-mediated phosphorylation of RKIP and inhibition of GRK2
The elevated blood pressure of human GRK4gamma A142V transgenic mice is not associated with increased ROS production
Insulin causes renal dopamine D1 receptor desensitization via GRK2-mediated receptor phosphorylation involving phosphatidylinositol 3-kinase and protein kinase C
Adrenergic ligands that block oviposition in the cattle tick Rhipicephalus microplus affect ovary contraction
Altered expression and subcellular distribution of GRK subtypes in the dopamine-depleted rat basal ganglia is not normalized by l-DOPA treatment
Muscarinic acetylcholine receptor M3 modulates odorant receptor activity via inhibition of β-arrestin-2 recruitment
Quantitative trait loci affecting phenotypic variation in the vacuolated lens mouse mutant, a multigenic mouse model of neural tube defects
Negative reciprocity between angiotensin II type 1 and dopamine D1 receptors in rat renal proximal tubule cells
Age-dependent effects of dopamine receptor inactivation on cocaine-induced behaviors in male rats: Evidence of dorsal striatal D2 receptor supersensitivity
The timing and amount of vagus nerve stimulation during rehabilitative training affect poststroke recovery of forelimb strength
Desensitization of the dopamine D1 and D2 receptor hetero-oligomer mediated calcium signal by agonist occupancy of either receptor
Chronic morphine up-regulates G alpha12 and cytoskeletal proteins in Chinese hamster ovary cells expressing the cloned mu opioid receptor
Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2
Heterodimerization of Mu Opioid Receptor Protomer with Dopamine D2 Receptor Modulates Agonist-Induced Internalization of Mu Opioid Receptor
A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal
Hyperinsulinemia promotes heterologous desensitization of β2 adrenergic receptor in airway smooth muscle in obesity.
Cloning and functional characterization of a gamma-hydroxybutyrate receptor identified in the human brain
Glucocorticoids regulate innate immunity in a model of multiple sclerosis: reciprocal interactions between the A1 adenosine receptor and beta-arrestin-1 in monocytoid cells
Shuttling of Peptide-Drug Conjugates by G Protein-Coupled Receptors Is Significantly Improved by Pulsed Application.
Uncoupling and endocytosis of 5-hydroxytryptamine 4 receptors. Distinct molecular events with different GRK2 requirements
Prolonged treatment with ligands affects ligand binding to the human serotonin(1A) receptor in Chinese hamster ovary cells
A novel CCR5-specific pharmacodynamic assay in whole blood using phosphoflow cytometry highlights different ligand-dependent responses but similar properties of antagonists in CD8+ and CD4+ T lymphocytes
Morphine desensitization, internalization, and down-regulation of the mu opioid receptor is facilitated by serotonin 5-hydroxytryptamine2A receptor coactivation
Phosphorylation of rat melanopsin at Ser-381 and Ser-398 by light/dark and its importance for intrinsically photosensitive ganglion cells (ipRGCs) cellular Ca2+ signaling.
A G Protein-biased Designer G Protein-coupled Receptor Useful for Studying the Physiological Relevance of Gq/11-dependent Signaling Pathways.
Cutting-Edge Search for Safer Opioid Pain Relief: Retrospective Review of Salvinorin A and Its Analogs
SCH23390 Reduces Methamphetamine Self-Administration and Prevents Methamphetamine-Induced Striatal LTD.
Gamma-aminobutyric acid type B receptors are constitutively internalized via the clathrin-dependent pathway and targeted to lysosomes for degradation
Structural and biochemical basis for ubiquitin ligase recruitment by arrestin-related domain-containing protein-3 (ARRDC3).
Identification and functional characterization of the phosphorylation sites of the neuropeptide FF2 receptor.
Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties
Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor
Type 2 diabetes-associated variants of the MT2 melatonin receptor affect distinct modes of signaling
Divergent expression patterns of pituitary gonadotropin subunit and GnRH receptor genes to continuous GnRH in vitro and in vivo
Mechanism of assembly of G protein betagamma subunits by protein kinase CK2-phosphorylated phosducin-like protein and the cytosolic chaperonin complex.
Lysophospholipids of different classes mobilize neutrophil secretory vesicles and induce redundant signaling through G2A
Chronic subcutaneous administration of kisspeptin-54 causes testicular degeneration in adult male rats
Dopamine receptor-interacting protein 78 acts as a molecular chaperone for Ggamma subunits before assembly with Gbeta
Allosteric modulation of family C G-protein-coupled receptors: from molecular insights to therapeutic perspectives
High-fat diet induces protein kinase A and G-protein receptor kinase phosphorylation of β2 -adrenergic receptor and impairs cardiac adrenergic reserve in animal hearts
Role of the guanine nucleotide binding protein, Gαo, in the development of morphine tolerance and dependence
Effect of the 5-HT4 receptor agonist tegaserod on the expression of GRK2 and GRK6 in the rat gastrointestinal tract
Unusually persistent Gαi -signaling of the neuropeptide Y2 receptor depletes cellular Gi/o pools and leads to a Gi -refractory state
Regulation of TrkB cell surface expression-a mechanism for modulation of neuronal responsiveness to brain-derived neurotrophic factor
Regulation of nuclear factor κB (NF-κB) in the nucleus of cardiomyocytes by G protein-coupled receptor kinase 5 (GRK5).
Agonist Binding and Desensitization of the μ-Opioid Receptor Is Modulated by Phosphorylation of the C-Terminal Tail Domain
Functional characterization of the cannabinoid receptors 1 and 2 in zebrafish larvae using behavioral analysis
Is there a role for antibodies targeting muscarinic acetylcholine receptors in the pathogenesis of schizophrenia?
A Split Luciferase Complementation Assay for the Quantification of β-Arrestin2 Recruitment to Dopamine D2 -Like Receptors
Negative relationship between brain α1A -AR neurotransmission and βArr2 levels in anxious adolescent rats subjected to early life stress
Spatiotemporal differences in CXCL12 expression and cyclic AMP underlie the unique pattern of optic glioma growth in neurofibromatosis type 1
Bryostatin-5 blocks stromal cell-derived factor-1 induced chemotaxis via desensitization and down-regulation of cell surface CXCR4 receptors
Time-to-treatment window and cross-sex potential of β2-adrenergic receptor-induced mitochondrial biogenesis-mediated recovery after spinal cord injury.
Carvedilol protects against hepatic ischemia/reperfusion injury in high-fructose/high-fat diet-fed mice: Role of G protein-coupled receptor kinase 2 and 5
Differences in invitro responses of the hypothalamo-pituitary-gonadal hormonal axis between low- and high-egg-producing turkey hens.
Prolonged dopamine D3 receptor stimulation promotes dopamine transporter ubiquitination and degradation through a PKC-dependent mechanism.
Profiling of MicroRNA Targets Using Activity-Based Protein Profiling: Linking Enzyme Activity to MicroRNA-185 Function.
A novel molecular mechanism involved in the crosstalks between homologous and PKC-mediated heterologous regulatory pathway of dopamine D2 receptor
Targeting the Autonomic Nervous System for Risk Stratification, Outcome Prediction and Neuromodulation in Ischemic Stroke.
Vagus Nerve Stimulation Rate and Duration Determine whether Sensory Pairing Produces Neural Plasticity
Multi-Electrode Array Analysis Identifies Complex Dopamine Responses and Glucose Sensing Properties of Substantia Nigra Neurons in Mouse Brain Slices.
Biosynthesis and NMR analysis of a 73-residue domain of a Saccharomyces cerevisiae G protein-coupled receptor
A limited range of vagus nerve stimulation intensities produce motor cortex reorganization when delivered during training.
Mu-opioid Receptor (MOR) Biased Agonists Induce Biphasic Dose-dependent Hyperalgesia and Analgesia, and Hyperalgesic Priming in the Rat
Dopaminergic Transmission Rapidly and Persistently Enhances Excitability of D1 Receptor-Expressing Striatal Projection Neurons.
Amygdala: Sensory Processes
Amygdalae, nuclei clusters located in the temporal lobe of the brain, play a role in memory, emotional responses, and decision-making. Here is the latest research on sensory processes in the amygdala.
Here is the latest research on barrel cortex, a region of somatosensory and motor corticies in the brain, which are used by animals that rely on whiskers for world exploration.
Amygdala and Midbrain Dopamine
The midbrain dopamine system is widely studied for its involvement in emotional and motivational behavior. Some of these neurons receive information from the amygdala and project throughout the cortex. When the circuit and transmission of dopamine is disrupted symptoms may present. Here is the latest research on the amygdala and midbrain dopamine.
Adrenergic Receptors: Trafficking
Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.
Calcium & Bioenergetics
Bioenergetic processes, including cellular respiration and photosynthesis, concern the transformation of energy by cells. Here is the latest research on the role of calcium in bioenergetics.
Basal Ganglia are a group of subcortical nuclei in the brain associated with control of voluntary motor movements, procedural and habit learning, emotion, and cognition. Here is the latest research.