No abstract listed.
G-protein-coupled receptor genes as protooncogenes: constitutively activating mutation of the alpha 1B-adrenergic receptor enhances mitogenesis and tumorigenicity
Regions of the alpha 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function
Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins
A constitutively activating mutation of the luteinizing hormone receptor in familial male precocious puberty
Regulation of basal adenylate cyclase activity in neuroblastoma x glioma hybrid, NG108-15, cells transfected to express the human beta 2 adrenoceptor: evidence for empty receptor stimulation of the adenylate cyclase cascade
Somatostatin receptor scintigraphy: its value in tumor localization in patients with Cushing's syndrome caused by ectopic corticotropin or corticotropin-releasing hormone secretion
Quantitative stoichiometry of the proteins of the stimulatory arm of the adenylyl cyclase cascade in neuroblastoma x glioma hybrid, NG108-15 cells
Agonist-independent effects of muscarinic antagonists on Ca2+ and K+ currents in frog and rat cardiac cells
Pharmacological characterisation of [35S]-GTPgammaS binding to Chinese hamster ovary cell membranes stably expressing cloned human 5-HT1D receptor subtypes
Comparison of naltrexone, 6alpha-naltrexol, and 6beta-naltrexol in morphine-dependent and in nondependent rhesus monkeys
Further evidence that naloxone acts as an inverse opiate agonist: implications for drug dependence and withdrawal
Adrenergic mechanisms in the control of gastrointestinal motility: from basic science to clinical applications
The stoichiometry of expression of protein components of the stimulatory adenylyl cyclase cascade and the regulation of information transfer
Involvement of histamine H1 and H2 receptors in the regulation of STAT-1 phosphorylation: inverse agonism exhibited by the receptor antagonists
Inverse agonist properties of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2, 4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide HCl (SR141716A) and 1-(2-chlorophenyl)-4-cyano-5-(4-methoxyphenyl)-1H-pyrazole-3-carboxyl ic acid phenylamide (CP-272871) for the CB(1) cannabinoid receptor
Temperature dependence of the affinity enhancement of selective adenosine A1 receptor agonism: a thermodynamic analysis
Elimination of palmitoylation sites in the human dopamine D1 receptor does not affect receptor-G protein interaction
Phencyclidine and dizocilpine modulate dopamine release from rat nucleus accumbens via sigma receptors
Constitutive activity of the histamine H(1) receptor reveals inverse agonism of histamine H(1) receptor antagonists
Molecular mechanisms involved in the activation and regulation of the alpha 1-adrenergic receptor subtypes
Recent advances in structure, binding sites with ligands and pharmacological function of beta-adrenoceptors obtained by molecular biology and molecular modeling
Basal signaling activity of human dopamine D2L receptor demonstrated with an ecdysone-inducible mammalian expression system
Histamine and histamine-receptor antagonists modify gene expression and biosynthesis of interferon gamma in peripheral human blood mononuclear cells and in CD19-depleted cell subsets
Mechanism of modulation of [3H]raclopride binding to dopaminergic receptors in rat striatal membranes by sodium ions
Neuropeptide Y-mediated enhancement of NMDA-stimulated [3H]dopamine release from rat prefrontal cortex is reversed by sigma1 receptor antagonists
Functional assessment of neuronal cannabinoid receptors in the muscular layers of human ileum and colon.
Involvement of the beta-adrenergic system in the cardiac chronic form of experimental Trypanosoma cruzi infection
Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro
Influence of receptor number on the stimulation by salmeterol of gene transcription in CHO-K1 cells transfected with the human beta2-adrenoceptor
Treatment with inverse agonists enhances baseline atrial contractility in transgenic mice with chronic beta2-adrenoceptor activation
Pharmacological examination of contractile responses of the guinea-pig isolated ileum produced by mu-opioid receptor antagonists in the presence of, and following exposure to, morphine
Partial to complete antagonism by putative antagonists at the wild-type alpha(2C)-adrenoceptor based on kinetic analyses of agonist:antagonist interactions
Detection of receptor ligands by monitoring selective stabilization of a Renilla luciferase-tagged, constitutively active mutant, G-protein-coupled receptor
Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardium
Histamine H3-receptor-mediated [35S]GTP gamma[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors
Activation of constitutive 5-hydroxytryptamine(1B) receptor by a series of mutations in the BBXXB motif: positioning of the third intracellular loop distal junction and its G(o)alpha protein interactions
Activation of muscarinic receptors induces protein synthesis-dependent long-lasting depression in the perirhinal cortex
Inverse agonists and neutral antagonists at mu opioid receptor (MOR): possible role of basal receptor signaling in narcotic dependence
Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors
Mahoganoid and mahogany mutations rectify the obesity of the yellow mouse by effects on endosomal traffic of MC4R protein.
Constitutively active G protein-coupled receptor mutants: implications on receptor function and drug action
Do recent operational studies indicate that a single state model is no longer applicable to G protein-coupled receptors?
The estrogen receptor antagonist ICI 182,780 can act both as an agonist and an inverse agonist when estrogen receptor α AF-2 is modified
Evidence for protean agonism of RX 831003 at alpha 2A-adrenoceptors by co-expression with different G alpha protein subunits
Opioid tolerance/dependence in neuroblastoma x glioma (NG108-15) hybrid cells is associated with a reduction in spontaneous stimulatory receptor activity
Modulation of forskolin-mediated adenylyl cyclase activation by constitutively active G(S)-coupled receptors
Up-regulation of a constitutively active form of the beta2-adrenoceptor by sustained treatment with inverse agonists but not antagonists
Central kappa-opioid receptor-mediated antidepressant-like effects of nor-Binaltorphimine: behavioral and BDNF mRNA expression studies
A peptide from the first fibronectin domain of NCAM acts as an inverse agonist and stimulates FGF receptor activation, neurite outgrowth and survival
Region-dependent regulation of mesoaccumbens dopamine neurons in vivo by the constitutive activity of central serotonin2C receptors
Loss of constitutive activity is correlated with increased thermostability of the human adenosine A2A receptor
Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors
Agonist-dependent and -independent dopamine-1-like receptor signalling differentially regulates downstream effectors
Kinetic and functional properties of [3H]ZM241385, a high affinity antagonist for adenosine A2A receptors
Palatability-dependent appetite and benzodiazepines: new directions from the pharmacology of GABA(A) receptor subtypes
Catecholaminergic activation of G-protein coupling in rat spinal cord: further evidence for the existence of dopamine and noradrenaline receptors in spinal grey and white matter
Effects of different beta adrenoceptor ligands in mice with permanent occlusion of the left anterior descending coronary artery
Interactions of alpha-melanotropin and agouti on B16 melanoma cells: evidence for inverse agonism of agouti
Clemastine causes immune suppression through inhibition of extracellular signal-regulated kinase-dependent proinflammatory cytokines
Antagonists reversibly reverse chemical LTD induced by group I, group II and group III metabotropic glutamate receptors
Getting it together: signal transduction in G-protein coupled receptors by association of receptor domains
Inverse agonist activity of sarpogrelate, a selective 5-HT2A-receptor antagonist, at the constitutively active human 5-HT2A receptor
H1-antihistamines Reduce Progression to Anaphylaxis Among Emergency Department Patients With Allergic Reactions
Clozapine and haloperidol differentially alter the constitutive activity of central serotonin2C receptors in vivo
Constitutively active Gq/11-coupled receptors enable signaling by co-expressed G(i/o)-coupled receptors
Monitoring receptor oligomerization using time-resolved fluorescence resonance energy transfer and bioluminescence resonance energy transfer. The human delta -opioid receptor displays constitutive oligomerization at the cell surface, which is not regulated by receptor occupancy
Functional coupling between adenosine A1 receptors and G-proteins in rat and postmortem human brain membranes determined with conventional guanosine-5'-O-(3-[35 S]thio)triphosphate ([35 S]GTPγS) binding or [35 S]GTPγS/immunoprecipitation assay
Minor modifications of a cholecystokinin-B/gastrin receptor non-peptide antagonist confer a broad spectrum of functional properties.
Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein
Partial agonist activity of bucindolol is dependent on the activation state of the human beta1-adrenergic receptor
Chronic infusion of beta-adrenoceptor antagonist and inverse agonists decreases elevated protein kinase A activity in transgenic mice with cardiac-specific overexpression of human beta 2-adrenoceptor
Regulation of melanocortin-4 receptor signaling: agonist-mediated desensitization and internalization
Does glutamine act as a substrate for transamination reactions in the liver of fed and fasted sheep?
Ligand-independent negative chronotropic responses of rat and mouse right atria to beta-adrenoceptor antagonists
Mutations of Cys-17 and Ala-271 in the human histamine H2 receptor determine the species selectivity of guanidine-type agonists and increase constitutive activity
Enhanced detection of receptor constitutive activity in the presence of regulators of G protein signaling: applications to the detection and analysis of inverse agonists and low-efficacy partial agonists
Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist
Selective stabilization of the high affinity binding conformation of glucagon receptor by the long splice variant of Galpha(s)
Genuine monovalent ligands of TrkA nerve growth factor receptors reveal a novel pharmacological mechanism of action
The conformational change responsible for AT1 receptor activation is dependent upon two juxtaposed asparagine residues on transmembrane helices III and VII.
Delineation of the structural basis for the activation properties of the dopamine D1 receptor subtypes.
Chloroethylclonidine and 2-aminoethyl methanethiosulfonate recognize two different conformations of the human alpha(2A)-adrenergic receptor.
Constitutive activation of the delta opioid receptor by mutations in transmembrane domains III and VII.
A peptide derived from a beta2-adrenergic receptor transmembrane domain inhibits both receptor dimerization and activation.
Alanine exchanges of polar amino acids in the transmembrane domains of a platelet-activating factor receptor generate both constitutively active and inactive mutants.
Allosteric effects of G protein overexpression on the binding of beta-adrenergic ligands with distinct inverse efficacies
Chronic exposure to mu-opioid agonists produces constitutive activation of mu-opioid receptors in direct proportion to the efficacy of the agonist used for pretreatment
Structure/function relationships of calcitonin analogues as agonists, antagonists, or inverse agonists in a constitutively activated receptor cell system
Chlorpropamide upregulates antidiuretic hormone receptors and unmasks constitutive receptor signaling
Ligand function at constitutively active receptor mutants is affected by two distinct yet interacting mechanisms
Histamine H(1)-receptor activation of nuclear factor-kappa B: roles for G beta gamma- and G alpha(q/11)-subunits in constitutive and agonist-mediated signaling
Resolution of inverse agonist-induced up-regulation from constitutive activity of mutants of the alpha(1b)-adrenoceptor
The cannabinoid receptor CB1 modulates the signaling properties of the lysophosphatidylinositol receptor GPR55.
Inverse agonist properties of dopaminergic antagonists at the D(1A) dopamine receptor: uncoupling of the D(1A) dopamine receptor from G(s) protein
Conditioning of beta(1)-adrenoceptor effect via beta(2)-subtype on L-type Ca(2+) current in canine ventricular myocytes
Constitutively active mu-opioid receptors inhibit adenylyl cyclase activity in intact cells and activate G-proteins differently than the agonist [D-Ala2,N-MePhe4,Gly-ol5]enkephalin
The influence of monovalent cations on trimeric G protein G(i)1α activity in HEK293 cells stably expressing DOR-G(i)1α (Cys(351)-Ile(351)) fusion protein
Fluorescent labeling of purified beta 2 adrenergic receptor. Evidence for ligand-specific conformational changes.
Dual expression of constitutively active Gαs-protein-coupled receptors differentially establishes the resting activity of the cAMP-gated HCN2 channel in a single compartment
Lack of effects by sigma ligands on neuropeptide Y-induced G-protein activation in rat hippocampus and cerebellum
Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.
STING Receptor Agonists
Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.
Chronic Fatigue Syndrome
Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.
Hereditary Sensory Autonomic Neuropathy
Hereditary Sensory Autonomic Neuropathies are a group of inherited neurodegenerative disorders characterized clinically by loss of sensation and autonomic dysfunction. Here is the latest research on these neuropathies.
Spatio-Temporal Regulation of DNA Repair
DNA repair is a complex process regulated by several different classes of enzymes, including ligases, endonucleases, and polymerases. This feed focuses on the spatial and temporal regulation that accompanies DNA damage signaling and repair enzymes and processes.
Glut1 deficiency, an autosomal dominant, genetic metabolic disorder associated with a deficiency of GLUT1, the protein that transports glucose across the blood brain barrier, is characterized by mental and motor developmental delays and infantile seizures. Follow the latest research on Glut1 deficiency with this feed.
Separation anxiety is a type of anxiety disorder that involves excessive distress and anxiety with separation. This may include separation from places or people to which they have a strong emotional connection with. It often affects children more than adults. Here is the latest research on separation anxiety.
KIF1A Associated Neurological Disorder
KIF1A associated neurological disorder (KAND) is a rare neurodegenerative condition caused by mutations in the KIF1A gene. KAND may present with a wide range and severity of symptoms including stiff or weak leg muscles, low muscle tone, a lack of muscle coordination and balance, and intellectual disability. Find the latest research on KAND here.
Regulation of Vocal-Motor Plasticity
Dopaminergic projections to the basal ganglia and nucleus accumbens shape the learning and plasticity of motivated behaviors across species including the regulation of vocal-motor plasticity and performance in songbirds. Discover the latest research on the regulation of vocal-motor plasticity here.