Keywords: فعالیت مؤثر; Glutamate; Receptor; Chloride; Constitutive activity; Allostery; GPCR;
مقالات ISI فعالیت مؤثر (ترجمه نشده)
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Keywords: فعالیت مؤثر; Receptor state affinity constants; Constitutive activity; Agonist bias; System bias; Monod-Wyman-Changeux model; Observed affinity; Efficacy; Receptor activation; Active state; Inactive state;
Keywords: فعالیت مؤثر; Schistosome; G protein-coupled receptor (GPCR); Constitutive activity; Acetylcholine (ACh); G protein-coupled acetylcholine receptor (GAR); RNA interference (RNAi)
Keywords: فعالیت مؤثر; G protein-coupled receptors (GPCRs); Bitter taste receptors (T2Rs); Intracellular loops (ICLs); Constitutive activity; Molecular modeling;
Blocking constitutive activity of GHSR1a in the lateral amygdala facilitates acquisition of conditioned taste aversion
Keywords: فعالیت مؤثر; Ghrelin; GHSR1a; CTA; lateral amygdala; inverse agonist; constitutive activity;
Melanocortin-4 receptor in swamp eel (Monopterus albus): Cloning, tissue distribution, and pharmacology
Keywords: فعالیت مؤثر; ACTH; Adrenocorticotropic hormone; AgRP; Agouti-related protein; α-MSH; α-melanocyte-stimulating hormone; BSA; bovine serum albumin; cAMP; 3â²,5â²-cyclic adenosine monophosphate; CNS; central nervous system; DMEM; Dulbecco's Modified Eagle Medium; ECL
Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor
Keywords: فعالیت مؤثر; Biosensor; Impedance; Label-free; mGlu2 receptor; Constitutive activity; Inverse agonism;
The DRY motif and the four corners of the cubic ternary complex model
Keywords: فعالیت مؤثر; GPRC; heptahelical G protein-coupled receptors; CA; constitutive activity; CAM; constitutively active mutant; CIM; constitutively inactive mutant; TCM; ternary complex model; ETC; extended ternary complex model; CTC; cubic ternary complex model; TM; trans
Increased Metabotropic Glutamate Receptor 5 Signaling Underlies Obsessive-Compulsive Disorder-like Behavioral and Striatal Circuit Abnormalities in Mice
Keywords: فعالیت مؤثر; Circuit; Constitutive activity; mGluR5; Obsessive-compulsive disorder; Positive allosteric modulator; Striatum;
5-HT2C receptors in psychiatric disorders: A review
Keywords: فعالیت مؤثر; 5HT2C signaling; MRNA-editing; Gene polymorphism; Constitutive activity; Psychiatric disorders;
Nucleus accumbens shell excitability is decreased by methamphetamine self-administration and increased by 5-HT2C receptor inverse agonism and agonism
Keywords: فعالیت مؤثر; Methamphetamine; Serotonin; Nucleus accumbens; Constitutive activity; Inverse agonist; 5-HT2C;
Unifying Family A GPCR Theories of Activation
Keywords: فعالیت مؤثر; GPCR; Activation; Constitutive activity; Conservational analysis5HT2A, serotonin 2A receptor; A2A, adenosine A2A receptor; CA, constitutive activity; CAM, constitutively active mutant; FSHR, follicle stimulating hormone receptor; GPCR, G protein-coupled r
Differential requirements of arrestin-3 and clathrin for ligand-dependent and -independent internalization of human G protein-coupled receptor 40
Keywords: فعالیت مؤثر; LA; linoleic acid; LNA; linolenic acid; GPCR; G-protein coupled receptor; HEK; human embryonic kidney; cAMP; cyclic AMP; siRNA; small interfering RNA; shRNA; small hairpin RNA; Rab; ras-related GTP-binding protein; BSA; bovine serum albumin; GRKs; G prote
Usefulness of HeLa cells to evaluate inverse agonistic activity of antihistamines
Keywords: فعالیت مؤثر; GAPDH; glyceraldehyde-3-phosphate dehydrogenase; H1R; histamine H1 receptor; IPs; Inositol phosphates; PKCδ; protein kinase C δ; PMA; phorbol 12-myristate 13-acetate; RT-PCR; reverse transcription-polymerase chain reaction; TCA; trichloroacetic acid; Al
Activation of MAPK by inverse agonists in six naturally occurring constitutively active mutant human melanocortin-4 receptors
Keywords: فعالیت مؤثر; Melanocortin-4 receptor; Inverse agonist; Biased signaling; Constitutive activity;
The three α1-adrenoceptor subtypes show different spatio-temporal mechanisms of internalization and ERK1/2 phosphorylation
Keywords: فعالیت مؤثر; α1-AR; α1 adrenoceptor; β2-AR; β2 adrenoceptor; AT1AR; angiotensin receptor type 1A; Bmax; maximum number of binding sites; BSA; bovine serum albumin; ConA; concanavalin A; DMSO; dimethyl sulfoxide; EGFR; epidermal growth factor receptor; GAPDH; glyce
Evidence for constitutively-active adenosine receptors at mammalian motor nerve endings
Keywords: فعالیت مؤثر; G-protein coupled receptor; Constitutive activity; A1 adenosine receptor; Neuromuscular junction; End-plate potential; Neurotransmitter release;
Chronic treatment with the opioid antagonist naltrexone favours the coupling of spinal cord μ-opioid receptors to Gαz protein subunits
Keywords: فعالیت مؤثر; Opioid antagonist; Opioid receptors; G-protein; Adenylyl cyclase; Constitutive activity; Inverse agonismAC, Adenylyl cyclase; DAMGO, Tyr-d-Ala-Gly-Me-Fe-Gly-ol-enkephalin; FK, Forskolin; ODN, oligodeoxyribonucleotides; PTX, Pertussis toxin
Diverse effects of 5-HT2C receptor blocking agents on c-Fos expression in the rat basal ganglia
Keywords: فعالیت مؤثر; 5-HT2C receptor; Endogenous 5-HT tone; Constitutive activity; 5-HT2C pharmacology; c-Fos expression; Basal ganglia;
Cannabinoid CB1 receptor ligand binding and function examined through mutagenesis studies of F200 and S383
Keywords: فعالیت مؤثر; Cannabinoid receptor; G protein-coupled receptor; Mutagenesis; Rimonabant; Constitutive activity; Aromatic stacking;
Modulation of histamine H3 receptor function by monovalent ions
Keywords: فعالیت مؤثر; GPCR, G protein-coupled receptor; h, human; H3R, histamine H3 receptor; H4R, histamine H4 receptor; TM, transmembrane domain; HA, histamine; THIO, thioperamide; NAMH, Nα-methylhistamineHistamine H3 receptor; Constitutive activity; Gi/Go-proteins; GTPase;
Molecular and pharmacological characterization of the melanocortin type 1 receptor in the sea bass
Keywords: فعالیت مؤثر; Melanocortin receptor 1 (MC1R); Agouti-related protein (AGRP); Constitutive activity; Inverse agonism; IBMX; Phosphodiesterase inhibitor; Fish
An Angiotensin II type 1 receptor activation switch patch revealed through Evolutionary Trace analysis
Keywords: فعالیت مؤثر; 7TM receptor; GPCR; Evolutionary Trace; Constitutive activity; Angiotensin
Metabotropic Glutamate Receptor 5/Homer Interactions Underlie Stress Effects on Fear
Keywords: فعالیت مؤثر; Conditioned fear; constitutive activity; Homer; metabotropic glutamate receptor 5; posttraumatic stress disorder; stress
A reporter assay for G-protein-coupled receptors using a B-cell line suitable for stable episomal expression
Keywords: فعالیت مؤثر; GPCR; Reporter assay; Chimeric G protein; Estrogen-inducible expression; Namalwa KJM-1; Episomal vector; Constitutive activity; Inverse agonist
Temperature dependent photolabeling of the human angiotensin II type 1 receptor reveals insights into its conformational landscape and its activation mechanism
Keywords: فعالیت مؤثر; GPCR; Photolabeling; Molecular modeling; Constitutive activity; Angiotensin II
Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28
Keywords: فعالیت مؤثر; HCMV; Viral GPCR; Nonpeptidergic; Constitutive activity; Chemokine; Inverse agonist; Herpesvirus
Sf9 cells: A versatile model system to investigate the pharmacological properties of G protein-coupled receptors
Keywords: فعالیت مؤثر; Sf9 insect cells; GPCR; G-protein; Functional reconstitution; Constitutive activity; Protein expression[125I]APT, 125I-labeled iodoaminopotentidine; [32P]AAGTP, [32P]P3(4-azidoanilido)-P1-5′-GTP; 5-HTxR, serotonine receptor subtypes; AC, adenylyl cyclase
Changes in the properties of allosteric and orthosteric GABAB receptor ligands after a continuous, desensitizing agonist pretreatment
Keywords: فعالیت مؤثر; GABAB receptor; Constitutive activity; Inverse agonism; Allosteric modulator; Desensitization; Ligand property; Efficacy
The constitutive activity of the ghrelin receptor attenuates apoptosis via a protein kinase C-dependent pathway
Keywords: فعالیت مؤثر; Ghrelin receptors; Constitutive activity; Apoptosis
Histamine H4 receptor–RGS fusion proteins expressed in Sf9 insect cells: A sensitive and reliable approach for the functional characterization of histamine H4 receptor ligands
Keywords: فعالیت مؤثر; Histamine H4 receptor; Fusion protein; RGS protein; Steady-state GTPase assay; Constitutive activity; Gi-proteins
Current status of inverse agonism at serotonin2A (5-HT2A) and 5-HT2C receptors
Keywords: فعالیت مؤثر; Serotonin 5-HT2A receptor; Serotonin 5-HT2C receptor; Inverse agonism; Constitutive activity; Stimulus trafficking
Differential coupling of the human cannabinoid receptors hCB1R and hCB2R to the G-protein Gαi2β1γ2
Keywords: فعالیت مؤثر; AM 251; 6-iodopravadoline; AM 630; (6-iodo-2-methyl-1-[2-4(morpholinyl)-ethyl]-[1H-indol-3-yl]-(4-methoxyphenyl)methan-none); β2ARβ; 2-adrenoceptor; CP 55, 940; [(-)-cis-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-trans-4-(3-hydroxypropyl)cyclohexanol];
Role of third intracellular loop of the melanocortin 4 receptor in the regulation of constitutive activity
Keywords: فعالیت مؤثر; Melanocortin; Melanocortin 4 receptor; Constitutive activity; G protein; Intracellular loop; Obesity; Mutation
Fine-tuning serotonin2c receptor function in the brain: Molecular and functional implications
Keywords: فعالیت مؤثر; 5-HT2C receptor; Constitutive activity; RNA editing; Dopamine; Microdialysis
Constitutive activity and inverse agonism at the α1adrenoceptors
Keywords: فعالیت مؤثر; GPCR, G protein-coupled receptor; AR, adrenoceptor; CAM, constitutively active mutant; MD, molecular dynamicsAdrenoceptors; G protein-coupled receptors; G proteins; Constitutive activity; Inverse agonism; Molecular dynamics
Histamine H3 and dopamine D2 receptor-mediated [35S]GTPγ[S] binding in rat striatum: Evidence for additive effects but lack of interactions
Keywords: فعالیت مؤثر; Histamine; H3 receptor; D2 receptor; Constitutive activity; Gi/o protein; [35S]GTPγS
The activation mechanism of chemokine receptor CCR5 involves common structural changes but a different network of interhelical interactions relative to rhodopsin
Keywords: فعالیت مؤثر; Activation; CCR5; Constitutive activity;
Proteometric study of ghrelin receptor function variations upon mutations using amino acid sequence autocorrelation vectors and genetic algorithm-based least square support vector machines
Keywords: فعالیت مؤثر; 7TM protein; Mutational studies; Kernel-based methods; QSAR; Ghrelin; Autocorrelation vectors; Constitutive activity
Clozapine and Haloperidol Differentially Alter the Constitutive Activity of Central Serotonin2C Receptors In Vivo
Keywords: فعالیت مؤثر; Dopamine release; 5-HT2C receptor; constitutive activity; clozapine; haloperidol; inverse agonist
Functional domains of the subtype 1 neurotensin receptor (NTS1)
Keywords: فعالیت مؤثر; NTS1; GPCR; G proteins; Agonist; Antagonist; Constitutive activity
Some implications of receptor theory for in vivo assessment of agonists, antagonists and inverse agonists
Keywords: فعالیت مؤثر; Inverse agonist; Agonist; Antagonist; Receptor theory; In vivo; Constitutive activity
Heterologous desensitization is evoked by both agonist and antagonist stimulation of the human 5-HT7 serotonin receptor
Keywords: فعالیت مؤثر; Adenylyl cyclase; Inverse agonist; Constitutive activity; Splice variant; Resensitization
The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat
Keywords: فعالیت مؤثر; Basolateral amygdala; Protean agonism; Contextual fear conditioning; Local administration; Systemic administration; Constitutive activity;
Constitutive activity of human angiotensin II type-1 receptors by Gq overexpression
Keywords: فعالیت مؤثر; Angiotensin II; AT1R; G protein; Gq; Constitutive activity; HEK293; Tet-On; Inducible; Overexpression;
Constitutive activity of endogenous receptors by inducible Gq overexpression
Keywords: فعالیت مؤثر; G protein; Gq; Constitutive activity; HEK293; Tet-On; Inducible; Overexpression;
A “locked-on,” constitutively active mutant of the adenosine A1 receptor
Keywords: فعالیت مؤثر; Adenosine A1 receptor; Inverse agonism; Constitutive activity; G14T mutant; “Locked-on” phenotype;
Neuronal nitric oxide modulates morphine antinociceptive tolerance by enhancing constitutive activity of the μ-opioid receptor
Keywords: فعالیت مؤثر; DAMGO; [D-Ala2, N-MePhe4, Gly-ol5]enkephalin; GDP; guanosine diphosphate; GPCR; G-protein-coupled receptor; GppNHp; 5â²guanylylimidodiphosphate; GTPγS; guanosine5â²-G-(3-thio)triphosphate; NaCl; sodium chloride; NO; nitric oxide; Constitutive activity;
Analysis of mGluR1a constitutive internalization using a pulse-chase enzyme-linked immuno-sorbant assay (ELISA)
Keywords: فعالیت مؤثر; DM; deletion mutant; DNM; dominant negative mutant; ELISA; enzyme-linked immuno-sorbant assay; Eps15; EGFR pathway substrate clone 15; GPT; glutamate pyruvate transaminase; HEK293; human embryonic kidney cells 293; HA; Hemagglutinin; mGluR; metabotropic g