Keywords: اشباع گیرنده; Mu opioid receptor; Morphine; Oxycodone; Receptor occupancy; Autoradiography;
مقالات ISI اشباع گیرنده (ترجمه نشده)
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در صورتی که به ترجمه آماده هر یک از مقالات زیر نیاز داشته باشید، می توانید سفارش دهید تا مترجمان با تجربه این مجموعه در اسرع وقت آن را برای شما ترجمه نمایند.
Keywords: اشباع گیرنده; Major depressive disorder; Cognitive function; Vortioxetine; Lu AA21004; Electrophysiology; Receptor occupancy;
Keywords: اشباع گیرنده; Ketamine; N-methyl-d-aspartate receptor; Receptor occupancy; Schizophrenia; Cognitive disruption; Depression;
Keywords: اشباع گیرنده; Glutamate; Antidepressant; Anxiolytic; Analgesic; Ketamine; STAR*D; Receptor occupancy; MOA; mechanism of action; NAM; negative allosteric modulator; PPS; painful physical symptoms; MDD; major depressive disorder; STAR*D; sequenced treatment alternatives
Dose-Related Target Occupancy and Effects on Circuitry, Behavior, and Neuroplasticity of the Glycine Transporter-1 Inhibitor PF-03463275 in Healthy and Schizophrenia Subjects
Keywords: اشباع گیرنده; Cognition; Glycine transporter inhibitor; Long-term potentiation; Neuroplasticity; NMDA receptor; Positron emission tomography; Receptor occupancy; Schizophrenia;
Optimization of maintenance therapy of Risperidone with CYP2D6 genetic polymorphisms through an extended translational framework-based prediction of target occupancies/clinical outcomes
Keywords: اشباع گیرنده; RO; receptor occupancy; EPS; extrapyramidal symptoms; PK; pharmacokinetic; PD; pharmacodynamic; EM; extensive metabolizer; IM; intermediate metabolizer; PM; poor metabolizer; PBPKPD; physiology-based pharmacokinetic and pharmacodynamic; P-gp; P-glycoprote
Review articleNK1 receptor antagonists for depression: Why a validated concept was abandoned
Keywords: اشباع گیرنده; PET; Receptor occupancy; NK1; Depression;
Simultaneous in-vivo receptor occupancy assays for serotonin 1A, 2A, and dopamine 2 receptors with the use of non-radiolabelled tracers: Proposed method in screening antipsychotics
Keywords: اشباع گیرنده; ED50; Effective dose producing 50% receptor occupancy; g; Gram; i.v.; Intravenous; p.o.; Per oral; Kg; Kilogram; min; Minute; mL; Millilitre; mg; Milligram; μg; Microgram; ng; Nanogram; rpm; Rotations per minute; RO; Receptor Occupancy; CNS; Central nerv
Quantitative prediction of histamine H1 receptor occupancy by the sedative and non-sedative antagonists in the human central nervous system based on systemic exposure and preclinical data
Keywords: اشباع گیرنده; Positron emission tomography; Central nervous system; Receptor occupancy; Histamine H1 receptor; P-glycoprotein; Physiologically based pharmacokinetic model; AUC; area under the curve; BBB; blood-brain barrier; CNS; central nervous system; Cblood; blood
GABAA receptor subtypes in the mouse brain: Regional mapping and diazepam receptor occupancy by in vivo [18F]flumazenil PET
Keywords: اشباع گیرنده; GABAA receptor; Alpha subunit; Selective; Benzodiazepine; Receptor occupancy;
Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists
Keywords: اشباع گیرنده; Histamine H3 receptor; SAR; Pharmacokinetic profile; Receptor occupancy;
N-phenylpropyl-Nâ²-substituted piperazines occupy sigma receptors and alter methamphetamine-induced hyperactivity in mice
Keywords: اشباع گیرنده; Behavior; Methamphetamine; Locomotor activity; Mouse; Dopamine transporter; Receptor occupancy; Sigma receptor;
An FDA oncology analysis of immune activating products and first-in-human dose selection
Keywords: اشباع گیرنده; MABEL; Immune oncology; First-in-human dose; ADCC; antibody-dependent cellular cytotoxicity; CRA; cytokine release assay; CRS; cytokine release syndrome; DLT; dose limiting toxicity; EMA; European Medicines Agency; FIH; first-in-human; HHD; highest human
Prediction of CNS occupancy of dopamine D2 receptor based on systemic exposure and in vitro experiments
Keywords: اشباع گیرنده; Positron emission tomography; Brain; Central nervous system; Human; Receptor occupancy; Dopamine D2 receptor; Physiologically based pharmacokinetic model; AUC; area under the blood concentration time curve; BBB; blood-brain barrier; BSA; bovine serum al
A PET study comparing receptor occupancy by five selective cannabinoid 1 receptor antagonists in non-human primates
Keywords: اشباع گیرنده; Cannabinoid 1 receptor (CB1R) antagonists; Obesity; Positron emission tomography (PET); Receptor occupancy; [11C]SD5024; Rimonabant; TaranabantAZ, AstraZeneca; AUC, area under the curve; BBB, blood–brain barrier; CB1R, cannabinoid 1 receptor; CD, candidat
A comparison of two semi-mechanistic models for prolactin release and prediction of receptor occupancy following administration of dopamine D2 receptor antagonists in rats
Keywords: اشباع گیرنده; Risperidone (PubChem CID: 5073); Paliperidone (PubChem CID: 115237); Remoxipride (PubChem CID: 54477)Precursor pool model; Prolactin; Agonist-antagonist interaction model; Receptor occupancy; Dopamine D2 receptor antagonists
A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334
Keywords: اشباع گیرنده; P2X7; Radioligand binding; Depression; Autoradiography; Receptor occupancy; JNJ-54232334; JNJ-54140515;
Design, synthesis and evaluation of [3H]PF-7191, a highly specific nociceptin opioid peptide (NOP) receptor radiotracer for in vivo receptor occupancy (RO) studies
Keywords: اشباع گیرنده; NOP receptor; ORL1; Radiotracer; Receptor occupancy; PET
Examining dopamine D3 receptor occupancy by antipsychotic drugs via [3H]7-OH-DPAT ex vivo autoradiography and its cross-validation via c-fos immunohistochemistry in the rat brain
Keywords: اشباع گیرنده; c-fos; D2; D3; Major islands of Calleja; Receptor occupancy
Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator
Keywords: اشباع گیرنده; mGlu5 receptor; Negative allosteric modulator; Receptor occupancy; Formalin model; Rotorod test;
Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression
Keywords: اشباع گیرنده; Neurokinin 1 antagonists; Serotonin transporter inhibitors; Receptor occupancy; Depression;
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor
Keywords: اشباع گیرنده; Ghrelin; Antagonist; Inverse agonist; Receptor; Receptor occupancy; Muscarinic;
A positron emission tomography study in healthy volunteers to estimate mGluR5 receptor occupancy of AZD2066 - Estimating occupancy in the absence of a reference region
Keywords: اشباع گیرنده; Nonlinear mixed effects modelling; Positron emission tomography; Receptor occupancy; [11C]-ABP688; mGluR5 receptor;
Non linear mixed effects analysis in PET PK-receptor occupancy studies
Keywords: اشباع گیرنده; Non-linear mixed effects approach; Non-linear least squares approach; Pharmacokinetics; Receptor occupancy; PET study;
Lu AA21004, a novel multimodal antidepressant, produces regionally selective increases of multiple neurotransmitters-A rat microdialysis and electrophysiology study
Keywords: اشباع گیرنده; Lu AA21004; Preclinical; Receptor occupancy; Neurotransmitters; Multimodal;
Rhythmic theta and delta activity of cortical and hippocampal neuronal networks in genetically or pharmacologically induced N-methyl-d-aspartate receptor hypofunction under urethane anesthesia
Keywords: اشباع گیرنده; AMPAR; alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor; ANOVA; analysis of variance; CA1; hippocampal region CA1; EEG; Electroencephalogram; Grin1; Grin1tm1Bhk mouse model expressing reduced NR1 NMDAR subunit expression; IV; intravenous;
Comparison of the ex vivo receptor occupancy profile of ketamine to several NMDA receptor antagonists in mouse hippocampus
Keywords: اشباع گیرنده; Ketamine; GluN2B; NMDA; Autoradiography; Receptor occupancy
3-Phenyl-5-isothiazole carboxamides with potent mGluR1 antagonist activity
Keywords: اشباع گیرنده; mGluR1; Receptor occupancy; Formalin model
Non-linear mixed effects modelling of positron emission tomography data for simultaneous estimation of radioligand kinetics and occupancy in healthy volunteers
Keywords: اشباع گیرنده; Nonlinear mixed effects modelling; Positron emission tomography; Receptor occupancy; [11C]AZD9272; mGluR5 receptor;
Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia
Keywords: اشباع گیرنده; Orexin; Hypocretin; Insomnia; Receptor occupancy; Pharmacology; MK-6096
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies
Keywords: اشباع گیرنده; Cannabinoid; Radioligand; Receptor occupancy; Obesity
5-HT4 receptor agonist mediated enhancement of cognitive function in vivo and amyloid precursor protein processing in vitro: A pharmacodynamic and pharmacokinetic assessment
Keywords: اشباع گیرنده; 5-HT4 receptor agonist; sAPPα; Cholinesterase; Morris water maze; Receptor occupancy; VelusetragAD, Alzheimer's disease; ACh, acetylcholine; AChEi, acetylcholine esterase inhibitor; APP, amyloid precursor protein; sAPPα, soluble amyloid precursor protein
Ex vivo delta opioid receptor autoradiography: CNS receptor occupancy of two novel compounds over their antihyperalgesic dose range
Keywords: اشباع گیرنده; Delta opioid agonist; Hyperalgesia; Ex vivo autoradiography; CFA thermal hyperalgesia; Receptor occupancy
Measurement of the pharmacokinetics and pharmacodynamics of neuroactive compounds
Keywords: اشباع گیرنده; Microdialysis; Receptor occupancy; Pharmacokinetics; Pharmacodynamics; Drug safety; Drug efficacy; DMPK; CNS disorder;
The application of drug dose equivalence in the quantitative analysis of receptor occupation and drug combinations
Keywords: اشباع گیرنده; Isobole; Additivity; Synergism; Sub-additivity; Inverted U-shaped dose–effect curves; Receptor occupancy; Competitive antagonism; Combinations with opposite effects
Impact of protein binding on receptor occupancy: A two-compartment model
Keywords: اشباع گیرنده; Plasma-protein binding; Receptor occupancy; Modelling complex systems behaviours; Blood-brain barrier;
Development of a selective and potent radioactive ligand for histamine H3 receptors: A compound potentially useful for receptor occupancy studies
Keywords: اشباع گیرنده; Histamine H3 receptors; Inverse agonist; Radioligand; Receptor occupancy;
Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R)
Keywords: اشباع گیرنده; Melanin-concentrating hormone 1-receptor; Antagonist; Radioligand; Receptor occupancy
Melanin-concentrating hormone 1-receptor antagonist suppresses body weight gain correlated with high receptor occupancy levels in diet-induced obesity mice
Keywords: اشباع گیرنده; Melanin-concentrating hormone 1-receptor Antagonist; Receptor occupancy; Obesity
Impact of plasma-protein binding on receptor occupancy: An analytical description
Keywords: اشباع گیرنده; Plasma-protein binding; Receptor occupancy; Modelling complex systems behaviours; Time scales; Analytical descriptions
Validation of a rat in vivo [3H]M100907 binding assay to determine a translatable measure of 5-HT2A receptor occupancy
Keywords: اشباع گیرنده; 5-HT2A receptor; Receptor occupancy; In vivo binding; Antipsychotics
In vivo rat brain opioid receptor binding of LY255582 assessed with a novel method using LC/MS/MS and the administration of three tracers simultaneously
Keywords: اشباع گیرنده; Opioid; Receptor occupancy; LY255582; In vivo binding; Rat
Comparison of in vivo and ex vivo [3H]flumazenil binding assays to determine occupancy at the benzodiazepine binding site of rat brain GABAA receptors
Keywords: اشباع گیرنده; Flumazenil (Ro 15-1788); In vivo binding; Ex vivo binding; Receptor occupancy; Dissociation; GABA
Comparison of rat dopamine D2 receptor occupancy for a series of antipsychotic drugs measured using radiolabeled or nonlabeled raclopride tracer
Keywords: اشباع گیرنده; Rat; Dopamine; D2; Receptor occupancy; In vivo binding; Striatum; Liquid chromatography; Mass spectroscopy; Chlorpromazine; Clozapine; Haloperidol; Olanzapine; Risperidone; Spiperone; Thioridazine; Ziprasidone; Raclopride;
Transgenic mouse expressing human CCR5 as a model for in vivo assessments of human selective CCR5 antagonists
Keywords: اشباع گیرنده; Chemokine CCR5 receptor; Human CCR5 transgenic mouse; Receptor occupancy; Pharmacodynamics;
Use of LC/MS to assess brain tracer distribution in preclinical, in vivo receptor occupancy studies: Dopamine D2, serotonin 2A and NK-1 receptors as examples
Keywords: اشباع گیرنده; Dopamine; D2; Serotonin; 5-HT2A; Neurokinin; NK-1; Receptor occupancy; In vivo binding; Liquid chromatography; Mass spectroscopy; Haloperidol; Clozapine; Olanzapine; MK-869; Raclopride; MDL-100907; GR205171; Rat; Gerbil;