Keywords: منحنی آلوزیستریک منفی; Cross-species translation; Drug discovery; Major depressive disorder; mGlu5 receptor; Negative allosteric modulator; Substance use disorder;
مقالات ISI منحنی آلوزیستریک منفی (ترجمه نشده)
مقالات زیر هنوز به فارسی ترجمه نشده اند.
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.
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: منحنی آلوزیستریک منفی; AC-42; 4-(4-Butyl-1-piperidinyl)-1-(2-methylphenyl)-1-butanone hydrochloride; ACh; acetylcholine; AM; allosteric modulator; BQCA; Benzyl quinolone carboxylic acid; ECL; extracellular loop; FRET; Förster resonance energy transfer; F-V curve; Function -
Keywords: منحنی آلوزیستریک منفی; Cannabinoid; Negative allosteric modulator; CB1 NAM; Indole sulfonamide
Keywords: منحنی آلوزیستریک منفی; DMAC; N,N-dimethylacetamide; DMF; N,N-dimethylformamide; LiHMDS; lithium bis(trimethylsilyl)amide; mGlu5; metabotropic glutamate receptor subtype 5; NAM; negative allosteric modulator; GPCR; G-protein coupled receptor; TFA; trifluoroacetic acid; TLC; thin
Keywords: منحنی آلوزیستریک منفی; 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
Keywords: منحنی آلوزیستریک منفی; NAM; negative allosteric modulator; nAChRs; neuronal nicotinic acetylcholine receptors; HBK; HEPES-buffered Krebs; LBVS; ligand-based virtual screening; SBVS; structure-based virtual screening; SAR; structure-activity relationship; nh; Hill coefficient;
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator; Hit to lead studies; CNS drug discovery
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator; 4-Aryl-3-arylsulfonyl-quinolines
Enantiomer-specific positive allosteric modulation of CB1 signaling in autaptic hippocampal neurons
Keywords: منحنی آلوزیستریک منفی; DSE; depolarization-induced suppression of excitation; 2-AG; 2-arachidonoyl glycerol; NAM; negative allosteric modulator; PAM; positive allosteric modulator; EPSC; excitatory postsynaptic current; Allosteric; Orthosteric; G protein-coupled receptor; Canna
Identification of compounds acting as negative allosteric modulators of the LPA1 receptor
Keywords: منحنی آلوزیستریک منفی; Negative allosteric modulator; LPA1 receptor; G-protein signalling; Backscattering interferometry; Fibrosis;
Design, synthesis, and functional assessment of Cmpd-15 derivatives as negative allosteric modulators for the β2-adrenergic receptor
Keywords: منحنی آلوزیستریک منفی; β2-Adrenergic receptor (β2AR); Negative allosteric modulator; Synthesis; Structure-activity relationships; Binding competition assays;
Identification by virtual screening and functional characterisation of novel positive and negative allosteric modulators of the α7 nicotinic acetylcholine receptor
Keywords: منحنی آلوزیستریک منفی; Nicotinic acetylcholine receptor; Ion channel; Allosteric modulation; Virtual screening; 5-HT; 5-hydroxytryptamine; DB04763; 1-N-(4-sulfamoylphenethyl)-2,4,6-trimethylpyridinium tetrafluoroborate; AUC; area under the curve; CAII; carbonic anhydrase II; CD
Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells
Keywords: منحنی آلوزیستریک منفی; Protease-Activated Receptor; PAR1; PAR2; GPCR; Calcium mobilization; Parmodulin; ML161; Vorapaxar; RWJ-58259; Negative allosteric modulator;
The metabotropic glutamate receptor 5 radioligand [11C]AZD9272 identifies unique binding sites in primate brain
Keywords: منحنی آلوزیستریک منفی; PET imaging; Autoradiography; Metabotropic glutamate receptor 5; Negative allosteric modulator; AZD9272; Fenobam;
mGlu4 allosteric modulation for treating Parkinson's disease
Keywords: منحنی آلوزیستریک منفی; Parkinson's disease; Dyskinesia; Glutamate; Dopamine; mGlu4; 6-OHDA; 6-hydroxydopamine; ADX88178; 4-methyl-N-[5-methyl-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-yl]pyrimidin-2-amine; AIM; abnormal involuntary movements; CODA-RET; complemented donor acceptor reson
Rescue of Fmr1KO phenotypes with mGluR5 inhibitors: MRZ-8456 versus AFQ-056
Keywords: منحنی آلوزیستریک منفی; mGluR5; Fmr1; MRZ-8456; AFQ-056; MPEP; Amyloid-beta precursor protein; Aβ; amyloid-beta; ABC-C; Aberrant Behavior Checklist-Community Edition; AGS; audiogenic-induced seizures; APP; amyloid-beta protein precursor; CNS; central nervous system; CTEP; 2-chl
Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor
Keywords: منحنی آلوزیستریک منفی; ACh; acetylcholine; mAChR; muscarinic acetylcholine receptor; GPCR; G protein-coupled receptor; AD; Alzheimer's disease; PAM; positive allosteric modulator; NAM; negative allosteric modulator; TM; transmembrane domain; ECL; extracellular loop; CHO; Chin
The GABAAα5-selective Modulator, RO4938581, Rescues Protein Anomalies in the Ts65Dn Mouse Model of Down Syndrome
Keywords: منحنی آلوزیستریک منفی; AD; Alzheimer's disease; AMPA; α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; BDNF; brain-derived neurotrophic factor; CFC; context fear conditioning; CS; context-shock; DS; Down syndrome; FDR; false discovery rate; FvN; failed vs. normal learni
Synthesis and optimization of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as potent and orally-active metabotropic glutamate receptor 5 negative allosteric modulators
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator; CNS drug discovery; Anti-depressant agent;
GRIN2B gain of function mutations are sensitive to radiprodil, a negative allosteric modulator of GluN2B-containing NMDA receptors
Keywords: منحنی آلوزیستریک منفی; GRIN2B; Mutation; Encephalopathy; Electrophysiology; Radiprodil; NMDA inhibitors; ANOVA; analysis of variance; ATD; amino-terminal domain; DMSO; dimethyl sulfoxide; LBD; ligand-binding domain; NAM; negative allosteric modulator; NMDA; N-methyl-d-aspartate
A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain
Keywords: منحنی آلوزیستریک منفی; NMDA receptor; Positive allosteric modulator; Transmembrane domain; ATD; amino terminal domain; iGluR; ionotropic glutamate receptor; LBD; ligand-binding domain; NAM; negative allosteric modulator; PAM; positive allosteric modulator; TMD; transmembrane do
Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators
Keywords: منحنی آلوزیستریک منفی; mGlu5 receptor; Negative allosteric modulator; 4-amino-3-arylsulfonyl-quinolines; Parallel synthesis; Optimization;
Molecular insights into allosteric modulation of Class C G protein-coupled receptors
Keywords: منحنی آلوزیستریک منفی; GABAB; γ-aminobutyric acid receptor B; BMD; bone mass and density; CaSR; calcium-sensing receptor; CHO; Chinese hamster ovary; CRD; cysteine-rich domain; ER; endoplasmic reticulum; Ca2+o; extracellular calcium; pERK1/2; extracellular signal-regulated kin
Further optimization of the M5 NAM MLPCN probe ML375: Tactics and challenges
Keywords: منحنی آلوزیستریک منفی; M5; Muscarinic receptor; Negative allosteric modulator; Matrix library; Pharmacokinetics
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator; Thieno[2,3-b]pyridines
Aiming for allosterism: Evaluation of allosteric modulators of CB1 in a neuronal model
Keywords: منحنی آلوزیستریک منفی; DSE; depolarization-induced suppression of excitation; 2-AG; 2-arachidonoly glycerol; NAM; negative allosteric modulator; PAM; positive allosteric modulator; Î9THC; tetrahydrocannabinol; EPSC; excitatory postsynaptic current; pERK; phospho extracellular
DSR-98776, a novel selective mGlu5 receptor negative allosteric modulator with potent antidepressant and antimanic activity
Keywords: منحنی آلوزیستریک منفی; mGlu5 receptor; Major depressive disorder; Mania; Bipolar disorder; Negative allosteric modulator
Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel
Keywords: منحنی آلوزیستریک منفی; Kv11.1(hERG) channel; Negative allosteric modulator; Radioligand binding assay; Antiarrhythmia; Kv11.1 blockers;
New paradigms in GPCR drug discovery
Keywords: منحنی آلوزیستریک منفی; cAMP; 3â²,5â²-cyclic adenosine monophosphate; ADP; adenosine 5â²- diphosphate; GPCR; G protein-coupled receptor; TM; transmembrane helix; ERK; extracellular signal-regulated kinase; T4L; T-4 lysozyme; BRIL; thermostabilized apocytochrome b562; StaRs; s
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Hit-to-lead optimization
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator;
mGlu2 receptor-mediated modulation of conditioned avoidance behavior in rats
Keywords: منحنی آلوزیستریک منفی; BINA; 3׳-{[(2-cyclopentyl-6,7-dimethyl-1-oxo-2,3-dihydro-1H-inden-5-yl)oxy]methyl}biphenyl-4-carboxylic acid; JNJ-42112265; 7-(dimethylamino)- 4-(3-pyridin-3-ylphenyl)-8-(trifluoromethyl)-1,3-dihydro-2H-1,5-benzodiazepin-2-one; JNJ-42153605; 3-(cyclopro
Carbamazepine derivatives with P2X4 receptor-blocking activity
Keywords: منحنی آلوزیستریک منفی; Heterocycles; Inflammation; Ligand-gated ion channel; Negative allosteric modulator; Neuropathic pain; P2X4 receptor; Structure-activity relationship; Synthesis; Tricyclics;
Development of allosteric modulators of GPCRs for treatment of CNS disorders
Keywords: منحنی آلوزیستریک منفی; 5MPEP; 5-methyl-6-(phenylethynyl)-pyridine; 6-OHDA; 6-hydroxydopamine; 7TMR; seven transmembrane receptor; 77-LH-28-1; 1-[3-(4-butyl-1-piperidinyl)propyl]-3,4-dihydro-2(1H)-quinolinone; AC-42; 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine; ACh
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: منحنی آلوزیستریک منفی; mGlu5 receptor; Negative allosteric modulator; Receptor occupancy; Formalin model; Rotorod test;
Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator;
Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator; GPCR; In vitro pharmacology; Pain; Clinical candidate;
Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists
Keywords: منحنی آلوزیستریک منفی; Glutamate; Excitatory amino acid; Metabotropic glutamate receptor; mGluR5; Negative allosteric modulator; 1H-pyrrolo[2,3-c]pyridine-7-carboxamides
Invited reviewMetabotropic glutamate receptors as therapeutic targets for schizophrenia
Keywords: منحنی آلوزیستریک منفی; Metabotropic; Glutamate; Schizophrenia; NMDA; allosteric; CNS; central nervous system; DA; dopamine; mGlu; metabotropic glutamate receptor; PAM; positive allosteric modulator; NAM; negative allosteric modulator; MPEP; 2-methyl-6-(phenylethynyl)pyridine; N
3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: Hit to lead studies
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator; Anxiolytic; LipE;
Strategies for the identification of allosteric modulators of G-protein-coupled receptors
Keywords: منحنی آلوزیستریک منفی; GPCR; G-protein-coupled receptor; PAM; positive allosteric modulator; NAM; negative allosteric modulator; SAM; silent allosteric modulator; NAL; neutral allosteric ligand; HTS; high-throughput screening; cAMP; 3â²-5â²-cyclic adenosine monophosphate; mGl
The identification of novel orally active mGluR5 antagonist GSK2210875
Keywords: منحنی آلوزیستریک منفی; mGluR; mGluR5; Brain free fraction; Negative allosteric modulator; Allosteric modulator; GPCR; Family C GPCR; Metabotropic glutamate receptor
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator; Parallel synthesis;
In vitro and in vivo characterization of a novel negative allosteric modulator of neuronal nAChRs
Keywords: منحنی آلوزیستریک منفی; Neuronal nicotinic acetylcholine receptors; Negative allosteric modulator; Patch-clamp; Binding; Nicotine-induced antinociception; nAChR; nicotinic acetylcholine receptor; NAM; negative allosteric modulator; PCP; phencyclidine; HDMP; 1,2,3,3a,4,8b-hexahyd
Effect of CFMTI, an allosteric metabotropic glutamate receptor 1 antagonist with antipsychotic activity, on Fos expression in regions of the brain related to schizophrenia
Keywords: منحنی آلوزیستریک منفی; metabotropic glutamate receptor; negative allosteric modulator; G protein coupled receptor; c-fos; prefrontal cortex; clozapine; ARC; arcuate hypothalamic nucleus; BCIP; 5-bromo-4-chloro-3-indolyl phosphate; BNST; bed nucleus of the stria terminalis; BSA;
Metabotropic glutamate mGlu1 receptor stimulation and blockade: Therapeutic opportunities in psychiatric illness
Keywords: منحنی آلوزیستریک منفی; Metabotropic glutamate mGlu1 receptor; Negative allosteric modulator; Positive allosteric modulator; Anxiety; Depression; Schizophrenia
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5
Keywords: منحنی آلوزیستریک منفی; Glutamate; Metabotropic glutamate receptor 5; Negative allosteric modulator; Non-competitive antagonist; Quinazoline
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS
Keywords: منحنی آلوزیستریک منفی; mGluR5; Negative allosteric modulator; Positive allosteric modulator
Target site occupancy: Emerging generalizations from clinical and preclinical studies
Keywords: منحنی آلوزیستریک منفی; Target site occupancy; Receptor reserve; Positron Emission Tomography; Single Photon Emission Computed Tomography; G protein-coupled receptor; Target biomarker; BZD; benzodiazepine; CNS; central nervous system; DAT; dopamine transporter; EEDQ; N-ethoxycar