Keywords: مدولاتور آلوده کننده; 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 -
مقالات ISI مدولاتور آلوده کننده (ترجمه نشده)
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Keywords: مدولاتور آلوده کننده; Glycine receptor; Phage display; Allosteric modulator; Electrophysiology; Xenopus oocytes
Keywords: مدولاتور آلوده کننده; Reproductive; 'Seat' sequence; LRR curvature estimation; Allosteric modulator; GPCR trimer; Receptor activation mechanism;
Keywords: مدولاتور آلوده کننده; Asu-ACR-16; Structure-based drug discovery; Homology modeling; Orthosteric site; Allosteric modulator; Xenopus expressionECD, extracellular domain; TID, transmembrane and intracellular domain; (+), principal subunit; (−), complementary subunit; NAM, negat
Randomized, controlled, proof-of-concept trial of MK-7622 in Alzheimer's disease
Keywords: مدولاتور آلوده کننده; MK-7622; Alzheimer's disease; Cholinergic; Muscarinic; Allosteric modulator; Clinical trial;
The role of human dopamine transporter in NeuroAIDS
Keywords: مدولاتور آلوده کننده; HIV-1 Tat; Dopamine transporter; Cocaine; Allosteric modulator; Mutation;
Positive allosteric modulation of M1 and M4 muscarinic receptors as potential therapeutic treatments for schizophrenia
Keywords: مدولاتور آلوده کننده; Schizophrenia; Allosteric modulator; Muscarinic receptors; M1; M4;
Urotensin core mimics that modulate the biological activity of urotensin-II related peptide but not urotensin-II
Keywords: مدولاتور آلوده کننده; Urotensin-II related peptide; Urotensin-II; Allosteric modulator; Head-to-tail cyclization; Peptide mimicry; SAM-linker;
Perinatal nicotine treatment induces transient increases in NACHO protein levels in the rat frontal cortex
Keywords: مدولاتور آلوده کننده; ANOVA; analysis of variance; EDTA; ethylenediaminetetraacetic acid; FC; frontal cortex; HIP; hippocampus; NACHO; nicotinic acetylcholine receptor regulator chaperone; nAChR; nicotinic acetylcholine receptor; PND; postnatal day; SD; Sprague-Dawley; TMEM3
Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters
Keywords: مدولاتور آلوده کننده; Glutamate receptor subtype 5 (mGlu5); Allosteric modulator; GET 73; Safety; Tolerability;
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor
Keywords: مدولاتور آلوده کننده; Allosteric modulator; CB1 receptor; Endocannabinoid system; MAPK/ERK signaling pathway; Serum response element;
Allosteric modulation of nicotinic and GABAA receptor subtypes differentially modify autism-like behaviors in the BTBR mouse model
Keywords: مدولاتور آلوده کننده; Autism; BTBR; GABA; Nicotinic; Allosteric modulator;
The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABAB receptor with a potential for treatment of anxiety, pain and spasticity
Keywords: مدولاتور آلوده کننده; Allosteric modulator; GABA; Anxiety; Pain; Body temperature; Baclofen; Spasticity; Clinical candidate; GABA (PubChem CID: 119); (R)-Baclofen (PubChem CID: 44602); Diazepam (PubChem CID: 3016); Chlordiazepoxide (PubChem CID: 2712);
Lynx1 and Aβ1-42 bind competitively to multiple nicotinic acetylcholine receptor subtypes
Keywords: مدولاتور آلوده کننده; Alzheimer's disease; nAChR; Lynx; Ly-6; Allosteric modulator;
Synthesis and biological evaluation of indole-2-carboxamides bearing photoactivatable functionalities as novel allosteric modulators for the cannabinoid CB1 receptor
Keywords: مدولاتور آلوده کننده; Cannabinoid receptor; Allosteric modulator; Photoaffinity labeling; Photoactivatable ligands; CB1; Cannabinoid type 1 receptor; GPCR; G-protein coupled receptor; nAChRs; nicotinic acetylcholine receptors; BP; benzophenone; PTFMD; phenyltrifluoromethyldiaz
A novel dualistic profile of an allosteric AMPA receptor modulator identified through studies on recombinant receptors, mouse hippocampal synapses and crystal structures
Keywords: مدولاتور آلوده کننده; ACSF; artificial cerebrospinal fluid; AMPA; 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid; BDNF; brain-derived neurotrophic factor; CA1; cornu ammonis area 1; CTZ; cyclothiazide; DEPC; diethylpyrocarbonate; DMSO; dimethyl sulfoxide; fEPSP; fie
Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study
Keywords: مدولاتور آلوده کننده; A1 adenosine receptor; Allosteric modulator; G protein-coupled receptors; Anti-nociceptive effect; BVIOAYZXVAUUIG-UHFFFAOYSA-N;
Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M1 positive allosteric modulators
Keywords: مدولاتور آلوده کننده; M1; Allosteric modulator; Muscarinic; Alzheimer’s disease; P-glycoprotein
Discovery of VU0431316: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety
Keywords: مدولاتور آلوده کننده; Glutamate; CNS; mGlu5; Allosteric modulator; Anxiety;
Allosteric modulators of the hERG K+ channel
Keywords: مدولاتور آلوده کننده; hERG K+ channel; Allosteric modulator; LUF6200; Potassium ions; [3H]astemizole; [3H]dofetilide;
mGlu2 receptor-mediated modulation of conditioned avoidance behavior in rats
Keywords: مدولاتور آلوده کننده; 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
QSAR design of triazolopyridine mGlu2 receptor positive allosteric modulators
Keywords: مدولاتور آلوده کننده; QSAR; Topomer CoMFA; Top-CoMFA; SVM; Allosteric modulator
Development of allosteric modulators of GPCRs for treatment of CNS disorders
Keywords: مدولاتور آلوده کننده; 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
Group II metabotropic glutamate receptor-mediated activation of G-proteins in rat hippocampal and striatal membranes
Keywords: مدولاتور آلوده کننده; CNS; central nervous system; NMDA; N-methyl-d-aspartate; AMPA; α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; GPCR; G-protein-coupled receptor; mGlu receptor; metabotropic glutamate receptor; [35S]GTPγS; guanosine-5â²-O-(3-[35S]thio)triphosphate
Synthesis and evaluation of a conditionally-silent agonist for the α7 nicotinic acetylcholine receptor
Keywords: مدولاتور آلوده کننده; Silent-agonist; Allosteric modulator; Ion-channel; Nicotinic receptor;
N-Acyl-Nâ²-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats
Keywords: مدولاتور آلوده کننده; Glutamate; GPCR; mGlu1; Allosteric modulator; CNS; Piperazine;
Neuropharmacology and analgesiaQuercetin antagonism of GABAAÏ1 receptors is prevented by ascorbic acid through a redox-independent mechanism
Keywords: مدولاتور آلوده کننده; GABA; γ-aminobutyric acid; NEM; N-ethylmaleimide; GABA receptor; Flavonoid; Quercetin; Ascorbic acid; Allosteric modulator;
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety
Keywords: مدولاتور آلوده کننده; Glutamate; CNS; mGlu5; Allosteric modulator; Anxiety;
Preclinical pharmacokinetic and toxicological evaluation of MIF-1 peptidomimetic, PAOPA: Examining the pharmacology of a selective dopamine D2 receptor allosteric modulator for the treatment of schizophrenia
Keywords: مدولاتور آلوده کننده; 5-HT2; 5-hydroxytryptamine; 6-OHDA; 6-hydroxydopamine; AM; allosteric modulator; AUC; area under curve; AUCINF; area under curve extrapolated to infinity; AUClast; area under curve from dosing to observation; AUMC; area under first moment curve; CL; total
Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1
Keywords: مدولاتور آلوده کننده; Glutamate; GPCR; mGlu1; Allosteric modulator; CNS; Octahydropyrrolo[3,4-c]pyrrole;
Functional selectivity induced by mGlu4 receptor positive allosteric modulation and concomitant activation of Gq coupled receptors
Keywords: مدولاتور آلوده کننده; Glutamate; Histamine; Receptor; Allosteric modulator; Functional selectivity; mGlu receptor; metabotropic glutamate receptor; CHO; Chinese Hamster Ovary; DHFR(â); Dihydrofolate Reductase; DMSO; Dimethyl Sulfoxide; GPCR; G-Protein-Coupled Receptor; 7TMR;
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators
Keywords: مدولاتور آلوده کننده; CIZDIEPYKQXGQG-UHFFFAOYSA-N; OFNVYYXEOJUGRH-UHFFFAOYSA-N; SONLNLJEFBMKGV-UHFFFAOYSA-N; Metabotropic glutamate receptor; mGluR5; Allosteric modulator; Scaffold hopping; AFQ-056;
Discovery, synthesis, and structure–activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators
Keywords: مدولاتور آلوده کننده; Metabotropic glutamate receptor; mGluR5; Allosteric modulator; Virtual screening; l-DOPA induced dyskinesia
Identification of an allosteric modulator of the serotonin transporter with novel mechanism of action
Keywords: مدولاتور آلوده کننده; Allosteric modulator; Hybrid structure based method; Monoamine transporters; Molecular dynamics; Psychostimulants; Virtual screeningANOVA, analysis of variance; ATM, allosteric transporter modulator; D-PBS, Dulbecco phosphate-buffered saline; EL, extracel
Structure-activity relationships for allosteric NMDA receptor inhibitors based on 2-naphthoic acid
Keywords: مدولاتور آلوده کننده; NMDA receptors; Glutamate; Allosteric modulator; Antagonist; Oocyte;
Orthosteric and allosteric drug binding sites in the Caenorhabditis elegans mgl-2 metabotropic glutamate receptor
Keywords: مدولاتور آلوده کننده; Allosteric modulator; Calcium-sensing receptor; Family C; MPEP; Pharmacophore; Phylogenetic; Venus flytrap;
Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotype
Keywords: مدولاتور آلوده کننده; Glutamate; mGluR5; Allosteric modulator; PAM; NAM; Efficacy switching
The synthesis and biological evaluation of 2-amino-4,5,6,7,8,9-hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor
Keywords: مدولاتور آلوده کننده; Allosteric modulator; A1 adenosine receptor (A1-AR); 2-Amino-3-benzoylthiophene; G protein-coupled receptors (GPCRs)
Fused heterocyclic M1 positive allosteric modulators
Keywords: مدولاتور آلوده کننده; Muscarinic; Alzheimer’s; Allosteric modulator
Opposing roles of mGluR8 in measures of anxiety involving non-social and social challenges
Keywords: مدولاتور آلوده کننده; Metabotropic; Group-III mGluR; Allosteric modulator; Zero maze; Acoustic startle; Social interaction
Structure based evolution of a novel series of positive modulators of the AMPA receptor
Keywords: مدولاتور آلوده کننده; AMPA receptor; Allosteric modulator; SBDD; Indane; Scaffold hopping
In vitro neuropharmacological evaluation of penitrem-induced tremorgenic syndromes: Importance of the GABAergic system
Keywords: مدولاتور آلوده کننده; Penitrem A; Allosteric modulator; GABAergic system; Convulsant
Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator
Keywords: مدولاتور آلوده کننده; Metabotropic glutamate receptor 5; mGlu5; Allosteric modulator; Schizophrenia
Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay
Keywords: مدولاتور آلوده کننده; Melanocortin-4 receptor; MC4R; cAMP assay; Allosteric modulator; High throughput screen
The complexity of their activation mechanism opens new possibilities for the modulation of mGlu and GABAB class C G protein-coupled receptors
Keywords: مدولاتور آلوده کننده; Dimerization; Allosteric communication; Allosteric modulator; Calcium sensing receptor; Taste receptor
Allosteric modulation of G protein-coupled receptors: A pharmacological perspective
Keywords: مدولاتور آلوده کننده; Allosteric modulator; Drug discovery; Functional selectivity; G protein-coupled receptor; Stimulus-bias; Structure–function
Allosteric modulation of metabotropic glutamate receptors: Structural insights and therapeutic potential
Keywords: مدولاتور آلوده کننده; Allosteric modulator; Chimeric receptors; G protein-coupled receptors; Neuromodulation; Site-directed mutagenesis; Homology modelADX47273, S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]oxadiazol-5-yl]-piperidin-1-yl}-methanone; AMN082, N,N’-Bis(diphe
A novel series of positive modulators of the AMPA receptor: Discovery and structure based hit-to-lead studies
Keywords: مدولاتور آلوده کننده; AMPA receptor; Allosteric modulator; SBDD; Hit-to-lead
The identification of novel orally active mGluR5 antagonist GSK2210875
Keywords: مدولاتور آلوده کننده; mGluR; mGluR5; Brain free fraction; Negative allosteric modulator; Allosteric modulator; GPCR; Family C GPCR; Metabotropic glutamate receptor
The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core
Keywords: مدولاتور آلوده کننده; Calcimimetic; Allosteric modulator