Keywords: انتخاب انتخابی زیر; Adenosine receptor; Docking; Homology modeling; Purine-2,6-dione; Species differences; Subtype selectivity; Xanthines
مقالات ISI انتخاب انتخابی زیر (ترجمه نشده)
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Keywords: انتخاب انتخابی زیر; κ-Hefutoxin 1; Voltage-gated potassium channel; Scorpion toxin; Synthetic analogs; Amino acid deletion; Subtype selectivity; Acm; acetamidomethyl; CD; circular dichroism; Fmoc; 9-fluorenylmethoxycarbonyl; Hef-1; κ-hefutoxin 1; MALDI-TOF-MS; matrix assis
Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1P5 receptor agonist chemotype
Keywords: انتخاب انتخابی زیر; S1P5 receptor agonists; Subtype selectivity; Spirocyclic scaffold; Molecular modelling; Homology model; Oral bioavailability; Turbidimetric aqueous solubility; Microsomal stability; Membrane permeation;
Design and synthesis of iodocarborane-containing ligands with high affinity and selectivity toward ERβ
Keywords: انتخاب انتخابی زیر; Carborane; Estrogen receptor; ERβ; Subtype selectivity;
Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior
Keywords: انتخاب انتخابی زیر; Dopamine D3 receptor; Selective D3 antagonist; Subtype selectivity; Positron emission tomography (PET); Fluorine-18; Autoradiography; Self-administration; Drug maintained behavior; Food maintained behavior;
Molecular and cellular pharmacologyCharacterization of PCS1055, a novel muscarinic M4 receptor antagonist
Keywords: انتخاب انتخابی زیر; Muscarinic M4 receptors; Competitive antagonists; PCS1055; Subtype selectivity;
Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands
Keywords: انتخاب انتخابی زیر; Magnolol; Honokiol; Cross-coupling; GABAA; Subtype selectivity;
Design and synthesis of carborane-containing estrogen receptor-beta (ERβ)-selective ligands
Keywords: انتخاب انتخابی زیر; Carborane; Estrogen receptor; Subtype selectivity; Docking study;
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH
Keywords: انتخاب انتخابی زیر; α1-ARs; Subtype selectivity; Arylpiperazine derivatives; Antagonic activity; Homology modeling; Structure-activity relationship;
Structural insights into ligand recognition and selectivity for classes A, B, and C GPCRs
Keywords: انتخاب انتخابی زیر; GPCR structure; GPCR subtype; X-ray crystallography; Ligand recognition; Subtype selectivity;
1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation
Keywords: انتخاب انتخابی زیر; 3D-QSAR; D2 partial agonist; CoMFA; CoMSIA; GPCR; Subtype selectivity; 5-HT2A/D2 selectivity; Dopamine receptor; Serotonin receptor; Phenylpiperazine; 1,4-DAP
Enhanced estrogen receptor beta (ERβ) selectivity of fluorinated carborane-containing ER modulators
Keywords: انتخاب انتخابی زیر; Carborane; Estrogen receptor; Fluorine; Subtype selectivity;
Discovery of dopamine D4 receptor antagonists with planar chirality
Keywords: انتخاب انتخابی زیر; GPCR; Dopamine; Subtype selectivity; Ligand efficacy; Paracyclophane; Planar chirality;
The effect of absolute configuration on activity, subtype selectivity (M3/M2) of 3α-acyloxy-6β-acetoxyltropane derivatives as muscarinic M3 receptor antagonists
Keywords: انتخاب انتخابی زیر; Tropane derivative; 6S Configuration; Muscarinic antagonist; Enantiomer; Subtype selectivity
α1-Adrenoceptor and serotonin 5-HT1A receptor affinity of homobivalent 4-aminoquinoline compounds: An investigation of the effect of linker length
Keywords: انتخاب انتخابی زیر; GPCR; α1-Adrenergic receptor; Subtype selectivity; Serotonin receptor; Diquinoline; Linker length
Identification of structural determinants of ligand selectivity in 5-HT2 receptor subtypes on the basis of protein–ligand interactions
Keywords: انتخاب انتخابی زیر; 5-HT2 receptor; Subtype selectivity; Homology modeling; Protein–ligand docking; Molecular dynamic simulation
Bivalent molecular probes for dopamine D2-like receptors
Keywords: انتخاب انتخابی زیر; GPCR; Subtype selectivity; Dopamine; Bivalent ligand; D3 receptor;
Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor
Keywords: انتخاب انتخابی زیر; GABAA ligands; Subtype selectivity; Metabolic stability
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonists
Keywords: انتخاب انتخابی زیر; Dipeptidyl peptidase IV; Enzyme inhibitor; Phthalimide; Non-competitive inhibition; Subtype selectivity
New 2-thioether-substituted apomorphines as potent and selective dopamine D2 receptor agonists
Keywords: انتخاب انتخابی زیر; Apomorphine derivatives; Parkinson’s disease; Structure–activity relationship; Dopamine receptor activity; Subtype selectivity
Structure based prediction of subtype-selectivity for adenosine receptor antagonists
Keywords: انتخاب انتخابی زیر; GPCR; G protein-coupled receptor; Adenosine receptor; Subtype selectivity; Homology modeling; Ligand docking; Conformational sampling; Structure based drug discoveryGPCR, G protein-coupled receptor; AR, adenosine receptor; A2AAR, subtype A2A; TM, transmem
Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: Relationship between absolute configuration and subtype selectivity
Keywords: انتخاب انتخابی زیر; PPAR agonist; Molecular design; Nuclear receptor; Subtype selectivity
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs)
Keywords: انتخاب انتخابی زیر; Histone deacetylase (HDAC); Class I and II HDAC inhibitor; Hydroxamic acid; Subtype selectivity; Gold docking
Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern
Keywords: انتخاب انتخابی زیر; Cannabinoid CB1 receptor; Site of metabolism prediction; Metasite; Rimonabant; Subtype selectivity; Polar surface area; Lipophilicity; P-Glycoprotein
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies
Keywords: انتخاب انتخابی زیر; Binding efficiency index; Ligand efficiency; Cannabinoid CB2 receptor; Inverse agonist; Polar surface area; Lipophilicity; Subtype selectivity; Ligand-lipophilicity efficiency; Lipophilic efficiency
GABAA receptor subtype selectivity underlying anxiolytic effect of 6-hydroxyflavone
Keywords: انتخاب انتخابی زیر; GABAA receptor; Benzodiazepine; Flavonoids; 6-Hydroxyflavone; Subtype selectivity
Pharmacological characterization of (4R)-alkyl glutamate analogues at the ionotropic glutamate receptors — Focus on subtypes iGlu5–7
Keywords: انتخاب انتخابی زیر; Glutamate receptor; Kainate receptor; Subtype selectivity; iGlu5; iGlu6; iGlu7
Newly developed PPAR-α agonist (R)-K-13675 inhibits the secretion of inflammatory markers without affecting cell proliferation or tube formation
Keywords: انتخاب انتخابی زیر; PPAR-α agonist; Subtype selectivity; Inflammatory markers; Cell proliferation; Tube formation;
Molecular modelling of subtypes (α2A, α2B and α2C) of α2-adrenoceptors: A comparative study
Keywords: انتخاب انتخابی زیر; α2-Adrenoceptor; Subtype selectivity; Homology modelling; Docking; Binding free energy; AutoDock
Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide
Keywords: انتخاب انتخابی زیر; Muscarinic receptors; Muscarinic agonists; 1,4-Dioxane nucleus; Subtype selectivity; Receptor enantioselectivity; Stereoselective synthesis
Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas
Keywords: انتخاب انتخابی زیر; Muscarinic acetylcholine receptor antagonists; M3 mAChR; SAR; Subtype selectivity; COPD; Asthma; Tyrosine ureas
Flavan-3-ol derivatives are positive modulators of GABAA receptors with higher efficacy for the α2 subtype and anxiolytic action in mice
Keywords: انتخاب انتخابی زیر; GABAA; Flavan-3-ol; Anxiolysis; Sedation; Subtype selectivity
Novel discriminative stimulus effects of TPA023B, subtype-selective γ-aminobutyric-acidA/benzodiazepine modulator: Comparisons with zolpidem, lorazepam, and TPA023
Keywords: انتخاب انتخابی زیر; GABA; Subtype selectivity; Anxiolytic; Drug discrimination; Abuse liability; Benzodiazepine; Lorazepam; Zolpidem; TPA023; TPA023B; Training; Rat;
Quantitative structure-selectivity relationship for M2 selectivity between M1 and M2 of piperidinyl piperidine derivatives as muscarinic antagonists
Keywords: انتخاب انتخابی زیر; QSSR; CoMFA; Muscarinic antagonists; Subtype selectivity;
6,2′-Dihydroxyflavone, a subtype-selective partial inverse agonist of GABAA receptor benzodiazepine site
Keywords: انتخاب انتخابی زیر; GABAA receptor; 6,2′-Dihydroxyflavone; Subtype selectivity; Anxiogenesis; Proconvulsant
Dioxane and oxathiane nuclei: Suitable substructures for muscarinic agonists
Keywords: انتخاب انتخابی زیر; Muscarinic agonists; Subtype selectivity; 1,4-Dioxane nucleus; 1,4-Oxathiane nucleus
Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype
Keywords: انتخاب انتخابی زیر; Dopamine; D4; Partial agonist; Regioselective synthesis; Subtype selectivity
GABAA receptor subtypes as targets for neuropsychiatric drug development
Keywords: انتخاب انتخابی زیر; GABAA receptor subtypes; Subtype selectivity; Intrinsic activity; Extrasynaptic receptors; Alcoholism; AnxietyBPAD, bipolar affective disorder; COGA, The Collaborative Study on the Genetics of Alcoholism; GABA, γ-aminobutyric acid; SNP, single nucleotide
NMDA-NR2B subtype selectivity of stereoisomeric 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives
Keywords: انتخاب انتخابی زیر; NMDA; Subtype selectivity; Isoquinolines; NMDA-NR2B; Enantiomers; Ifenprodil binding site;
Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4
Keywords: انتخاب انتخابی زیر; Murine GABA transporter (mGAT1-4); GABA (γ-aminobutyric acid) uptake; Structure activity relationship; Subtype selectivity;
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs
Keywords: انتخاب انتخابی زیر; Osteoporosis; Estrogen receptor; Chromane; Subtype selectivity; Estrogen receptor alpha; SERM; SERAM; Estrogen receptor antagonist; Cancer;
Muscarinic subtype affinity and functional activity profile of 1-methyl-2-(2-methyl-1,3-dioxolan-4-yl)pyrrolidine and 1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine derivatives
Keywords: انتخاب انتخابی زیر; Muscarinic agonist; Subtype selectivity; Dioxolane derivative; Oxathiolane derivative; Binding studies; Functional studies; CHO; Chinese hamster ovary; hm1-hm5; human muscarinic subtypes; M1-M5; muscarinic subtypes; Ki; inhibitor equilibrium dissociat