123 articles for thisTarget
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The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Virginia Commonwealth University
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s
University Of Catania
Norbenzomorphan Scaffold: Chemical Tool for Modulating Sigma Receptor-Subtype Selectivity.
The University Of Texas At Austin
Synthesis and biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents.
University Of Pavia
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University Of Kansas
Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines.
University Of Pavia
Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.
National Institute On Drug Abuse
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.
Icahn School Of Medicine At Mount Sinai
Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.
University Of Trieste
Oxa-Pictet-Spengler reaction as key step in the synthesis of novels receptor ligands with 2-benzopyran structure.
Universit£T M£Nster
Rigidity versus Flexibility: Is This an Issue ins1 Receptor Ligand Affinity and Activity?
University Of M£Nster
One-pot synthesis and sigma receptor binding studies of novel spirocyclic-2,6-diketopiperazine derivatives.
University Of Tehran
Synthesis and Biological Evaluation of Novels1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones.
Huazhong University Of Science And Technology
Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and biological evaluation of novel 6,7-dihydro-5H-cyclopenta[d]pyrimidine and 5,6,7,8-tetrahydroquinazoline derivatives as sigma-1 (s1) receptor antagonists for the treatment of pain.
Renmin Hospital Of Wuhan University
Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives.
Universit£
Development of sigma-1 (s1) receptor fluorescent ligands as versatile tools to studys1 receptors.
Universit£
Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists ors1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.
Universit£
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.
Washington University
Synthesis and evaluation of tetrahydroindazole derivatives as sigma-2 receptor ligands.
Guangdong Medical College
Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
University Of Trieste
Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.
Universit£
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted¿-opioid receptor agonists.
Westf£Lische Wilhelms-Universit£T M£Nster
Pyridine analogues of spirocyclics1 receptor ligands.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Ether modifications to 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine (SA4503): effects on binding affinity and selectivity for sigma receptors and monoamine transporters.
University Of Missouri
Deconstruction of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline moiety to separate P-glycoprotein (P-gp) activity froms2 receptor affinity in mixed P-gp/s2 receptor agents.
Universit£
From mixed sigma-2 receptor/P-glycoprotein targeting agents to selective P-glycoprotein modulators: small structural changes address the mechanism of interaction at the efflux pump.
Universit£
Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain.
Huazhong University Of Science And Technology
Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane baseds1 receptor ligands.
University Of Trieste
Combination of cyclohexane and piperazine based¿-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues ass2 receptor ligands.
Washington University
Novel derivatives of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with improved fluorescent ands receptors binding properties.
Universit£
Synthesis, pharmacological evaluation, ands1 receptor interaction analysis of hydroxyethyl substituted piperazines.
University Of M£Nster
Thes2 receptor: a novel protein for the imaging and treatment of cancer.
Washington University
Synthesis and biological evaluation of a novel sigma-1 receptor antagonist based on 3,4-dihydro-2(1H)-quinolinone scaffold as a potential analgesic.
Huazhong University Of Science And Technology
Involvement of apoptosis and autophagy in the death of RPMI 8226 multiple myeloma cells by two enantiomeric sigma receptor ligands.
University Of Greifswald
Structure of thes1 receptor and its ligand binding site.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Design, synthesis and receptor affinity of novel conformationally restricteds ligands based on the [4.3.3]propellane scaffold.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging ofs2 receptors.
Universit£
New combination of pharmacophoric elements of potents1 ligands: design, synthesis ands receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes.
Universit£T M£Nster
2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.
Virginia Commonwealth University
Structure activity relationship study of benzo[d]thiazol-2(3H)one baseds receptor ligands.
University Of Mississippi
Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter.
Washington University
Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class ofs1 ligands.
Nstri
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
Ucl School Of Pharmacy
Improvement ofs1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones.
Wilhelms-Universit£T M£Nster
Investigation ofs receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines.
Universit£
3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (s1) receptor.
Northeast Ohio Medical University
Design and synthesis of new bifunctional sigma-1 selective ligands with antioxidant activity.
University Of Catania
Enantiomerically pure 1,3-dioxanes as highly selective NMDA ands1 receptor ligands.
Westf£Lische Wilhelms-Universit£T M£Nster
Pd-catalyzed direct C-H bond functionalization of spirocyclics1 ligands: generation of a pharmacophore model and analysis of the reverse binding mode by docking into a 3D homology model of thes1 receptor.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Exploration of ring size in a series of cyclic vicinal diamines withs1 receptor affinity.
The University Of Sydney
Thiophene bioisosteres of spirocyclics receptor ligands: relationships between substitution pattern ands receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
Washington University
Microwave assisted synthesis of spirocyclic pyrrolidines -s1 receptor ligands with modified benzene-N-distance.
Institut F£R Pharmazeutische Und Medizinische Chemie
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with highs1 receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Arylamides hybrids of two high-affinitys2 receptor ligands as tools for the development of PET radiotracers.
Universit£
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
Washington University
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Wilhelms-Universit£T M£Nster
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
University Of Minnesota
Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety.
Institut F£R Pharmazeutische Und Medizinische Chemie
Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28).
Universita Degli Studi Di Bari
Relationships between the structure of 6-substituted 6,8-diazabicyclo[3.2.2]nonan-2-ones and their sigma receptor affinity and cytotoxic activity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol.
National Institute On Drug Abuse-Intramural Research Program
Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity.
Universita Degli Studi Di Bari
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure.
Westf£Lische Wilhelms-Universit£T M£Nster
Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.
University Of Missouri-Columbia
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
University M£Nster
Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.
Universit£
Synthesis of bridged piperazines with sigma receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie
Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor.
Universit£
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for centrals1 receptors and comparison with fluoroalkyl homologs.
Institute Of Radiopharmacy
Synthesis and biological characterization of 3-substituted-1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors.
Universit£
Synthesis and binding assays of novel 3,3-dimethylpiperidine derivatives with various lipophilicities ass¿? receptor ligands.
Universit£
Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.
University Of Pavia
Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novels1 receptor PET imaging agent.
The University Of Sydney
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.
The University Of Sydney
Fluorescent derivatives ofs receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) as a tool for uptake and cellular localization studies in pancreatic tumor cells.
Universita` Degli Studi Di Bari Aldo Moro
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues fors1 receptors.
Washington University
Synthesis and characterization of selective dopamine D2 receptor ligands using aripiprazole as the lead compound.
Washington University
Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis of 4-(aminoalkyl) substituted 1,3-dioxanes as potent NMDA ands receptor antagonists.
Westf£Lischen Wilhelms-Universit£T M£Nster
Design, synthesis and pharmacological evaluation of spirocyclics(1) receptor ligands with exocyclic amino moiety (increased distance 1).
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Novel potent and selectives ligands: evaluation of their agonist and antagonist properties.
University Of Catania
Synthesis and pharmacological evaluation of fluorine-containing D3 dopamine receptor ligands.
Washington University
Effect of structural modification in the amine portion of substituted aminobutyl-benzamides as ligands for bindings1 ands2 receptors.
University Of Missouri-Columbia
Analogues ofs receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with added polar functionality and reduced lipophilicity for potential use as positron emission tomography radiotracers.
Universita` Degli Studi Di Bari Aldo Moro
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
University Of Catania
Synthesis, pharmacological activity and structure affinity relationships of spirocyclics(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols.
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
Synthesis and resolution of cis-(+/-)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [(+/-)-PPCC)]: new sigma receptor ligands with neuroprotective effect.
University Of Catania
5D-QSAR for spirocyclic sigma1 receptor ligands by Quasar receptor surface modeling.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and characterization of N,N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derived compounds as high affinity ligands for sigma receptors.
University Of Wisconsin School Of Medicine And Public Health
Synthesis and NMDA receptor affinity of fluorinated dioxadrol analogues.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhems-Universit£T M£Nster
Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
Washington University
Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability.
Institut FüR Pharmazeutische Und Medizinische Chemie Der UniversitäT MüNster
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
Institut Fur Pharmazeutische Und Medizinische Chemie Der Westfalischen Wilhelms-Universitat Munster
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
Washington University
Relationships between the structure of 6-allyl-6,8-diazabicyclo[3.2.2]nonane derivatives and their sigma receptor affinity and cytotoxic activity.
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
Thiophene bioisosteres of spirocyclic sigma receptor ligands. 1. N-substituted spiro[piperidine-4,4'-thieno[3,2-c]pyrans].
Institut FüR Pharmazeutische And Medizinische Chemie Der UniversitäT MüüNster
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
Institut FüR Pharmazeutische Und Medizinische Chemie
Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma.
Radiopharmaceuticals Research Institute
Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography.
Washington University
Synthesis and in vitro evaluation of tetrahydroisoquinolinyl benzamides as ligands for sigma receptors.
University Of Missouri-Columbia
Rapid synthesis of flavone-based monoamine oxidase (MAO) inhibitors targeting two active sites using click chemistry.
Zhejiang University Of Technology
One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.
University Of Karachi
2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket.
Boehringer Ingelheim Pharmaceuticals