234 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Synthesis and biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents.
University of Pavia
Rigidity versus Flexibility: Is This an Issue ins1 Receptor Ligand Affinity and Activity?
University of M£Nster
Tetrahydroprotoberberine alkaloids with dopamine ands receptor affinity.
City University of New York
Development of sigma-1 (s1) receptor fluorescent ligands as versatile tools to studys1 receptors.
Universit£
Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.
City University of New York
Novel 1-(2-aryl-2-adamantyl)piperazine derivatives with antiproliferative activity.
University of Athens
Synthesis and structure-activity relationship study of a new series of selectives(1) receptor ligands for the treatment of pain: 4-aminotriazoles.
Esteve
Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands.
University of Lille
Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.
Northwestern University
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University of Missouri
Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.
University of Lille
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues ass2 receptor ligands.
Washington University
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
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
University of Missouri
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
Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).
National Institute of Mental Health
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
Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.
Universit£
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
Glaxosmithkline
New combination of pharmacophoric elements of potents1 ligands: design, synthesis ands receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes.
Universit£T M£Nster
Discovery of ML314, a Brain Penetrant Non-Peptidic?-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Sanford-Burnham Medical Research Institute
Synthesis and in vivo evaluation of [(18)F]2-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)-dione ([(18)F]FECUMI-101) as an imaging probe for 5-HT1A receptor agonist in nonhuman primates.
Columbia University Medical Center
Synthesis and biological evaluation of Esaprazole analogues showings1 binding and neuroprotective properties in vitro.
Nensius Research
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
Broad Institute of Mit and Harvard
Synthesis and evaluation of novel (18)F-labeled spirocyclic piperidine derivatives ass1 receptor ligands for positron emission tomography imaging.
Key Laboratory of Radiopharmaceuticals Beijing Normal University
Synthesis and biological evaluation of a new series of hexahydro-2H-pyrano[3,2-c]quinolines as novel selectives1 receptor ligands.
Esteve
Design and synthesis of new bifunctional sigma-1 selective ligands with antioxidant activity.
University of Catania
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.
University of North Carolina
Spiropiperidines as high-affinity, selective sigma ligands.
Merck Sharp and Dohme Research Laboratories
Benz[f]isoquinoline analogues as high-affinity sigma ligands.
Merck Sharp and Dohme Research Laboratories
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
Universit£
New adamantane phenylalkylamines withs-receptor binding affinity and anticancer activity, associated with putative antagonism of neuropathic pain.
National and Kapodistrian University of Athens
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research and Development
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
TBA
Synthesis and biological evaluation of the 1-arylpyrazole class ofs(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Esteve
Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents.
Sk Biopharmaceuticals
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
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
National Institute of Mental Health
Synthesis,s1,s2-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes.
National and Kapodistrian University of Athens
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.
Ono Pharmaceutical
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
University of Innsbruck
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
Universit£
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.
Nida-Irp
Synthesis of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites.
Universit£
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.
Pharmazeutisches Institut Der Universit£T Freiburg
Synthesis of (+)-cis-N-(4-isothiocyanatobenzyl)-N-normetazocine, an isothiocyanate derivative of N-benzylnormetazocine as acylant agent for the sigma(1) receptor.
University of Catania
Current and novel approaches to the drug treatment of schizophrenia.
Merck Sharp and Dohme Research Laboratories
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.
Warner-Lambert
Synthesis and SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover sigma(1) ligands.
Taisho Pharmaceutical
Mixture-based synthetic combinatorial libraries.
Torrey Pines Institute For Molecular Studies
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.
National Taiwan University
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
University of Catania
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.
Cooperation Pharmaceutique Fran�Aise
Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers.
Cambridge Neuroscience
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
National Institute of Diabetes and Digestive and Kidney Diseases
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
Universit£
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
Hoechst-Roussel Pharmaceuticals
Synthesis and sigma binding properties of 2'-substituted 5,9 alpha-dimethyl-6,7-benzomorphans.
Research Triangle Institute
Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties.
Virginia Commonwealth University
A new approach to the design of sigma-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1- pyrrolidinyl)ethylamine-related polyamines at sigma-1 and sigma-2 receptor subtypes.
National Institutes of Diabetes and Digestive and Kidney Diseases
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
Albany Molecular Research
Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and pharmacological evaluation of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for a novel receptor with sigma-like neuromodulatory activity.
University of North Carolina
Synthesis and evaluation of conformationally restricted N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamines at sigma receptors. 2. Piperazines, bicyclic amines, bridged bicyclic amines, and miscellaneous compounds.
National Institute of Diabetes and Digestive and Kidney Diseases
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
National Institute On Drug Abuse
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
Bristol-Myers Squibb
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.
National Institute of Diabetes and Digestive and Kidney Diseases
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.
Virginia Commonwealth University
Identification and exploitation of the sigma-opiate pharmacophore.
Virginia Commonwealth University
Synthesis and structure-activity relationships of N,N'-di-o-tolylguanidine analogues, high-affinity ligands for the haloperidol-sensitive sigma receptor.
University of Oregon
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes.
National Institute of Diabetes and Digestive and Kidney Diseases
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.
Pfizer
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
National Institute of Digestive
Synthesis of potent sigma-1 receptor ligands via fragmentation of dextromethorphan.
Ucb Pharma
Trishomocubanes, a new class of selective and high affinity ligands for the sigma binding site
TBA
(5S)-3-aryl-5-(1-piperidinylmethyl)-2-oxazolidinones, a new class of potential neuroleptics with a high affinity for sigma receptors
TBA
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
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.
The University of Mississippi
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.
Glaxosmithkline
Synthesis and SAR studies of chiral non-racemic dexoxadrol analogues as uncompetitive NMDA receptor antagonists.
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
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
Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling.
University of Sydney
An aromatic moiety is not essential for pharmacophore binding to sigma binding sites: Synthesis of N-alkylazacycloheptane derivatives as potent sigma ligands
TBA
Synthesis and evaluation of n-substituted 1-(5-fluoro-2-pyrimidinyl)piperazine derivatives as potential anti-ischemic agents
TBA
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
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Merck Research Laboratories
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
National Institute of Mental Health
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
Preparation of novel analogs of 2-arylpiperidines and evaluation of their sigma receptor binding affinities.
University of Texas At Austin
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College of Physicians and Surgeons
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.
Université
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2.
Université
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
Universit£
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
University of Trieste
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
Beijing Normal University
Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress.
Guizhou Medical University
Structure-Activity Studies of 1
National Institute of Diabetes and Digestive and Kidney Diseases
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Fluoroalkylation of Dextromethorphan Improves CNS Exposure and Metabolic Stability.
The University of Kansas
Propionamide Derivatives as Dual ?-Opioid Receptor Agonists and ?
Esteve Pharmaceuticals
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity.
Università
Thioxanthene-derived analogs as sigma(1) receptor ligands.
Virginia Commonwealth University
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M
Vanderbilt University
Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
Wake Forest University School of Medicine
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of Heterocyclic P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
The State University of New Jersey
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain.
Huazhong University of Science and Technology
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.
Università
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
Soochow University
Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands.
Université
Negative allosteric modulators of the GluN2B NMDA receptor with phenylethylamine structure embedded in ring-expanded and ring-contracted scaffolds.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Sigma-1 and Sigma-2 Receptor Modulators as Potential Therapeutics for Alzheimer's Disease.
Usona Institute
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Pharmazeutisches Institut Der UniversitäT Freiburg
Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands.
Wake Forest University School of Medicine
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu
Vanderbilt University
Exploration of Alternative Scaffolds for P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
Wake Forest University School of Medicine
Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents.
University of Modena and Reggio Emilia
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.
East China Normal University
A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays.
University of Maryland
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Asymmetric synthesis of 9-alkyl-2-benzyl-6,7-benzomorphans: characterization as novel sigma receptor ligands.
Research Triangle Institute
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A
Medical College of Wisconsin
Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.
University of Minnesota
Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.
Northwestern University
New analogs of SYA013 as sigma-2 ligands with anticancer activity.
Florida A&M University
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina At Chapel Hill
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety.
Universit£T M£Nster
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
Centro De InvestigacióN Grupo Ferrer
Combinatorial chemistry: from peptides and peptidomimetics to small organic and heterocyclic compounds.
Institute For Molecular Studies
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual ?-Opioid Receptor Agonists and ?
Esteve Pharmaceuticals
Characterization of novel N,N'-disubstituted piperazines as sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents.
The George Washington University Medical Center
Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.
Wake Forest University School of Medicine
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
University of Camerino
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
University of Louvain
N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters.
University of Minnesota
Halogenated 4-(phenoxymethyl)piperidines as potential radiolabeled probes for sigma-1 receptors: in vivo evaluation of [123I]-1-(iodopropen-2-yl)-4-[(4-cyanophenoxy)methyl]pip eri dine.
Ansto
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
National Institute of Diabetes and Digestive and Kidney Diseases
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Synthesis and evaluation of aryl-substituted N-(arylethyl)-N-methyl-2-(1-pyrrolidinyl)ethylamines and corresponding arylacetamides for sigma receptor affinity.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and in vitro evaluation of 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: high-affinity ligands for the N,N'-di-o-tolylguanidine-labeled sigma binding site.
Scios Nova
Synthesis and structure-activity studies of N,N'-diarylguanidine derivatives. N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: a new, selective noncompetitive NMDA receptor antagonist.
Cambridge Neuroscience
Structural features important for sigma 1 receptor binding.
Virginia Commonwealth University
Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells.
George Washington University Medical Center
A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.
National Taiwan University
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
Warner-Lambert
N-(1-arylpropionyl)-4-aryltetrahydropyridines, a new class of high-affinity selective sigma receptor ligands.
New York University
(+)-cis-N-(para-, meta-, and ortho-substituted benzyl)-N-normetazocines: synthesis and binding affinity at the [3H]-(+)-pentazocine-labeled (sigma 1) site and quantitative structure-affinity relationship studies.
Research Triangle Institute
Preparation of 18F-labeled muscarinic agonist with M2 selectivity.
National Institutes of Health
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.
Università
Synthesis and sigma binding properties of 1'- and 3'-halo- and 1',3'-dihalo-N-normetazocine analogues.
Research Triangle Institute
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Qbi Covid-19 Research Group (Qcrg)
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
Glaxosmithkline
Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.
Guangdong Medical University
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
Iqog, Csic
Synthesis and pharmacological evaluation of benzamide derivatives as potent and selective sigma-1 protein ligands.
Universities of Lille
?-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.
Friedrich-Alexander University Erlangen-N£Rnberg
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.
Pfizer
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.
Harvard Medical School
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.
Virginia Commonwealth University
Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines.
Institutions
Synthesis, configuration, and activity of isomeric 2-phenyl-2-(N-piperidinyl)bicyclo[3.1.0]hexanes at phencyclidine and sigma binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methylethylenediam ines as sigma receptor ligands. 1. Pyrrolidine, piperidine, homopiperidine, and tetrahydroisoquinoline classes.
National Institute of Diabetes and Digestive and Kidney Diseases
Reevaluation of fenpropimorph as a? receptor ligand: Structure-affinity relationship studies at human?
Virginia Commonwealth University
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.
Drexel University College of Medicine
Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the sigma receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
YM90K: pharmacological characterization as a selective and potent alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor antagonist.
Yamanouchi Pharmaceutical
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.
Gsk