319 articles for thisTarget
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Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
National Institute Of Diabetes And Digestive And Kidney Diseases
Design, synthesis and in vitro activity of 1,4-disubstituted piperazines and piperidines as triple reuptake inhibitors.
Chonnam National University
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.
The University Of Newcastle
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University Of Kansas
Polycyclic Polyprenylated Acylphloroglucinol Congeners from Hypericum scabrum.
Chinese Academy Of Medical Sciences And Peking Union Medical College
Design, synthesis, and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitors - Part 3.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of arylpiperazine-benzylpiperidines with dual serotonin and norepinephrine reuptake inhibitory activities.
Chonnam National University
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Emerging targets and new small molecule therapies in Parkinson's disease treatment.
School Of Medicine Of University Of Electronic Science And Technology Of China
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.
Glenmark Research Centre
Design and synthesis of 4-benzylpiperidine carboxamides as dual serotonin and norepinephrine reuptake inhibitors.
Chonnam National University
Ethylenedioxy homologs of N-methyl-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) and its corresponding cathinone analog methylenedioxymethcathinone: Interactions with transporters for serotonin, dopamine, and norepinephrine.
Virginia Commonwealth University
Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors.
Shanghai Institute Of Pharmaceutical Industry
Design, synthesis and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitor.
Takeda Pharmaceutical
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.
City University Of New York
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.
Amri
Design, synthesis, and biological activities of 1-aryl-1,4-diazepan-2-one derivatives as novel triple reuptake inhibitors.
Takeda Pharmaceutical
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.
Korea University
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram.
National Institute On Drug Abuse-Intramural Research Program
Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists.
University Of Copenhagen
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.
Bristol-Myers Squibb
A rhodamine-labeled citalopram analogue as a high-affinity fluorescent probe for the serotonin transporter.
National Institute On Drug Abuse-Intramural Research Program
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.
Astrazeneca
chi-Conopeptide pharmacophore development: toward a novel class of norepinephrine transporter inhibitor (Xen2174) for pain.
Xenome
Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.
Roche Palo Alto
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.
Abbott Laboratories
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.
Amri
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).
The University Of Sydney
Characterisation of [¹¹C]PR04.MZ in Papio anubis baboon: a selective high-affinity radioligand for quantitative imaging of the dopamine transporter.
Johannes Gutenberg University
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
Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists.
Suven Life Sciences
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.
Korea Institute Of Science And Technology
Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors.
Shanghai Institute Of Pharmaceutical Industry
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.
Florida A&M University
First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain.
Neuraxon
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.
Amgen
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
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.
University Of Namur
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
Cephalon
Nicotinic Acetylcholine Receptor Efficacy and Pharmacological Properties of 3-(Substituted phenyl)-2ß-substituted Tropanes.
Research Triangle Institute
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
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
Aska Pharmaceutical
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
Korea Institute Of Science And Technology
Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomography.
Emory University
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Pfizer
Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores.
Pfizer
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College And The Graduate Center Of The City University Of New York
Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression.
Human Biomolecular Research Institute
Antagonists of the calcium receptor. 2. Amino alcohol-based parathyroid hormone secretagogues.
Glaxosmithkline
Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters.
Research Triangle Institute
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction.
Research Triangle Institute
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.
Wyeth Research
3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors.
Wyeth Research
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
Veterans Affairs Medical Center
2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors.
Human Biomolecular Research Institute
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
Neurocrine Biosciences
Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists.
Emory University
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomography radioligands for in vivo imaging of the norepinephrine transporter.
Emory University
Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression.
Human Biomolecular Research Institute
Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
Wyeth Research
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.
Virginia Commonwealth University
Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.
Wyeth Research
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Neurocrine Biosciences
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Neurocrine Biosciences
Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.
Neurocrine Biosciences
Synthesis and monoamine transporter binding properties of 2beta-[3'-(substituted benzyl)isoxazol-5-yl]- and 2beta-[3'-methyl-4'-(substituted phenyl)isoxazol-5-yl]-3beta-(substituted phenyl)tropanes.
Research Triangle Institute
chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model.
The University Of Queensland
Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives.
Research Triangle Institute
Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity.
Pfizer
[4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors.
Pfizer
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
Neurocrine Bioscience
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.
Neurocrine Bioscience
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.
Neurocrine Bioscience
Synthesis, in vitro characterization, and radiolabeling of reboxetine analogs as potential PET radioligands for imaging the norepinephrine transporter.
Emory University
1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.
Pfizer
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.
University Of Aarhus
Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes.
Research Triangle Institute
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
Research Triangle Institute
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
Massachusetts College Of Pharmacy And Health Sciences
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.
Pfizer
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.
Pfizer
Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction.
Chinese Academy Of Sciences
Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol.
Research Triangle Institute
Discovery of novel and selective tertiary alcohol containing inhibitors of the norepinephrine transporter.
Eli Lilly
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.
Organix
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.
National Institute On Drug Abuse-Intramural Research Program
Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol.
Medical University Of South Carolina
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.
Alcon Research
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
Research Triangle Institute
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Drew University
Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse.
Pharm-Eco Laboratories
Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands.
Massachusetts General Hospital
Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter.
Georgetown University Medical Center
Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors.
Massachusetts General Hospital
TROTEC-1: a new high-affinity ligand for labeling of the dopamine transporter.
Institut F£R Bioanorganische Und Radiopharmazeutische Chemie
Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors.
University Of Michigan
Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes.
Organix
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.
Georgetown University Medical Center
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.
Hong Kong University Of Science And Technology
Discovery of cis-N-(1-(4-(methylamino)cyclohexyl)indolin-6-yl)thiophene-2-carboximidamide: a 1,6-disubstituted indoline derivative as a highly selective inhibitor of human neuronal nitric oxide synthase (nNOS) without any cardiovascular liabilities.
Neuraxon
Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test.
Cephalon
QSAR study and synthesis of new phenyltropanes as ligands of the dopamine transporter (DAT).
University Of Tours
Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.
Research Triangle Institute
Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporter.
Key Laboratory Of Radiopharmaceuticals (Beijing Normal University)
Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-ß2-agonist for the treatment of chronic obstructive pulmonary disease.
Pfizer
Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).
Pfizer
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.
The University Of Mississippi
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.
The University Of Sydney
Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.
Research Triangle Institute
The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).
Astrazeneca Charnwood
Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitor.
Sunovion Pharmaceuticals
Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor.
Sunovion Pharmaceuticals
Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor.
Sunovion Pharmaceuticals
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.
Sepracor
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.
The University Of Sydney
The identification, and optimisation of hERG selectivity, of a mixed NET/SERT re-uptake inhibitor for the treatment of pain.
Msd
Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT(1A) partial agonists.
Pfizer
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Bristol-Myers Squibb
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
Abbott Laboratories
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
National Institute Of Mental Health
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical And Public Health Institute
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B.
Csiro Molecular And Health Technologies
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Barrow Neurological Institute
Synthesis and in vitro toxicity of 4-MTA, its characteristic clandestine synthesis byproducts and related sulfur substituted alpha-alkylthioamphetamines.
Trinity College
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).
Pfizer
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.
Wyeth Research
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
Amgen
Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.
Trinity College
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Pfizer
Synthesis and hSERT activity of homotryptamine analogs. Part 6: [3+2] dipolar cycloaddition of 3-vinylindoles.
Bristol-Myers Squibb
Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
Pfizer
Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands.
University Of Tours
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.
Research Triangle Institute
1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors.
Wyeth Research
Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling.
University Of Sydney
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj
Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.
Pfizer
Discovery of a new series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols.
Wyeth Research
Structure-activity relationships of the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ol series of monoamine reuptake inhibitors.
Wyeth Research
Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
Pfizer
Synthesis of 1,1-[1-naphthyloxy-2-thiophenyl]-2-methylaminomethylcyclopropanes and their evaluation as inhibitors of serotonin, norepinephrine, and dopamine transporters.
Oregon State University
Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.
Pfizer
Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships.
Pfizer
Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.
Sirtris Pharmaceuticals
Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.
Glaxosmithkline
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
National Institute On Drug Abuse-Intramural Research Program
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.
University Of Illinois At Chicago
Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.
Pfizer
Synthesis, radiosynthesis, and biological evaluation of fluorine-18-labeled 2beta-carbo(fluoroalkoxy)-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography.
Emory University
Development of 3-phenyltropane analogues with high affinity for the dopamine and serotonin transporters and low affinity for the norepinephrine transporter.
Research Triangle Institute
Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
Roche Palo Alto
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.
Neurocrine Biosciences
Docking study, synthesis, and in vitro evaluation of fluoro-MADAM derivatives as SERT ligands for PET imaging.
University Of Tours
Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: structure-activity relationships of (thioalkyl)phenoxy benzylamines.
Pfizer
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.
Neurocrine Biosciences
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination.
Institut FüR InterdisziplinäRe Isotopenforschung
N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors.
Pfizer
Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.
Pfizer
Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines.
Pfizer
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.
Wyeth Research
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.
Hadassah Hebrew University Hospital
Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions.
University Of Maryland
Antidepressant principles of the roots of Polygala tenuifolia.
Medical And Pharmaceutical Industry Technology And Development Center
Synthesis and in vivo evaluation of halogenated N,N-dimethyl-2-(2'-amino-4'-hydroxymethylphenylthio)benzylamine derivatives as PET serotonin transporter ligands.
Emory University
2-(2'-((dimethylamino)methyl)-4'-(fluoroalkoxy)-phenylthio)benzenamine derivatives as serotonin transporter imaging agents.
University Of Pennsylvania
High dopamine transporter selectivity can be displayed by remarkably simple non-nitrogen containing inhibitors.
University Of Aarhus
Synthesis and in vivo evaluation of fluorine-18 and iodine-123 labeled 2beta-carbo(2-fluoroethoxy)-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane as a candidate serotonin transporter imaging agent.
Emory University
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
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
Synthesis and biological evaluation of 2beta,3alpha-(substituted phenyl)nortropanes as potential norepinephrine transporter imaging agents.
Emory University
CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity.
Johnson & Johnson Pharmaceutical Research & Development
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.
Pfizer
Synthesis, radiosynthesis, and biological evaluation of carbon-11 labeled 2beta-carbomethoxy-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography.
Emory University
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.
Johnson & Johnson Pharmaceutical Research And Development
Synthesis of 11C-labelled (R)-OHDMI and CFMME and their evaluation as candidate radioligands for imaging central norepinephrine transporters with PET.
Institutet
2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and monoamine transporter affinity of front bridged tricyclic 3beta-(4'-halo or 4'-methyl)phenyltropanes bearing methylene or carbomethoxymethylene on the bridge to the 2beta-position.
Emory University
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Pfizer
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
(R)-sila-venlafaxine: a selective noradrenaline reuptake inhibitor for the treatment of emesis.
Paradigm Therapeutics
Design and synthesis of promiscuous high-affinity monoamine transporter ligands: unraveling transporter selectivity.
Niddk
N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake.
Eli Lilly
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
Evaluation of carbon-11-labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-iodoethenyl)phenyl]nortropane as a potential radioligand for imaging the serotonin transporter by PET.
Emory University
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Alcon Research
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 biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
F. Hoffmann-La Roche
Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands.
University Of Tours
Designing rapid onset selective serotonin re-uptake inhibitors. Part 1: Structure-activity relationships of substituted (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthaleneamine.
Pfizer
Rhodamine-labeled 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)tropane analogues as high-affinity fluorescent probes for the dopamine transporter.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes.
University Of Illinois At Chicago
1-Aryl-3,4-dihydro-1H-quinolin-2-one derivatives, novel and selective norepinephrine reuptake inhibitors.
Eli Lilly
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.
Emory University
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.
Columbia University College Of Physicians And Surgeons
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.
University Of Pennsylvania
Synthesis and biological activity of some known and putative duloxetine metabolites.
Eli Lilly
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).
Virginia Commonwealth University
Synthesis and monoamine transporter affinity of 3'-analogs of 2-beta-carbomethoxy-3-beta-(4'-iodophenyl)tropane (beta-CIT).
Yale School Of Medicine
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.
Emory University
Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake.
Eli Lilly
Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Virginia Commonwealth University
Bicyclo[2.2.1]heptanes as novel triple re-uptake inhibitors for the treatment of depression.
Eli Lilly
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.
Emory University
Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter.
Niddk
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Drew University
Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines.
Centre For Addiction And Mental Health
Exploration of substituted arylpiperazine-tetrazoles as promising dual norepinephrine and dopamine reuptake inhibitors.
Chonnam National University
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.
East China Normal University
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Virginia Commonwealth University
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute Of Neurological Disorders And Stroke
Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.
Georgetown University Medical Center
Norepinephrine-Transporter-Targeted and DNA-Co-Targeted Theranostic Guanidines.
University Of Nebraska Medical Center
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D
University Of Pennsylvania
Structure-Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters.
University Of Vienna
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol.
University Of Pennsylvania
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
Astrazeneca
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons.
Novartis Pharma
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.
National Institute On Drug Abuse
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University Of Minnesota Twin Cities
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Hoechst-Roussel Pharmaceuticals
Synthesis, radiosynthesis and first in vitro evaluation of novel PET-tracers for the dopamine transporter: [(11)C]IPCIT and [(18)F]FE@IPCIT.
Medical University Of Vienna
Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors.
Sogang University
Neuroactive diol and acyloin metabolites from cone snail-associated bacteria.
University Of Utah
Novel triple reuptake inhibitors with low risk of CAD associated liabilities: design, synthesis and biological activities of 4-[(1S)-1-(3,4-dichlorophenyl)-2-methoxyethyl]piperidine and related compounds.
Takeda Pharmaceutical
Conformationally restricted homotryptamines. Part 6: indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors.
Bristol-Myers Squibb Research And Development
A novel class of 3-(phenoxy-phenyl-methyl)-pyrrolidines as potent and balanced norepinephrine and serotonin reuptake inhibitors: synthesis and structure-activity relationships.
Theravance
Cyclic MrIA: a stable and potent cyclic conotoxin with a novel topological fold that targets the norepinephrine transporter.
University Of Queensland
Design, synthesis, and systematic evaluation of 4-arylpiperazine- and 4-benzylpiperidine napthyl ethers as inhibitors of monoamine neurotransmitters reuptake.
Chonnam National University
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.
Texas Tech University Health Sciences Center
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors.
Chonnam National University
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
Csir-National Chemical Laboratory
Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges.
Biocon Bristol-Myers Squibb R&D Centre
Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter.
Organix
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute Of Diabetes And Digestive And Kidney Diseases
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University Of Texas At Austin
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.
Phenex Pharmaceuticals
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.
Chonnam National University
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.
National Institute Of Diabetes And Digestive And Kidney Diseases
Heterocyclic Analogues of Modafinil as Novel, Atypical Dopamine Transporter Inhibitors.
University Of Vienna
Discovery of Novel Allosteric Eg5 Inhibitors Through Structure-Based Virtual Screening.
Southern Research Institute
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.
Chulabhorn Research Institute
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents.
University Of Wisconsin-Madison
Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA.
The Royal Danish School Of Pharmacy
Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Janssen Research Foundation
Pharmacological properties of two recombinant splice variants of the PACAP type I receptor, transfected and stably expressed in CHO cells.
UniversitÉ
Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.
Washington University
CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo.
Celera Genomics
Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.
Methylgene