259 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
Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.
National Institute On Drug Abuse
Lobelane analogues containing 4-hydroxy and 4-(2-fluoroethoxy) aromatic substituents: Potent and selective inhibitors of [(3)H]dopamine uptake at the vesicular monoamine transporter-2.
University Of Arkansas For Medical Sciences
Emerging targets and new small molecule therapies in Parkinson's disease treatment.
School Of Medicine Of University Of Electronic Science And Technology Of China
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
Development of potent dopamine-norepinephrine uptake inhibitors (DNRIs) based on a (2S,4R,5R)-2-benzhydryl-5-((4-methoxybenzyl)amino)tetrahydro-2H-pyran-4-ol molecular template.
Wayne State University
Alpha-ethyltryptamines as dual dopamine-serotonin releasers.
Research Triangle Institute
Hybrid dopamine uptake blocker-serotonin releaser ligands: a new twist on transporter-focused therapeutics.
Rti International
Conformationally rigid amphetamine analogs as inhibitors of monoamine uptake by brain synaptosomes.
TBA
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.
Astrazeneca
Characterisation of [¹¹C]PR04.MZ in Papio anubis baboon: a selective high-affinity radioligand for quantitative imaging of the dopamine transporter.
Johannes Gutenberg University
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
H. Lundbeck
A novel spirocyclic tropanyl-¿²-isoxazoline derivative enhances citalopram and paroxetine binding to serotonin transporters as well as serotonin uptake.
Universit£
Wake promoting agents: search for next generation modafinil, lessons learned: part III.
Cephalon
Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues.
National Institute On Drug Abuse-Intramural Research Program
Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.
University Of Kentucky
Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes.
University Of New Orleans
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
Neurocrine Biosciences
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
1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors.
The State University Of New York
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Neurocrine Biosciences
Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an exocyclic hydroxyl group: interaction with dopamine, serotonin, and norepinephrine transporters.
Wayne State University
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
The University Of Mississippi
3-{2-[Bis-(4-fluorophenyl)methoxy]ethyl}-6-substituted-3,6-diazabicyclo[3.1.1]heptanes as novel potent dopamine uptake inhibitors.
Universit£
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate.
Georgia Institute Of Technology
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Janssen-Cilag
Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
National Institute On Drug Abuse-Intramural Research Program
Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction.
Chinese Academy Of Sciences
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.
National Institute On Drug Abuse-Intramural Research Program
The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines.
Wake Forest University Health Sciences
Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter.
Universit£
Synthesis and biological evaluation of meperidine analogues at monoamine transporters.
University Of New Orleans
Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds.
Research Triangle Institute
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
Acenta Discovery
Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine transporters.
Wayne State University
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency.
Yale University
Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring.
University Of Illinois At Chicago
Synthesis and monoamine transporter binding of 2-(diarylmethoxymethyl)-3 beta-aryltropane derivatives.
University Of New Orleans
Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes.
Research Triangle Institute
Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors.
Georgia Institute Of Technology
High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo.
Wayne State University
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
Faes Farma
Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter.
National Institute On Drug Abuse
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
Interaction of cis-(6-benzhydrylpiperidin-3-yl)benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl)piperidin-4-ylmethyl]amine.
Wayne State University
Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites.
Georgetown University Medical Center
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
Research Triangle Institute
Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transporter inhibitors.
Georgetown University Medical Center
Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters.
University Of New Orleans
Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules.
Wayne State University
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Drew University
Synthesis and transporter binding properties of 3beta-[4'-(phenylalkyl, -phenylalkenyl, and -phenylalkynyl)phenyl]tropane-2beta-carboxylic acid methyl esters: evidence of a remote phenyl binding domain on the dopamine transporter.
Research Triangle Institute
SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement.
Georgetown University Medical Center
Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters.
Wayne State University
Structure-activity relationships at monoamine transporters and muscarinic receptors for N-substituted-3alpha-(3'-chloro-, 4'-chloro-, and 4',4''-dichloro-substituted-diphenyl)methoxytropanes.
National Institute On Drug Abuse-Intramural Research Program
Novel tropane-based irreversible ligands for the dopamine transporter.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.
National Institute Of Diabetes And Digestive And Kidney Diseases
Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors.
Georgetown University Medical Center
Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors.
Georgetown University Medical Center
Highly selective chiral N-substituted 3alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues for the dopamine transporter: synthesis and comparative molecular field analysis.
National Institute On Drug Abuse-Intramural Research Program
Design, synthesis, and monoamine transporter binding site affinities of methoxy derivatives of indatraline.
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909).
National Institute Of Diabetes And Digestive And Kidney Diseases
Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects.
Georgetown University Medical Center
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
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane dopamine uptake inhibitors.
Georgia Institute Of Technology
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.
Georgia Institute Of Technology
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.
National Institute On Drug Abuse-Intramural Research Program
CoMFA study of novel phenyl ring-substituted 3alpha-(diphenylmethoxy)tropane analogues at the dopamine transporter.
National Institute On Drug Abuse-Intramural Research Program
(-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake.
University Of Maryland
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters.
Georgetown University Medical Center
Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.
University Of Minnesota
Synthesis and ligand binding of tropane ring analogues of paroxetine.
Research Triangle Institute
Synthesis and dopamine transporter affinity of the four stereoisomers of (+/-)-2-(methoxycarbonyl)-7-methyl-3-phenyl-7-azabicyclo[2.2.1]heptane.
University Of New Orleans
2beta-Substituted analogues of 4'-iodococaine: synthesis and dopamine transporter binding potencies.
University Of Oklahoma Health Sciences Center
Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton.
Georgetown University Medical Center
Synthesis and ligand binding of nortropane derivatives: N-substituted 2beta-carbomethoxy-3beta-(4'-iodophenyl)nortropane and N-(3-iodoprop-(2E)-enyl)-2beta-carbomethoxy-3beta-(3',4'-disubstituted phenyl)nortropane. New high-affinity and selective compounds for the dopamine transporter.
University Of Tours
Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters.
Research Triangle Institute
Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives.
University Of New Orleans
3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.
National Institutes Of Health
Synthesis, structure, dopamine transporter affinity, and dopamine uptake inhibition of 6-alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane derivatives.
University Of New Orleans
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
3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter.
Research Triangle Institute
Synthesis and ligand binding studies of 4'-iodobenzoyl esters of tropanes and piperidines at the dopamine transporter.
University Of Oklahoma
Synthesis and ligand binding of eta(6)-(2beta-carbomethoxy-3beta-phenyltropane) transition metal complexes.
University Of New Orleans
Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogs.
Georgia Institute Of Technology
Synthesis and dopamine transporter affinity of 2-(methoxycarbonyl)-9-methyl-3-phenyl-9-azabicyclo[3.3.1]nonane derivatives.
University Of New Orleans
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
3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter.
Research Triangle Institute
Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs.
Research Triangle Institute
N-substituted analogs of 2 beta-carbomethoxy-3 beta- (4'-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain.
Research Biochemicals International
Synthesis, ligand binding, and quantitative structure-activity relationship study of 3 beta-(4'-substituted phenyl)-2 beta-heterocyclic tropanes: evidence for an electrostatic interaction at the 2 beta-position.
Research Triangle Institute
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.
National Institutes Of Health
Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter.
Research Triangle Institute
Synthesis and ligand binding study of 3 beta-(4'-substituted phenyl)-2 beta-(heterocyclic)tropanes.
Research Triangle Institute
Chemistry and biology of the 2 beta-alkyl-3 beta-phenyl analogues of cocaine: subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position.
Mayo Foundation
Synthesis of 2 beta-acyl-3 beta-aryl-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites in rat striatum and frontal cortex.
Wake Forest University
Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters.
National Institute On Drug Abuse
Synthesis, cocaine receptor affinity, and dopamine uptake inhibition of several new 2 beta-substituted 3 beta-phenyltropanes.
University Of New Orleans
Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding.
Trophix Pharmaceuticals
Synthesis, ligand binding, and QSAR (CoMFA and classical) study of 3 beta-(3'-substituted phenyl)-, 3 beta-(4'-substituted phenyl)-, and 3 beta-(3',4'-disubstituted phenyl)tropane-2 beta-carboxylic acid methyl esters.
Research Triangle Institute
Novel 3 alpha-(diphenylmethoxy)tropane analogs: potent dopamine uptake inhibitors without cocaine-like behavioral profiles.
National Institutes Of Health
Synthesis of substituted 3-carbamoylecgonine methyl ester analogues: irreversible and photoaffinity ligands for the cocaine receptor/dopamine transporter.
University Of Maryland
N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters.
Research Biochemicals International
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.
University Of Tennessee At Knoxville
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
Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites.
National Institute Of Diabetes And Digestive And Kidney Diseases
Analysis of cocaine receptor site ligand binding by three-dimensional Voronoi site modeling approach.
University Of Michigan
3-Aryl-2-(3'-substituted-1',2',4'-oxadiazol-5'-yl)tropane analogues of cocaine: affinities at the cocaine binding site at the dopamine, serotonin, and norepinephrine transporters.
Research Triangle Institute
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
Research Triangle Institute
Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue.
Mayo Foundation
Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter.
Research Triangle Institute
Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter.
Research Triangle Institute
N-modified analogues of cocaine: synthesis and inhibition of binding to the cocaine receptor.
Research Triangle Institute
2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor.
Research Triangle Institute
Synthesis, ligand binding, QSAR, and CoMFA study of 3 beta-(p-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters.
Research Triangle Institute
Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor.
Research Biochemicals
Synthesis and ligand binding of cocaine isomers at the cocaine receptor.
Research Triangle Institute
[123I]-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane: high-affinity SPECT radiotracer of monoamine reuptake sites in brain.
Research Biochemicals
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.
H. Lundbeck
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
TBA
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake.
TBA
Pyrroloisoquinoline antidepressants. Potent, enantioselective inhibition of tetrabenazine-induced ptosis and neuronal uptake of norepinephrine, dopamine, and serotonin.
TBA
Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins.
TBA
3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake.
TBA
Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters.
National Institute Of Diabetes And Digestive And Kidney Diseases
The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor.
National Institute On Drug Abuse-Intramural Research Program
Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter.
Wayne State University
Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors.
University Of Michigan
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors.
Georgetown University Medical Center
Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors.
Georgetown University Medical Center
Synthesis and dopamine transporter binding affinities of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes.
University Of New Orleans
Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines.
Southern Research Institute
Discovery of substituted 3,4-diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol.
University Of Michigan
Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors.
Georgetown University Medical Center
Effects of two-carbon bridge region methoxylation of benztropine: discovery of novel chiral ligands for the dopamine transporter.
Universit£
[3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and binding affinities of 2 beta-(3-iodoallyloxycarbonyl)-3 beta-(4-substituted-aryl)tropane analogues as ligands for the dopamine transporter studies.
Inha University
Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter.
Wayne State University
Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles.
Georgetown University Medical Center
3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter.
Research Triangle Institute
Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors.
Georgetown University Medical Center
An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes.
Georgetown University Medical Center
N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter.
Georgetown University Medical Center
Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.
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
Synthesis and transporter binding properties of (R)-2 beta, 3 beta- and (R)-2 alpha, 3 alpha-diaryltropanes.
Research Triangle Institute
Further evidence for a dopamine reuptake pharmacophore. The effect of N-methylation on Threo-methylphenidate and its analogs
TBA
Synthesis and evaluation of novel-N-[2-(bis-aryl-methoxy)ethyl-N-aralkyl-,-alkanediamines as potent and selective dopamine reuptake inhibitors: Seco analogs of GBR12935 and GBR12909
TBA
Further structure-activity relationship studies on 8-substituted-3-[2-(diarylmethoxyethylidenyl)]-8-azabicyclo[3.2.1]octane derivatives at monoamine transporters.
University Of New Orleans
Further structure-activity relationship studies on 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: identification of compounds with triple uptake inhibitory activity as potential antidepressant agents.
Wayne State University
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.
Sepracor
Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.
University Of New Orleans
Discovery and synthesis of novel luteolin derivatives as DAT agonists.
Zhengzhou University
Quantitative structure-activity relationship studies of threo-methylphenidate analogs.
Institute Of Technology
Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile) analogues at monoamine transporters.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and antidepressant activity of optical isomers of 2-(4-benzylpiperazin-1-yl)-1-(5-chloro-6-methoxynaphthalen-2-yl) propan-1-ol (SIPI5056).
Institute Of Pharmaceutical Industry
Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter.
University Of Glasgow
Synthesis, radiolabeling and preliminary in vivo evaluation of [18F]FE-PE2I, a new probe for the dopamine transporter.
Institutet
Effects of Various Isoquinoline Alkaloids on In Vitro 3H-Dopamine Uptake by Rat Striatal Synaptosomes
TBA
N-Phthalimidoalkyl derivatives of 2β-carbomethoxy-3β-(4′-iodophenyl)tropane (β-CIT): Brain monoamine transporter affinity
TBA
A novel photoaffinity label for the dopamine transporter based on N-substituted 3α-[bis(4′-fluorophenyl)methoxy]tropane
TBA
New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter.
University Of Glasgow
New fluoro-diphenylchalcogen derivatives to explore the serotonin transporter by PET.
University Of Tours
Synthesis of enantiomerically pure milnacipran analogs and inhibition of dopamine, serotonin, and norepinephrine transporters.
University Of Oslo
DAT/SERT selectivity of flexible GBR 12909 analogs modeled using 3D-QSAR methods.
University Heights
Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER.
Institute For Degenerative Diseases
Design and synthesis of a novel photoaffinity ligand for the dopamine and serotonin transporters based on 2beta-carbomethoxy-3beta-biphenyltropane.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(4'-p-substituted phenyl)-piperidine analogs of cocaine.
Yale University
Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.
University Of Kentucky
Further structural exploration of trisubstituted asymmetric pyran derivatives (2S,4R,5R)-2-benzhydryl-5-benzylamino-tetrahydropyran-4-ol and their corresponding disubstituted (3S,6S) pyran derivatives: a proposed pharmacophore model for high-affinity interaction with the dopamine, serotonin, and no
Wayne State University
Further structure-activity relationship studies of piperidine-based monoamine transporter inhibitors: effects of piperidine ring stereochemistry on potency. Identification of norepinephrine transporter selective ligands and broad-spectrum transporter inhibitors.
University Of Illinois At Chicago
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[aryl or heteroaryl]phenyltropanes.
Yale University
Discovery of novel trisubstituted asymmetric derivatives of (2S,4R,5R)-2-benzhydryl-5-benzylaminotetrahydropyran-4-ol, exhibiting high affinity for serotonin and norepinephrine transporters in a stereospecific manner.
Wayne State University
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Acenta Discovery
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Janssen-Cilag
Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.
National Institute On Drug Abuse
Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.
Harvard Medical School
Synthesis and monoamine transporter affinity of 3'-analogs of 2-beta-carbomethoxy-3-beta-(4'-iodophenyl)tropane (beta-CIT).
Yale School Of Medicine
Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites.
State University Of New York
Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate.
Organix
Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine.
Niddk
Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter.
Niddk
Synthesis of dopamine transporter selective 3-[2-(diarylmethoxyethylidene)]-8-alkylaryl-8-azabicyclo[3.2.1]octanes.
University Of New Orleans
Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents.
National Institute Of Diabetes And Digestive And Kidney Diseases
New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine).
University Of Pennsylvania
Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter.
National Institute On Drug Abuse-Intramural Research Program/Nih
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Drew University
Enantioselective synthesis of S-(+)-2beta-carboalkoxy-3alpha-[bis(4-fluorophenyl)methoxy]tropanes as novel probes for the dopamine transporter.
National Institute On Drug Abuse-Intramural Research Program
Synthesis of iodinated 3beta-aryltropanes with selective binding to either the dopamine or serotonin transporters.
State University Of New York
Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents: chiral hydroxyl-containing derivatives of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine.
National Institute Of Diabetes And Digestive And Kidney Diseases
Substituted diphenyl sulfides as selective serotonin transporter ligands: synthesis and in vitro evaluation.
University Of Tours
Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: potential positron emission tomography (PET) imaging agents for the dopamine transporter.
Alcohol And Drug Abuse Research Center
Enantioselective syntheses of dopaminergic (R)- and (S)-benzyltetrahydroisoquinolines.
Universidad De Valencia
Synthesis of 2beta-acyl-3beta-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites.
State University Of New York
Synthesis and monoamine transporter affinity of 3beta-(4-(2-pyrrolyl)phenyl)-8-azabicycl.
State University Of New York
A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents.
Georgetown University Medical Center
Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(2''-, 3''- or 4''-substituted) biphenyltropanes.
Yale University
Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.
University Of Tokyo
Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies.
Georgetown University Medical Center
Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine.
University Of New Orleans
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.
National Institute Of Diabetes And Digestive And Kidney Diseases
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons.
Novartis Pharma
Tolerance in the replacement of the benzhydrylic O atom in 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives by an N atom: development of new-generation potent and selective N-analogue molecules for the dopamine transporter.
Organix
Potent and selective ligands for the dopamine transporter (DAT): structure-activity relationship studies of novel 4-[2-(diphenylmethoxy)ethyl]-1-(3-phenylpropyl)piperidine analogues.
Organix
Specificity of diastereomers of [99mTc]TRODAT-1 as dopamine transporter imaging agents.
University Of Pennsylvania
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.
National Institute On Drug Abuse
1-[1-2-Benzo[b]thiopheneyl)cyclohexyl]piperidine hydrochloride (BTCP) yields two active primary metabolites in vitro: synthesis, identification from rat liver microsome extracts, and affinity for the neuronal dopamine transporter.
University Of Montpellier
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
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
Highly selective, novel analogs of 4-[2-(diphenylmethoxy)ethyl]- 1-benzylpiperidine for the dopamine transporter: effect of different aromatic substitutions on their affinity and selectivity.
Organix
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
Drew University
Synthesis of 3 beta-aryl-8-azabicyclo[3.2.1]octanes with high binding affinities and selectivities for the serotonin transporter site.
State University Of New York
Structure-activity relationship studies of novel 4-[2-[bis(4-fluorophenyl)methoxy]ethyl]-1-(3-phenylpropyl)piperidine analogs: synthesis and biological evaluation at the dopamine and serotonin transporter sites.
Organix
Inhibition and inactivation of presynaptic cholinergic markers using redox-reactive choline analogs.
University Of Toledo
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
University Of Oklahoma
Selective monoamine oxidase inhibitors. 3. Cyclic compounds related to 4-aminophenethylamine. Preparation and neuron-selective action of some 5-(2-aminoethyl)-2,3-dihydroindoles.
TBA
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
Universit£
Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography.
Brookhaven National Laboratory
Structure-Activity Relationship Studies on a Series of 3?-[Bis(4-fluorophenyl)methoxy]tropanes and 3?-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders.
National Institute On Drug Abuse-Intramural Research Program
Covalent Modifiers: A Chemical Perspective on the Reactivity of?,?-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.
University Of Pittsburgh
Design, synthesis and biological evaluation of novel coumarin thiazole derivatives as a-glucosidase inhibitors.
Jishou University
Mechanism of the Flavoprotein l-Hydroxynicotine Oxidase: Kinetic Mechanism, Substrate Specificity, Reaction Product, and Roles of Active-Site Residues.
University Of Texas At San Antonio
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.
Chulabhorn Research Institute