48 articles for thisTarget
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Synthesis and pharmacological characterization of new neuronal nicotinic acetylcholine receptor ligands derived from Sazetidine-A.
Georgetown University Medical Center
Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selectivea4ß2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats.
Georgetown University Medical Center
Predicting new indications for approved drugs using a proteochemometric method.
Georgetown University Medical Center
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
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
SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement.
Georgetown University Medical Center
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.
Georgetown University Medical Center
Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis.
Georgetown University Medical Center
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
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 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
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 biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
Georgetown University Medical Center
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 of more potent analogues of the acetylcholinesterase inhibitor, huperzine B.
Georgetown University Medical Center
Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors.
Georgetown University Medical Center
Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles.
Georgetown University Medical Center
Synthesis of N(1)-substituted analogues of (2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid as agonists, partial agonists, and antagonists of group II metabotropic glutamate receptors.
Georgetown University Medical Center
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.
Georgetown University Medical Center
Synthesis, chiral chromatographic separation, and biological activities of the enantiomers of 10,10-dimethylhuperzine A.
Georgetown University Medical Center
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
1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.
Georgetown University Medical Center
Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation.
Georgetown University Medical Center
The nucleoside analog sangivamycin induces apoptotic cell death in breast carcinoma MCF7/adriamycin-resistant cells via protein kinase Cdelta and JNK activation.
Georgetown University Medical Center
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.
Georgetown University Medical Center
New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.
Georgetown University Medical Center
Structural basis of RasGRP binding to high-affinity PKC ligands.
Georgetown University Medical Center
Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase.
Georgetown University Medical Center
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth.
Georgetown University Medical Center
A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents.
Georgetown University Medical Center
Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity.
Georgetown University Medical Center
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 and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.
Georgetown University Medical Center
Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations.
Georgetown University Medical Center
alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.
Georgetown University Medical Center
3-Deoxy-D-myo-inositol 1-phosphate, 1-phosphonate, and ether lipid analogues as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth.
Georgetown University Medical Center
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.
Georgetown University Medical Center
Synthesis and structure-activity relationship studies of small molecule disruptors of EWS-FLI1 interactions in Ewing's sarcoma.
Georgetown University Medical Center
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
Georgetown University Medical Center
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.
Georgetown University Medical Center
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.
Georgetown University Medical Center
