| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Chunyang Jin, Hernán A Navarro, F Ivy Carrol. Development of 3-phenyltropane analogues with high affinity for the dopamine and serotonin transporters and low affinity for the norepinephrine transporter. Journal of medicinal chemistry. vol 51. issue 24. 2009-01-22. PMID:19053748. |
in this study, a series of 3beta-(substituted phenyl)tropane-2beta-carboxylic acid methyl esters (7a-g), 3beta-(4-methoxyphenyl)tropane-2beta-carboxylic acid esters (8a-j), and 3beta-(4-methoxyphenyl)-2beta-[3-(4'-methylphenyl)isoxazol-5-yl]tropane (9) were synthesized and evaluated for their monoamine transporter binding affinities to identify potent and selective compounds for both the dat and 5-htt relative to the norepinephrine transporter (net). |
2009-01-22 |
2023-08-12 |
Not clear |
| Jeffrey S Stehouwer, Nachwa Jarkas, Fanxing Zeng, Ronald J Voll, Larry Williams, Vernon M Camp, Eugene J Malveaux, John R Votaw, Leonard Howell, Michael J Owens, Mark M Goodma. 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. Journal of medicinal chemistry. vol 51. issue 24. 2009-01-22. PMID:19053782. |
in vitro competition binding assays demonstrated that 1-4 have a high affinity for the sert (k(i) values = 0.3-0.4 nm) and are selective for the sert over the dopamine and norepinephrine transporters (dat and net). |
2009-01-22 |
2023-08-12 |
monkey |
| Kelly Lengyel, Rick Pieschl, Todd Strong, Thaddeus Molski, Gail Mattson, Nicholas J Lodge, Yu-Wen L. Ex vivo assessment of binding site occupancy of monoamine reuptake inhibitors: methodology and biological significance. Neuropharmacology. vol 55. issue 1. 2008-11-05. PMID:18538356. |
the goal of this study was to develop and validate ex vivo binding assays for serotonin (sert), norepinephrine (net) and dopamine (dat) transporters, and to use these assays to evaluate the binding site occupancy of triple and double monoamine reuptake inhibitors in rat brains. |
2008-11-05 |
2023-08-12 |
rat |
| Aloke K Dutta, Balaram Ghosh, Swati Biswas, Maarten E A Reit. D-161, a novel pyran-based triple monoamine transporter blocker: behavioral pharmacological evidence for antidepressant-like action. European journal of pharmacology. vol 589. issue 1-3. 2008-10-24. PMID:18561912. |
one of our lead molecules, d-161 exhibited triple monoamine transporter inhibitory activity with the highest affinity for norepinephrine transporter (net) followed by its affinity for serotonin transporter (sert) and dopamine transporter (dat). |
2008-10-24 |
2023-08-12 |
mouse |
| Chunyang Jin, Hernán A Navarro, Kevin Page, F Ivy Carrol. 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. Bioorganic & medicinal chemistry. vol 16. issue 14. 2008-09-11. PMID:18556210. |
all tested compounds were selective for the dat relative to the norepinephrine transporter (net) and serotonin transporter (5-htt). |
2008-09-11 |
2023-08-12 |
Not clear |
| Leah Aluisio, Brian Lord, Ann J Barbier, Ian C Fraser, Sandy J Wilson, Jamin Boggs, Lisa K Dvorak, Michael A Letavic, Bruce E Maryanoff, Nicholas I Carruthers, Pascal Bonaventure, Timothy W Lovenber. In-vitro and in-vivo characterization of JNJ-7925476, a novel triple monoamine uptake inhibitor. European journal of pharmacology. vol 587. issue 1-3. 2008-08-25. PMID:18499098. |
triple reuptake inhibitors, which block the serotonin transporter (sert), norepinephrine transporter (net) and dopamine transporter (dat) in the central nervous system have been described as therapeutic alternatives for classical selective serotonin reuptake inhibitors, with advantages due to their multiple mechanisms of action. |
2008-08-25 |
2023-08-12 |
mouse |
| Michael R Tilley, Howard H G. Dopamine transporter inhibition is required for cocaine-induced stereotypy. Neuroreport. vol 19. issue 11. 2008-08-25. PMID:18596615. |
the primary mechanism by which cocaine induces stereotypy has been difficult to discern because cocaine has three high-affinity targets: the reuptake transporters for dopamine (dat), norepinephrine, and serotonin. |
2008-08-25 |
2023-08-12 |
mouse |
| Christopher D Verrico, Laurie Lynch, Michele A Fahey, Ashley-Kay Fryer, Gregory M Miller, Bertha K Madra. MDMA-induced impairment in primates: antagonism by a selective norepinephrine or serotonin, but not by a dopamine/norepinephrine transport inhibitor. Journal of psychopharmacology (Oxford, England). vol 22. issue 2. 2008-08-18. PMID:18308800. |
we postulated that mdma will compromise executive function in primates and that an inhibitor of the serotonin transporter (sert) and the norepinephrine transporter (net) but not the dopamine (dat) transporter, will prevent impairment. |
2008-08-18 |
2023-08-12 |
human |
| Chunyang Jin, Hernán A Navarro, F Ivy Carrol. Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives. Bioorganic & medicinal chemistry. vol 16. issue 10. 2008-08-18. PMID:18434164. |
one of the most potent and selective compounds in the series was 3beta-(4-chlorophenyl)-2beta-(4-nitrophenylethynyl)tropane (10c) that possessed an ic(50) value of 0.9nm at the dat and k(i) values of 230nm and 620nm at the norepinephrine transporter (net) and serotonin transporter (5-htt), respectively. |
2008-08-18 |
2023-08-12 |
Not clear |
| Susanne Jørgensen, Elsebet Østergaard Nielsen, Dan Peters, Tino Dyhrin. Validation of a fluorescence-based high-throughput assay for the measurement of neurotransmitter transporter uptake activity. Journal of neuroscience methods. vol 169. issue 1. 2008-06-23. PMID:18222006. |
pre-synaptic dopamine, norepinephrine and serotonin transporters (dat, net and sert) terminate synaptic catecholamine transmission through reuptake of released neurotransmitter. |
2008-06-23 |
2023-08-12 |
Not clear |
| Manoj Mishra, Rohit Kolhatkar, Juan Zhen, Ingrid Parrington, Maarten E A Reith, Aloke K Dutt. 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. Bioorganic & medicinal chemistry. vol 16. issue 6. 2008-06-13. PMID:18249549. |
all synthesized derivatives were tested for their affinities for the dopamine transporter (dat), serotonin (5-ht) transporter (sert), and norepinephrine transporter (net) in the brain by measuring their potency in inhibiting the uptake of [(3)h]da, [(3)h]5-ht, and [(3)h]ne, respectively. |
2008-06-13 |
2023-08-12 |
Not clear |
| Panayotis K Thanos, Michael Michaelides, Helene Benveniste, Gene Jack Wang, Nora D Volko. The effects of cocaine on regional brain glucose metabolism is attenuated in dopamine transporter knockout mice. Synapse (New York, N.Y.). vol 62. issue 5. 2008-06-03. PMID:18286542. |
cocaine-induced decreases in metabolism in thalamus (region with dense noradrenergic innervation) in dat(-/-) suggest that these were mediated by cocaine's blockade of norepinephrine transporters. |
2008-06-03 |
2023-08-12 |
mouse |
| Gang Zhao, Shao-Yun Zang, Xiang-Wei Zheng, Xiao-Hua Zhang, Li-He Gu. Bakuchiol analogs inhibit monoamine transporters and regulate monoaminergic functions. Biochemical pharmacology. vol 75. issue 9. 2008-05-27. PMID:18329002. |
monoamine transporter inhibition by delta3,2-hydroxybakuchiol was more selective for the dopamine transporter (dat) (ic50=0.58+/-0.1 microm) and norepinephrine transporter (net) (ic50=0.69+/-0.12 microm) than for the serotonin transporter (sert) (ic50=312.02+/-56.69 microm). |
2008-05-27 |
2023-08-12 |
mouse |
| Nachwa Jarkas, Ronald J Voll, Larry Williams, John R Votaw, Mike Owens, Mark M Goodma. Synthesis and in vivo evaluation of halogenated N,N-dimethyl-2-(2'-amino-4'-hydroxymethylphenylthio)benzylamine derivatives as PET serotonin transporter ligands. Journal of medicinal chemistry. vol 51. issue 2. 2008-04-17. PMID:18085744. |
the in vitro binding studies in cells transfected with human sert, norepinephrine transporter (net), and dopamine transporter (dat) showed that 35, 36, and 37 exhibited high sert affinity with k is (sert) = 1.26, 0.29, and 0.31 nm (vs [(3)h]citalopram), respectively. |
2008-04-17 |
2023-08-12 |
human |
| L Keith Henry, Jens Meiler, Randy D Blakel. Bound to be different: neurotransmitter transporters meet their bacterial cousins. Molecular interventions. vol 7. issue 6. 2008-04-17. PMID:18199851. |
the neurotransmitter transporters belonging to the solute carrier 6 (slc6) family, including the gamma-aminobutyric acid (gat), norepinephrine (net), serotonin (sert) and dopamine (dat) transporters are extremely important drug targets of great clinical relevance. |
2008-04-17 |
2023-08-12 |
human |
| Fanxing Zeng, Nachwa Jarkas, Jeffrey S Stehouwer, Ronald J Voll, Michael J Owens, Clinton D Kilts, Charles B Nemeroff, Mark M Goodma. Synthesis, in vitro characterization, and radiolabeling of reboxetine analogs as potential PET radioligands for imaging the norepinephrine transporter. Bioorganic & medicinal chemistry. vol 16. issue 2. 2008-02-20. PMID:17983754. |
six new (s,s)-enantiomers of reboxetine derivatives were synthesized and their binding affinities were determined via competition binding assays in cells expressing the human norepinephrine transporter (net), serotonin transporter (sert) or dopamine transporter (dat). |
2008-02-20 |
2023-08-12 |
human |
| Paulo H C Diniz, Janice H Silva, Marcus V Gomez, Cristina Guatimosim, Renato S Gome. Halothane increases non-vesicular [(3)H]dopamine release from brain cortical slices. Cellular and molecular neurobiology. vol 27. issue 6. 2007-12-07. PMID:17680357. |
these data suggest that [(3)h]da release induced by halothane is non-vesicular and would be mediated by the dopamine transporter (dat) and norepinephrine transporter (net). |
2007-12-07 |
2023-08-12 |
rat |
| Johnny Vercouillie, Winnie Deuther-Conrad, Matthias Scheunemann, Patrick Emond, Steffen Fischer, Uta Funke, Jörg Steinbach, Denis Guilloteau, Peter Brus. New fluoro-diphenylchalcogen derivatives to explore the serotonin transporter by PET. Bioorganic & medicinal chemistry letters. vol 17. issue 17. 2007-11-20. PMID:17658253. |
the compounds were synthesized and assayed toward the serotonin (sert), dopamine (dat), and norepinephrine (net) transporters. |
2007-11-20 |
2023-08-12 |
Not clear |
| Christophe Plisson, Jeffrey S Stehouwer, Ronald J Voll, Leonard Howell, John R Votaw, Michael J Owens, Mark M Goodma. 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. Journal of medicinal chemistry. vol 50. issue 19. 2007-10-23. PMID:17705359. |
the binding affinity of 1 to human monoamine transporters showed a high affinity for the sert (ki = 0.08 nm) with respect to the dopamine transporter (dat) (ki = 13 nm) and the norepinephrine transporter (net) (ki = 28 nm). |
2007-10-23 |
2023-08-12 |
human |
| Paul K Gong, Bruce E Blough, Lawrence E Brieaddy, Xiaodong Huang, Michael J Kuhar, Hernán A Navarro, F Ivy Carrol. Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes. Journal of medicinal chemistry. vol 50. issue 15. 2007-10-15. PMID:17602602. |
in general, the compounds showed higher dopamine transporter (dat) affinity relative to the serotonin and norepinephrine transporters (sert and net, respectively) and greater [3h]dopamine uptake inhibition potency relative to [3h]serotonin and [3h]norepinephrine uptake inhibition. |
2007-10-15 |
2023-08-12 |
rat |