| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| 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 |
| 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 |
| 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 |
| Prashant S Kharkar, Maarten E A Reith, Aloke K Dutt. Three-dimensional quantitative structure-activity relationship (3D QSAR) and pharmacophore elucidation of tetrahydropyran derivatives as serotonin and norepinephrine transporter inhibitors. Journal of computer-aided molecular design. vol 22. issue 1. 2008-06-03. PMID:18060532. |
three-dimensional quantitative structure-activity relationship (3d qsar) using comparative molecular field analysis (comfa) was performed on a series of substituted tetrahydropyran (thp) derivatives possessing serotonin (sert) and norepinephrine (net) transporter inhibitory activities. |
2008-06-03 |
2023-08-12 |
Not clear |
| 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 |
| Yosuke Yamauchi, Takaya Izumi, Kazuhiro Unemura, Yoshie Uenishi, Takayuki Nakagawa, Shuji Kanek. Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethamphetamine (MDMA) under acidic conditions. Neuroscience letters. vol 428. issue 2-3. 2008-03-26. PMID:17949903. |
perfusion with sert substrates at ph 7.4 dose-dependently evoked a transport-associated inward current response with the following rank order of potency: 5-ht>mdma>dopamine>>norepinephrine. |
2008-03-26 |
2023-08-12 |
xenopus_laevis |
| Ann J Barbier, Leah Aluisio, Brian Lord, Ying Qu, Sandy J Wilson, Jamin D Boggs, Pascal Bonaventure, Kirsten Miller, Ian Fraser, Lisa Dvorak, Cindy Pudiak, Christine Dugovic, Jonathan Shelton, Curt Mazur, Michael A Letavic, Nicholas I Carruthers, Timothy W Lovenber. Pharmacological characterization of JNJ-28583867, a histamine H(3) receptor antagonist and serotonin reuptake inhibitor. European journal of pharmacology. vol 576. issue 1-3. 2008-03-06. PMID:17765221. |
jnj-28583867 (2-methyl-4-(4-methylsulfanyl-phenyl)-7-(3-morpholin-4-yl-propoxy)-1,2,3,4-tetrahydro-isoquinoline) is a selective and potent histamine h(3) receptor antagonist (k(i)=10.6 nm) and inhibitor of the serotonin transporter (sert) (k(i)=3.7 nm), with 30-fold selectivity for sert over the dopamine and norepinephrine transporters. |
2008-03-06 |
2023-08-12 |
mouse |
| 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 |
| Mona M Hanna, Nahed M Eid, Riham F George, Hani M Safwa. Synthesis of some tropane derivatives of anticipated activity on the reuptake of norepinephrine and/or serotonin. Bioorganic & medicinal chemistry. vol 15. issue 24. 2008-02-19. PMID:17870537. |
the prepared compounds were tested for their activity and selectivity toward the norepinephrine transporter (net) and serotonin transporter (sert) using yohimbine-induced mortality and 5-hydroxytryptophan-induced neurotoxicity in mice, respectively. |
2008-02-19 |
2023-08-12 |
mouse |
| Georgianna G Gould, Bryan W Brooks, Alan Fraze. [(3)H] citalopram binding to serotonin transporter sites in minnow brains. Basic & clinical pharmacology & toxicology. vol 101. issue 3. 2008-01-02. PMID:17697042. |
mammalian serotonin (sert) and norepinephrine transporters (net) are target sites for antidepressants and are affected by pesticide exposures. |
2008-01-02 |
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 |
| Zheng Zhou, Juan Zhen, Nathan K Karpowich, Regina M Goetz, Christopher J Law, Maarten E A Reith, Da-Neng Wan. LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake. Science (New York, N.Y.). vol 317. issue 5843. 2007-09-21. PMID:17690258. |
tricyclic antidepressants exert their pharmacological effect-inhibiting the reuptake of serotonin, norepinephrine, and dopamine-by directly blocking neurotransmitter transporters (sert, net, and dat, respectively) in the presynaptic membrane. |
2007-09-21 |
2023-08-12 |
human |
| Vishakantha Murthy, Huw M L Davies, Simon J Hedley, Steven R Childer. Irreversible binding of a novel phenylisothiocyanate tropane analog to monoamine transporters in rat brain. Biochemical pharmacology. vol 74. issue 2. 2007-08-16. PMID:17540345. |
irreversible tropane analogs have been useful in identifying binding sites of cocaine on biogenic amine transporters, including transporters for dopamine (dat), serotonin (sert) and norepinephrine (net). |
2007-08-16 |
2023-08-12 |
rat |
| Shunichi Oya, Seok-Rye Choi, Mei-Ping Kung, Hank F Kun. 5-Chloro-2-(2'-((dimethylamino)methyl)-4'-iodophenylthio)benzenamine: a new serotonin transporter ligand. Nuclear medicine and biology. vol 34. issue 2. 2007-07-20. PMID:17307121. |
the new ligands displayed extremely high binding affinities to sert (k(i)=0.22+/-0.09 and 0.11+/-0.04 nm, respectively), with very low binding affinities to dopamine and norepinephrine transporters (k(i)>1000 nm). |
2007-07-20 |
2023-08-12 |
rat |
| Michael Decker, Jochen Lehman. Agonistic and antagonistic bivalent ligands for serotonin and dopamine receptors including their transporters. Current topics in medicinal chemistry. vol 7. issue 4. 2007-06-07. PMID:17305576. |
selectivity profiles and affinities depend strongly on the length of the alkylene-spacer: for some dimeric inhibitors the norepinephrine transporter (net) and the dopamine transporter (dat) affinities changed gradually, but for the serotonin transporter (sert) a pentamethylene spacer showed the highest potency. |
2007-06-07 |
2023-08-12 |
Not clear |