| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Horrick Sharma, Soumava Santra, Joy Debnath, Tamara Antonio, Maarten Reith, Aloke Dutt. Flexible and biomimetic analogs of triple uptake inhibitor 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: Synthesis, biological characterization, and development of a pharmacophore model. Bioorganic & medicinal chemistry. vol 22. issue 1. 2014-11-06. PMID:24315194. |
the model revealed features important for inhibitors to exhibit a balanced activity against dopamine transporter (dat), serotonin transporter (sert), and norepinephrine transporter (net). |
2014-11-06 |
2023-08-12 |
Not clear |
| Y-S Ding, M Naganawa, J-D Gallezot, N Nabulsi, S-F Lin, J Ropchan, D Weinzimmer, T J McCarthy, R E Carson, Y Huang, M Laruell. Clinical doses of atomoxetine significantly occupy both norepinephrine and serotonin transports: Implications on treatment of depression and ADHD. NeuroImage. vol 86. 2014-09-03. PMID:23933039. |
atomoxetine (atx), a drug for treatment of depression and adhd, has a high affinity for the norepinephrine transporter (net); however, our previous study showed it had a blocking effect similar to fluoxetine on binding of [(11)c]dasb, a selective serotonin transporter (sert) ligand. |
2014-09-03 |
2023-08-12 |
monkey |
| Shuang Liu, Congxiang Zha, Kassoum Nacro, Min Hu, Wenge Cui, Yuh-Lin Yang, Ulhas Bhatt, Aruna Sambandam, Matthew Isherwood, Larry Yet, Michael T Herr, Sarah Ebeltoft, Carla Hassler, Linda Fleming, Anthony D Pechulis, Anne Payen-Fornicola, Nicholas Holman, Dennis Milanowski, Ian Cotterill, Vadim Mozhaev, Yuri Khmelnitsky, Peter R Guzzo, Bruce J Sargent, Bruce F Molino, Richard Olson, Dalton King, Snjezana Lelas, Yu-Wen Li, Kim Johnson, Thaddeus Molski, Anitra Orie, Alicia Ng, Roy Haskell, Wendy Clarke, Robert Bertekap, Jonathan O'Connell, Nicholas Lodge, Michael Sinz, Stephen Adams, Robert Zaczek, John E Maco. Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors. ACS medicinal chemistry letters. vol 5. issue 7. 2014-07-22. PMID:25050161. |
a series of 4-bicyclic heteroaryl 1,2,3,4-tetrahydroisoquinoline inhibitors of the serotonin transporter (sert), norepinephrine transporter (net), and dopamine transporter (dat) was discovered. |
2014-07-22 |
2023-08-13 |
mouse |
| Vivek Kumar, Troels Rahbek-Clemmensen, Christian B Billesbølle, Trine Nygaard Jorgensen, Ulrik Gether, Amy Hauck Newma. Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram. ACS medicinal chemistry letters. vol 5. issue 6. 2014-06-19. PMID:24944746. |
novel rhodamine-labeled ligands, based on (s)-citalopram, were synthesized and evaluated for uptake inhibition at the human serotonin, dopamine, and norepinephrine transporters (hsert, hdat, and hnet, respectively) and for binding at sert, in transiently transfected cos7 cells. |
2014-06-19 |
2023-08-13 |
human |
| Dean G Brown, Peter R Bernstein, Ye Wu, Rebecca A Urbanek, Christopher W Becker, Scott R Throner, Bruce T Dembofsky, Gary B Steelman, Lois A Lazor, Clay W Scott, Michael W Wood, Steven S Wesolowski, David A Nugiel, Stephanie Koch, Jian Yu, Donald E Pivonka, Shuang Li, Carol Thompson, Anna Zacco, Charles S Elmore, Patricia Schroeder, JianWei Liu, Christopher A Hurley, Stuart Ward, Hazel J Hunt, Karen Williams, Joseph McLaughlin, Valerie Hoesch, Simon Sydserff, Donna Maier, David Aharon. Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity. ACS medicinal chemistry letters. vol 4. issue 1. 2014-06-05. PMID:24900562. |
herein, we describe the discovery of inhibitors of norepinephrine (net) and dopamine (dat) transporters with reduced activity relative to serotonin transporters (sert). |
2014-06-05 |
2023-08-13 |
rat |
| Jacob Andersen, Nicolai Stuhr-Hansen, Linda Grønborg Zachariassen, Heidi Koldsø, Birgit Schiøtt, Kristian Strømgaard, Anders S Kristense. Molecular basis for selective serotonin reuptake inhibition by the antidepressant agent fluoxetine (Prozac). Molecular pharmacology. vol 85. issue 5. 2014-05-15. PMID:24516100. |
inhibitors of the serotonin transporter (sert) are widely used antidepressant agents, but the structural mechanism for inhibitory activity and selectivity over the closely related norepinephrine transporter (net) is not well understood. |
2014-05-15 |
2023-08-12 |
human |
| Linda D Simmler, Anna Rickli, York Schramm, Marius C Hoener, Matthias E Liecht. Pharmacological profiles of aminoindanes, piperazines, and pipradrol derivatives. Biochemical pharmacology. vol 88. issue 2. 2014-04-22. PMID:24486525. |
we investigated norepinephrine (ne), dopamine (da), and serotonin (5-hydroxytryptamine [5-ht]) uptake inhibition using human embryonic kidney 293 (hek 293) cells that express the respective human monoamine transporters (net, dat, and sert). |
2014-04-22 |
2023-08-12 |
human |
| Seyed Khosrow Tayebati, Daniele Tomassoni, Innocent Ejike Nwankwo, Antonio Di Stefano, Piera Sozio, Laura Serafina Cerasa, Francesco Ament. Modulation of monoaminergic transporters by choline-containing phospholipids in rat brain. CNS & neurological disorders drug targets. vol 12. issue 1. 2013-12-23. PMID:23244432. |
the present study was designed to assess the influence of treatment for 7 days with choline-equivalent doses (cdp-choline: 325 mg/kg/day; gpc: 150 mg/kg/day) of these compounds on brain dopamine (da), and serotonin (5-ht) levels and on da plasma membrane transporter (dat), vesicular monoamine transporters (vmat1 and vmat2), serotonin transporter (sert), and norepinephrine transporter (net) in the rat. |
2013-12-23 |
2023-08-12 |
rat |
| Stephen M Stahl, Clara Lee-Zimmerman, Sylvia Cartwright, Debbi Ann Morrissett. Serotonergic drugs for depression and beyond. Current drug targets. vol 14. issue 5. 2013-10-29. PMID:23531115. |
the original trend to do this selectively (e.g., with ssris or selective serotonin reuptake inhibitors) has given way to combining various additional pharmacologic mechanisms with sert inhibition, including dual actions by single drugs (e.g., snris or serotonin norepinephrine reuptake inhibitors), or by augmenting ssris with a second drug of a different mechanism (e.g., bupropion with dopamine and norepinephrine reuptake inhibition; trazodone with 5ht2a antagonism; mirtazapine with 5ht2a/5ht2c/5ht3/alpha2 antagonism; buspirone or some atypical antipsychotics with 5ht1a partial agonism; other atypical antipsychotics with 5ht2c/5ht7 antagonism and other mechanisms). |
2013-10-29 |
2023-08-12 |
Not clear |
| Stephen M Stahl, Clara Lee-Zimmerman, Sylvia Cartwright, Debbi Ann Morrissett. Serotonergic drugs for depression and beyond. Current drug targets. vol 14. issue 5. 2013-10-29. PMID:23531115. |
novel drugs in development include those that combine multiple simultaneous pharmacologic mechanisms in addition to sert inhibition within the same molecule, such as vilazodone (combining 5ht1a partial agonism with sert inhibition), triple reuptake inhibitors (combining norepinephrine and dopamine reuptake inhibition with sert inhibition), and vortioxetine, a multimodal antidepressant combining actions at the g protein receptor mode (5ht1a and 5ht1b partial agonism and 5ht7 antagonism), at the ion channel mode (5ht3 antagonism) as well as the neurotransmitter transporter mode (sert inhibition). |
2013-10-29 |
2023-08-12 |
Not clear |
| Richard J Karpowicz, Matthew Dunn, David Sulzer, Dalibor Same. APP+, a fluorescent analogue of the neurotoxin MPP+, is a marker of catecholamine neurons in brain tissue, but not a fluorescent false neurotransmitter. ACS chemical neuroscience. vol 4. issue 5. 2013-10-22. PMID:23647019. |
app+ is a substrate for the dopamine transporter (dat), norepinephrine transporter (net), and serotonin transporter (sert), and as such represented a candidate for the development of new ffn probes. |
2013-10-22 |
2023-08-12 |
mouse |
| Robert A Comley, Cristian A Salinas, Mark Slifstein, Marcella Petrone, Carmine Marzano, Idriss Bennacef, Paul Shotbolt, Jasper Van der Aart, Marta Neve, Laura Iavarone, Roberto Gomeni, Marc Laruelle, Frank A Gray, Roger N Gunn, Eugenii A Rabine. Monoamine transporter occupancy of a novel triple reuptake inhibitor in baboons and humans using positron emission tomography. The Journal of pharmacology and experimental therapeutics. vol 346. issue 2. 2013-09-25. PMID:23685546. |
studies were performed in baboons (papio anubis) to determine the relationship between plasma concentration and occupancy of brain serotonin reuptake transporter (sert), dopamine reuptake transporter (dat), and norepinephrine uptake transporter (net) using the radioligands [(11)c]dasb [(n,n-dimethyl-2-(2-amino-4-cyanophenylthio) benzylamine], [(11)c]pe2i [n-(3-iodoprop-2e-enyl)-2β-carbomethoxy-3β-(4-methylphenyl)nortropane], and [(11)c]2-[(2-methoxyphenoxy)phenylmethyl]morpholine (also known as [(11)c]mrb) and in humans using [(11)c]dasb and [(11)c]pe2i. |
2013-09-25 |
2023-08-12 |
Not clear |
| Les Iversen, Simon Gibbons, Ric Treble, Vincent Setola, Xi-Ping Huang, Bryan L Rot. Neurochemical profiles of some novel psychoactive substances. European journal of pharmacology. vol 700. issue 1-3. 2013-08-05. PMID:23261499. |
thirteen of the test substances acted as inhibitors of monoamine uptake at submicromolar concentrations, including 9 potent inhibitors of the dopamine transporter (dat), 12 potent inhibitors of the norepinephrine transporter (net) and 4 potent inhibitors of the serotonin transporter (sert). |
2013-08-05 |
2023-08-12 |
human |
| Akihiro Takano, Christer Halldin, Lars Fard. SERT and NET occupancy by venlafaxine and milnacipran in nonhuman primates: a PET study. Psychopharmacology. vol 226. issue 1. 2013-07-30. PMID:23090625. |
serotonin and norepinephrine reuptake inhibitors (snris) are antidepressants which have high affinity to both serotonin transporter (sert) and norepinephrine transporter (net). |
2013-07-30 |
2023-08-12 |
Not clear |
| Narattaphol Charoenphandhu, Amporn Nuntapornsak, Kannikar Wongdee, Nateetip Krishnamra, Jantarima Charoenphandh. Upregulated mRNA levels of SERT, NET, MAOB, and BDNF in various brain regions of ovariectomized rats exposed to chronic aversive stimuli. Molecular and cellular biochemistry. vol 375. issue 1-2. 2013-07-26. PMID:23208077. |
herein, we used quantitative real-time pcr to quantify the mrna levels of serotonin reuptake transporter (sert), norepinephrine transporter (net), monoamine oxidase-b (maob), tryptophan hydroxylase (tph), and tyrosine hydroxylase (th) in various brain regions of ovariectomized (ovx) rats which had been exposed for 4 weeks to chronic aversive stimuli (cas), such as water deprivation, cage tilt, and illumination. |
2013-07-26 |
2023-08-12 |
rat |
| Michael H Baumann, John S Partilla, Kurt R Lehne. Psychoactive "bath salts": not so soothing. European journal of pharmacology. vol 698. issue 1-3. 2013-06-10. PMID:23178799. |
similar to other psychomotor stimulants, synthetic cathinones target plasma membrane transporters for dopamine (i.e., dat), norepinephrine (i.e., net) and serotonin (i.e, sert). |
2013-06-10 |
2023-08-12 |
rat |
| Peng Zhang, Trine Nygaard Jørgensen, Claus J Loland, Amy Hauck Newma. A rhodamine-labeled citalopram analogue as a high-affinity fluorescent probe for the serotonin transporter. Bioorganic & medicinal chemistry letters. vol 23. issue 1. 2013-05-28. PMID:23168018. |
the resulting rhodamine-labeled ligand 8 inhibited [(3)h]5-ht uptake in cos-7 cells (k(i)=225 nm) with similar potency to the tropane-based jhc 1-064 (1), but with higher specificity towards the sert relative to the transporters for dopamine and norepinephrine. |
2013-05-28 |
2023-08-12 |
Not clear |
| Soumava Santra, Sanjib Gogoi, Bhaskar Gopishetty, Tamara Antonio, Juan Zhen, Maarten E A Reith, Aloke K Dutt. Structural exploration of (3S,6S)-6-benzhydryl-N-benzyltetrahydro-2H-pyran-3-amine analogues: identification of potent triple monoamine reuptake inhibitors as potential antidepressants. ChemMedChem. vol 7. issue 12. 2013-04-29. PMID:23060293. |
the new compounds were tested for their affinities for the dopamine transporter (dat), the serotonin transporter (sert), and the norepinephrine transporter (net) in rat brain by measuring their capacity to inhibit the uptake of [(3)h]da, [(3)h]5-ht, and [(3)h]ne, respectively. |
2013-04-29 |
2023-08-12 |
rat |
| Lena Sørensen, Jacob Andersen, Mette Thomsen, Stinna M R Hansen, Xiaobei Zhao, Albin Sandelin, Kristian Strømgaard, Anders S Kristense. Interaction of antidepressants with the serotonin and norepinephrine transporters: mutational studies of the S1 substrate binding pocket. The Journal of biological chemistry. vol 287. issue 52. 2013-02-26. PMID:23086945. |
the serotonin transporter (sert) and the norepinephrine transporter (net) are sodium-dependent neurotransmitter transporters responsible for reuptake of released serotonin and norepinephrine, respectively, into nerve terminals in the brain. |
2013-02-26 |
2023-08-12 |
human |
| Rachel W S Li, Cui Yang, Y W Kwan, S W Chan, Simon M Y Lee, George P H Leun. Involvement of organic cation transporter-3 and plasma membrane monoamine transporter in serotonin uptake in human brain vascular smooth muscle cells. Frontiers in pharmacology. vol 4. 2013-02-15. PMID:23407616. |
the specific serotonin re-uptake transporter (sert) inhibitor citalopram, the specific norepinephrine transporter (net) inhibitor desipramine, and the dopamine transporter (dat) inhibitor gbr12935 inhibited 5-ht uptake in hbvsmcs with ic(50) values of 97.03 ± 40.10, 10.49 ± 5.98, and 2.80 ± 1.04 μm, respectively. |
2013-02-15 |
2023-08-12 |
human |