| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Liming Shao, Michael C Hewitt, Scott C Malcolm, Fengjiang Wang, Jianguo Ma, Una C Campbell, Nancy A Spicer, Sharon R Engel, Larry W Hardy, Zhi-Dong Jiang, Rudy Schreiber, Kerry L Spear, Mark A Varne. Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues. Journal of medicinal chemistry. vol 54. issue 15. 2011-10-07. PMID:21739935. |
the present work expands the chemical space known to offer potent inhibition of the serotonin transporter (sert), norepinephrine transporter (net), and dopamine transporter (dat) and discloses novel bicyclic octahydrocyclopenta[c]pyrrole and octahydro-1h-isoindole scaffolds as potent triple reuptake inhibitors (tris) for the potential treatment of depression. |
2011-10-07 |
2023-08-12 |
mouse |
| Stacey J Sukoff Rizzo, Sarah K Leonard, Adam Gilbert, Paul Dollings, Deborah L Smith, Mei-Yi Zhang, Li Di, Brian J Platt, Sarah Neal, Jason M Dwyer, Corey N Bender, Jean Zhang, Tim Lock, Dianne Kowal, Angela Kramer, Andrew Randall, Christine Huselton, Karthick Vishwanathan, Susanna Y Tse, John Butera, Robert H Ring, Sharon Rosenzweig-Lipson, Zoë A Hughes, John Dunlo. The metabotropic glutamate receptor 7 allosteric modulator AMN082: a monoaminergic agent in disguise? The Journal of pharmacology and experimental therapeutics. vol 338. issue 1. 2011-08-30. PMID:21508084. |
in vitro selectivity profiling of met-1 demonstrated physiologically relevant transporter binding affinity at serotonin transporter (sert), dopamine transporter (dat), and norepinephrine transporter (net) (323, 3020, and 3410 nm, respectively); whereas the parent compound amn082 had appreciable affinity at net (1385 nm). |
2011-08-30 |
2023-08-12 |
rat |
| Jingying Liu, Lin Zhu, Karl Plössl, Brian P Lieberman, Hank F Kun. Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporter. Bioorganic & medicinal chemistry letters. vol 21. issue 10. 2011-08-23. PMID:21458259. |
a series of novel n-fluoropyridyl-containing tropane derivatives were synthesized and their binding affinities for the dopamine transporter (dat), serotonin transporter (sert) and norepinephrine (net) were determined via competitive radioligand binding assays. |
2011-08-23 |
2023-08-12 |
Not clear |
| Zhishan Li, Alcmène Chalazonitis, Yung-Yu Huang, J John Mann, Kara Gross Margolis, Qi Melissa Yang, Dolly O Kim, Francine Côté, Jacques Mallet, Michael D Gersho. Essential roles of enteric neuronal serotonin in gastrointestinal motility and the development/survival of enteric dopaminergic neurons. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 31. issue 24. 2011-08-22. PMID:21677183. |
rings of sert-immunoreactive terminal axons surrounded myenteric dopaminergic neurons and sert knock-out increased intestinal levels of dopamine metabolites, implying that enteric dopaminergic neurons receive a serotonergic innervation. |
2011-08-22 |
2023-08-12 |
mouse |
| Sara Bettè, Michela Castagna, Elena Bossi, Antonio Peres, Vellea Franca Sacch. The SLC6/NSS family members KAAT1 and CAATCH1 have weak chloride dependence. Channels (Austin, Tex.). vol 2. issue 5. 2011-07-29. PMID:19066444. |
transport by aaleut is cl⁻ independent, whereas many neurotransmitter:sodium symporters like serotonin transporter (sert), gaba transporter (gat1), dopamine transporter, and norephinephrine transporter, among others, are strongly cl⁻ dependent. |
2011-07-29 |
2023-08-12 |
Not clear |
| Philippe Huot, Tom H Johnston, Katie D Lewis, James B Koprich, M Gabriela Reyes, Susan H Fox, Matthew J Piggott, Jonathan M Brotchi. Characterization of 3,4-methylenedioxymethamphetamine (MDMA) enantiomers in vitro and in the MPTP-lesioned primate: R-MDMA reduces severity of dyskinesia, whereas S-MDMA extends duration of ON-time. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 31. issue 19. 2011-07-25. PMID:21562283. |
r-mdma (rectus-mdma) is relatively selective for 5-ht(2a) receptors, whereas s-mdma (sinister-mdma) inhibits both serotonin (sert) and dopamine transporters (dat; sert/dat ratio of 10 to 1). |
2011-07-25 |
2023-08-12 |
marmoset |
| Bhaskar Gopishetty, Stuart Hazeldine, Soumava Santra, Mark Johnson, Gyan Modi, Solav Ali, Juan Zhen, Maarten Reith, Aloke Dutt. 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. Journal of medicinal chemistry. vol 54. issue 8. 2011-07-04. PMID:21446715. |
the novel compounds were tested for their affinities for the dopamine transporter (dat), serotonin 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. |
2011-07-04 |
2023-08-12 |
rat |
| Sonja Sucic, Ali El-Kasaby, Oliver Kudlacek, Subhodeep Sarker, Harald H Sitte, Philippe Marin, Michael Freissmut. The serotonin transporter is an exclusive client of the coat protein complex II (COPII) component SEC24C. The Journal of biological chemistry. vol 286. issue 18. 2011-07-01. PMID:21454670. |
the transporters for serotonin (sert), dopamine, and noradrenaline have a conserved hydrophobic core but divergent n and c termini. |
2011-07-01 |
2023-08-12 |
mouse |
| Teodora-Adriana Perles-Barbacaru, Daniel Procissi, Andrey V Demyanenko, F Scott Hall, George R Uhl, Russell E Jacob. Quantitative pharmacologic MRI: mapping the cerebral blood volume response to cocaine in dopamine transporter knockout mice. NeuroImage. vol 55. issue 2. 2011-06-10. PMID:21185387. |
cocaine acts to block the dopamine, norepinephrine, and serotonin transporters (dat, net, and sert) that clear their respective neurotransmitters from the synapses, helping to terminate cognate neurotransmission. |
2011-06-10 |
2023-08-12 |
mouse |
| Susanna Nencetti, Maria R Mazzoni, Gabriella Ortore, Annalina Lapucci, Janette Giuntini, Elisabetta Orlandini, Irene Banti, Elisa Nuti, Antonio Lucacchini, Gino Giannaccini, Armando Rossell. Synthesis, molecular docking and binding studies of selective serotonin transporter inhibitors. European journal of medicinal chemistry. vol 46. issue 3. 2011-06-02. PMID:21272963. |
with the aim of obtaining compounds possessing high sert selectivity, in the present work we synthesized and studied the inhibition of serotonin (sert), dopamine (dat) and norepinephrine (net) transporters by docking studies and experimental binding measurements of a series of 4-(aryl)piperidin-3-one o-4-benzyl oxime hydrochlorides (1-10) of both e and z configuration. |
2011-06-02 |
2023-08-12 |
Not clear |
| Britta Haenisch, Heinz Bönisc. Depression and antidepressants: insights from knockout of dopamine, serotonin or noradrenaline re-uptake transporters. Pharmacology & therapeutics. vol 129. issue 3. 2011-05-19. PMID:21147164. |
major targets of ads are the serotonin transporter (sert), the noradrenaline transporter (nat) and also the dopamine transporter (dat) located in the plasma membrane of corresponding neurons. |
2011-05-19 |
2023-08-12 |
mouse |
| Anja W Fjorback, Heidi K Müller, Jana Haase, Merete K Raarup, Ove Wibor. Modulation of the dopamine transporter by interaction with Secretory Carrier Membrane Protein 2. Biochemical and biophysical research communications. vol 406. issue 2. 2011-05-05. PMID:21295544. |
the monoamine transporters for dopamine (dat), norepinephrine (net) and serotonin (sert) facilitate the homeostatic balance of neurotransmitters in the synaptic cleft and thus, play a fundamental role in regulating neuronal activity. |
2011-05-05 |
2023-08-12 |
Not clear |
| Karl Strecker, Florian Wegner, Swen Hesse, Georg-Alexander Becker, Marianne Patt, Philipp M Meyer, Donald Lobsien, Johannes Schwarz, Osama Sabr. Preserved serotonin transporter binding in de novo Parkinson's disease: negative correlation with the dopamine transporter. Journal of neurology. vol 258. issue 1. 2011-04-25. PMID:20644949. |
since the loss of dopaminergic neurons is the pathologic hallmark of pd and sert might be associated with psychiatric co-morbidity, we further sought to correlate sert availability with the availability of dopamine transporter (dat) and depressive or motor symptoms in early pd. |
2011-04-25 |
2023-08-12 |
human |
| David B Horton, Kiran B Siripurapu, Seth D Norrholm, John P Culver, Marhaba Hojahmat, Joshua S Beckmann, Steven B Harrod, Agripina G Deaciuc, Michael T Bardo, Peter A Crooks, Linda P Dwoski. meso-Transdiene analogs inhibit vesicular monoamine transporter-2 function and methamphetamine-evoked dopamine release. The Journal of pharmacology and experimental therapeutics. vol 336. issue 3. 2011-04-21. PMID:21177475. |
meso-transdiene (mtd), a lobeline analog, lacks nicotinic receptor affinity, retains affinity for vesicular monoamine transporter 2 (vmat2), and, surprisingly, has enhanced affinity for dopamine (da) and serotonin transporters [da transporter (dat) and serotonin transporter (sert), respectively]. |
2011-04-21 |
2023-08-12 |
rat |
| Derek Angus, Matilda Bingham, Dawn Buchanan, Neil Dunbar, Linsday Gibson, Richard Goodwin, Anders Haunsø, Andrea Houghton, Margaret Huggett, Richard Morphy, Susan Napier, Olaf Nimz, Joanna Passmore, Glenn Walke. The identification, and optimisation of hERG selectivity, of a mixed NET/SERT re-uptake inhibitor for the treatment of pain. Bioorganic & medicinal chemistry letters. vol 21. issue 1. 2011-04-14. PMID:21112782. |
hit compound 1, a selective noradrenaline re-uptake transporter (net) inhibitor was optimised to build in potency at the serotonin re-uptake transporter (sert) whilst maintaining selectivity against the dopamine re-uptake transporter (dat). |
2011-04-14 |
2023-08-12 |
mouse |
| Madhusudhan Purushotham, Anjaneyulu Sheri, Duy-Phong Pham-Huu, Bertha K Madras, Aaron Janowsky, Peter C Meltze. The synthesis and biological evaluation of 2-(3-methyl or 3-phenylisoxazol-5-yl)-3-aryl-8-thiabicyclo[3.2.1]octanes. Bioorganic & medicinal chemistry letters. vol 21. issue 1. 2011-04-14. PMID:21146984. |
cocaine, a potent stimulant of the central nervous system, owes its reinforcing and stimulant properties to its ability to inhibit monoamine uptake systems such as the dopamine transporter (dat), and the serotonin transporter (sert) located on presynaptic neurons in the striatum. |
2011-04-14 |
2023-08-12 |
Not clear |
| Pei Chun Hsieh, I Hui Lee, Tzung Lieh Yeh, Kao Chin Chen, Hui Chun Huang, Po See Chen, Yen Kuang Yang, Wei Jen Yao, Ru-Band Lu, Nan Tsing Chi. Distribution volume ratio of serotonin and dopamine transporters in euthymic patients with a history of major depression - a dual-isotope SPECT study. Psychiatry research. vol 184. issue 3. 2011-02-03. PMID:21030217. |
serotonin transporter (sert) and dopamine transporter (dat) levels differ in patients with major depression who are in a depressed state in comparison with healthy controls. |
2011-02-03 |
2023-08-12 |
human |
| Morten Ziebell, Signe Holm-Hansen, Gerda Thomsen, Aase Wagner, Peter Jensen, Lars H Pinborg, Gitte Moos Knudse. Serotonin transporters in dopamine transporter imaging: a head-to-head comparison of dopamine transporter SPECT radioligands 123I-FP-CIT and 123I-PE2I. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. vol 51. issue 12. 2010-12-22. PMID:21078806. |
current spect radioligands available for in vivo imaging of the dopamine transporter (dat) also show affinity for monoamine transporters other than dat, especially the serotonin transporter (sert). |
2010-12-22 |
2023-08-12 |
Not clear |
| Jörn Reese, Adrian Kraschewski, Ion Anghelescu, Georg Winterer, Lutz G Schmidt, Jürgen Gallinat, Franz Rüschendorf, Hans Rommelspacher, Catrin Wernick. Haplotypes of dopamine and serotonin transporter genes are associated with antisocial personality disorder in alcoholics. Psychiatric genetics. vol 20. issue 4. 2010-11-04. PMID:20505557. |
the dopamine transporter (dat) and the serotonin transporter (sert) are involved in endophenotypes that are associated with these subtypes. |
2010-11-04 |
2023-08-12 |
Not clear |
| Li Jijun, Li Zaiwang, Li Anyuan, Wang Shuzhen, Qi Fanghua, Zhao Lin, Lv Hon. Abnormal expression of dopamine and serotonin transporters associated with the pathophysiologic mechanism of Tourette syndrome. Neurology India. vol 58. issue 4. 2010-10-26. PMID:20739786. |
it is also well known that dopamine and serotonin transporters (dat and sert) are monoamine neurotransmitter transporters, which participate in the metabolism of da and 5-ht, respectively. |
2010-10-26 |
2023-08-12 |
Not clear |