| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Ole V Mortensen, Susan G Amar. Gain of function mutants reveal sites important for the interaction of the atypical inhibitors benztropine and bupropion with monoamine transporters. Journal of neurochemistry. vol 98. issue 5. 2006-10-03. PMID:16923164. |
taking advantage of the differential sensitivity of the dopamine and the norepinephrine transporters (dat and net) to benztropine and bupropion, we have used site-directed mutagenesis to produce gain-of-function mutants in net which demonstrate that ala279 in the trans-membrane domain 5 (tm5) and ser359 in the tm7 of dat are responsible for the higher sensitivity of dat to both bupropion and benztropine. |
2006-10-03 |
2023-08-12 |
Not clear |
| Rong Chen, Michael R Tilley, Hua Wei, Fuwen Zhou, Fu-Ming Zhou, San Ching, Ning Quan, Robert L Stephens, Erik R Hill, Timothy Nottoli, Dawn D Han, Howard H G. Abolished cocaine reward in mice with a cocaine-insensitive dopamine transporter. Proceedings of the National Academy of Sciences of the United States of America. vol 103. issue 24. 2006-09-11. PMID:16754872. |
there are three known high-affinity targets for cocaine: the dopamine transporter (dat), the serotonin transporter (sert), and the norepinephrine transporter (net). |
2006-09-11 |
2023-08-12 |
mouse |
| Shijun Zhang, Fernando Fernandez, Stuart Hazeldine, Jeffrey Deschamps, Juan Zhen, Maarten E A Reith, Aloke K Dutt. Further structural exploration of trisubstituted asymmetric pyran derivatives (2S,4R,5R)-2-benzhydryl-5-benzylamino-tetrahydropyran-4-ol and their corresponding disubstituted (3S,6S) pyran derivatives: a proposed pharmacophore model for high-affinity interaction with the dopamine, serotonin, and norepinephrine transporters. Journal of medicinal chemistry. vol 49. issue 14. 2006-09-11. PMID:16821783. |
all synthesized derivatives 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. |
2006-09-11 |
2023-08-12 |
Not clear |
| Shijun Zhang, Juan Zhen, Maarten E A Reith, Aloke K Dutt. Design, synthesis, and preliminary SAR study of 3- and 6-side-chain-extended tetrahydro-pyran analogues of cis- and trans-(6-benzhydryl-tetrahydropyran-3-yl)-benzylamine. Bioorganic & medicinal chemistry. vol 14. issue 11. 2006-08-14. PMID:16481172. |
all synthesized derivatives 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. |
2006-08-14 |
2023-08-12 |
Not clear |
| Terrence L Boos, Elisabeth Greiner, W Jason Calhoun, Thomas E Prisinzano, Barbara Nightingale, Christina M Dersch, Richard B Rothman, Arthur E Jacobson, Kenner C Ric. Structure-activity relationships of substituted N-benzyl piperidines in the GBR series: Synthesis of 4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-1-(2-trifluoromethylbenzyl)piperidine, an allosteric modulator of the serotonin transporter. Bioorganic & medicinal chemistry. vol 14. issue 11. 2006-08-14. PMID:16563775. |
a series of 4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-(substituted benzyl) piperidines with substituents at the ortho and meta positions in the aromatic ring of the n-benzyl side chain were synthesized and their affinities and selectivities for the dopamine transporter (dat), serotonin transporter (sert), and norepinephrine transporter (net) were determined. |
2006-08-14 |
2023-08-12 |
Not clear |
| Dawn D Han, Howard H G. Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs. BMC pharmacology. vol 6. 2006-08-03. PMID:16515684. |
the transporters for the monoamines dopamine, norepinephrine, and serotonin (dat, net, and sert) are targets for several popular psychostimulant drugs of abuse. |
2006-08-03 |
2023-08-12 |
mouse |
| Peter Grundt, Theresa A Kopajtic, Jonathan L Katz, Amy Hauck Newma. N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands. Bioorganic & medicinal chemistry letters. vol 15. issue 24. 2006-06-27. PMID:16213721. |
a series of n-8-substituted benztropinamines was synthesized and evaluated for binding at the dopamine (dat), serotonin (sert), norepinephrine (net) transporters, and muscarinic m1 receptors. |
2006-06-27 |
2023-08-12 |
Not clear |
| Elisabeth Greiner, Terrence L Boos, Thomas E Prisinzano, Maria G De Martino, Brian Zeglis, Christina M Dersch, Jamila Marcus, John S Partilla, Richard B Rothman, Arthur E Jacobson, Kenner C Ric. Design and synthesis of promiscuous high-affinity monoamine transporter ligands: unraveling transporter selectivity. Journal of medicinal chemistry. vol 49. issue 5. 2006-04-25. PMID:16509591. |
a series of 4-[2-[bis(4-fluorophenyl)methoxy]ethyl]-piperidines and 4-[2-[(bisphenyl)methoxy]ethyl]-piperidines with different types of substituents in the phenylpropyl side-chain were synthesized and examined for their ability to bind to the dopamine transporter (dat), the serotonin transporter (sert), and the norepinephrine transporter (net). |
2006-04-25 |
2023-08-12 |
Not clear |
| Kevin B Freeman, Kenner C Rice, Anthony L Rile. Assessment of monoamine transporter inhibition in the mediation of cocaine-induced conditioned taste aversion. Pharmacology, biochemistry, and behavior. vol 82. issue 3. 2006-03-02. PMID:16337262. |
using the conditioned taste aversion (cta) preparation, the present study examined the role of monoamine uptake inhibition in cocaine's aversive effects by comparing cocaine to three reuptake inhibitors with relative specificity for the transporters of dopamine (dat; gbr 12909), norepinephrine (net; desipramine) and serotonin (sert; clomipramine). |
2006-03-02 |
2023-08-12 |
rat |
| Sharadsrikar V Kotturi, Songchun Jiang, An-Chih Chang, Philip Abraham, Hernán A Navarro, Michael J Kuhar, F Ivy Carrol. Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes. Journal of medicinal chemistry. vol 48. issue 23. 2006-01-17. PMID:16279803. |
the compounds were evaluated for inhibition of radioligand binding at the dopamine, norepinephrine, and serotonin transporters (dat, net, and 5-htt, respectively). |
2006-01-17 |
2023-08-12 |
Not clear |
| Jean Logan, Yu-Shin Ding, Kuo-Shyan Lin, Deborah Pareto, Joanna Fowler, Anat Biego. Modeling and analysis of PET studies with norepinephrine transporter ligands: the search for a reference region. Nuclear medicine and biology. vol 32. issue 5. 2005-12-07. PMID:15982584. |
the development of positron emission tomography (pet) ligands for the norepinephrine transporter (net) has been slow compared to the development of radiotracers for others systems, such as the dopamine (dat) or the serotonin transporters (sert). |
2005-12-07 |
2023-08-12 |
Not clear |
| Katherine L Holton, Merewyn K Loder, Haley E Melikia. Nonclassical, distinct endocytic signals dictate constitutive and PKC-regulated neurotransmitter transporter internalization. Nature neuroscience. vol 8. issue 7. 2005-09-20. PMID:15924135. |
the dat internalization signal is conserved across slc6 neurotransmitter carriers and is functional in the homologous norepinephrine transporter, suggesting that this region is likely to be the endocytic signal for all slc6 neurotransmitter transporters. |
2005-09-20 |
2023-08-12 |
Not clear |
| Anu J Airaksinen, Marko Huotari, Alexander Shvetsov, Pirjo Vainiotalo, Pekka T Männisto, Leena Tuomisto, Kim A Bergström, Jouko Vepsäläine. Synthesis and biological evaluation of 6/7-exo-methyl-3beta-(4-iodo)phenyltropane-2beta-carboxylic acid methyl esters. European journal of medicinal chemistry. vol 40. issue 3. 2005-08-29. PMID:15725499. |
the effect of 6/7-groups was evaluated by in vitro receptor binding to dopamine (dat), serotonin (sert) and norepinephrine (net) transporters. |
2005-08-29 |
2023-08-12 |
mouse |
| Christian Pifl, Gabor Nagy, Sándor Berényi, Alexandra Kattinger, Harald Reither, Sándor Antu. Pharmacological characterization of ecstasy synthesis byproducts with recombinant human monoamine transporters. The Journal of pharmacology and experimental therapeutics. vol 314. issue 1. 2005-08-26. PMID:15831439. |
mdma and eight chemically defined byproducts of mdma synthesis were investigated for their interaction with the primary sites of action of mdma, namely the human plasmalemmal monamine transporters for norepinephrine, serotonin, and dopamine [(norepinephrine transporter (net), serotonin transporter (sert), and dopamine transporter (dat)]. |
2005-08-26 |
2023-08-12 |
human |
| Nachwa Jarkas, Jonathan McConathy, Ronald J Voll, Mark M Goodma. Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands. Journal of medicinal chemistry. vol 48. issue 13. 2005-08-23. PMID:15974579. |
competition binding in cells stably expressing the transfected human sert, dopamine transporter (dat), and norepinephrine transporter (net) using [(3)h]citalopram, [(3)h]win 35,428 or [(125)i]rti-55, and [(3)h]nisoxetine, respectively, demonstrated the following order of sert affinity (k(i) (nm)): 14a (0.25) > 16 (0.49) > 20 (0.57) > 14b (1.12) > 13 (1.59) > 33b (1.94) = 35 (2.04) >> 23 (8.50) = 28 (8.55) > 41 (15.11) >> 22 (51) > 33a (83.43) > 27 (92). |
2005-08-23 |
2023-08-12 |
human |
| Shijun Zhang, Juan Zhen, Maarten E A Reith, Aloke K Dutt. Discovery of novel trisubstituted asymmetric derivatives of (2S,4R,5R)-2-benzhydryl-5-benzylaminotetrahydropyran-4-ol, exhibiting high affinity for serotonin and norepinephrine transporters in a stereospecific manner. Journal of medicinal chemistry. vol 48. issue 15. 2005-08-23. PMID:16033275. |
all synthesized derivatives 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. |
2005-08-23 |
2023-08-12 |
Not clear |
| Brett C Ginsburg, Heather L Kimmel, F Ivy Carroll, Mark M Goodman, Leonard L Howel. Interaction of cocaine and dopamine transporter inhibitors on behavior and neurochemistry in monkeys. Pharmacology, biochemistry, and behavior. vol 80. issue 3. 2005-08-16. PMID:15740791. |
rti-177 and fecnt, two dat inhibitors with low affinity at norepinephrine transporters (net), produced dose-dependent stimulant effects on behavior maintained by a fixed-interval schedule of stimulus termination. |
2005-08-16 |
2023-08-12 |
human |
| Bertha K Madras, Gregory M Miller, Alan J Fischma. The dopamine transporter and attention-deficit/hyperactivity disorder. Biological psychiatry. vol 57. issue 11. 2005-07-29. PMID:15950014. |
in brain regions expressing both the dat and the norepinephrine transporter (net), the relative contributions of dopamine and norepinephrine to adhd pathophysiology and therapeutic response are obfuscated by the capacity of the net to clear dopamine as well as norepinephrine. |
2005-07-29 |
2023-08-12 |
human |
| J N Mason, H Farmer, I D Tomlinson, J W Schwartz, V Savchenko, L J DeFelice, S J Rosenthal, R D Blakel. Novel fluorescence-based approaches for the study of biogenic amine transporter localization, activity, and regulation. Journal of neuroscience methods. vol 143. issue 1. 2005-06-30. PMID:15763132. |
pre-synaptic norepinephrine (ne) and dopamine (da) transporters (net and dat) terminate catecholamine synaptic transmission through reuptake of released neurotransmitter. |
2005-06-30 |
2023-08-12 |
Not clear |
| Nachwa Jarkas, Jonathan McConathy, John R Votaw, Ronald J Voll, Eugene Malveaux, Vernon M Camp, Larry Williams, Robin R Goodman, Clinton D Kilts, Mark M Goodma. Synthesis and characterization of EADAM: a selective radioligand for mapping the brain serotonin transporters by positron emission tomography. Nuclear medicine and biology. vol 32. issue 1. 2005-06-24. PMID:15691664. |
competition binding assays in cells stably expressing the transfected human dopamine transporter (dat), sert and norepinephrine transporter (net) labeled with [3h]win 35428 or [(125)i]rti-55, [3h]citalopram and [3h]nisoxetine, respectively, indicated the following order of sert affinity: adam>eadam>>fluvoxamine. |
2005-06-24 |
2023-08-12 |
human |