| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| C Deleuze-Masquefa, M Michaud-Dutreilh, J Vignon, J M Kamenk. 1-[1-(2-Benzo[b]thiopheneyl)cyclohexyl]piperidine hydrochloride (BTCP) yields two active primary metabolites in vivo. Identification and quantification of BTCP primary metabolites in mice plasma, urine, and brain and their affinity for the neuronal dopamine transporter. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. vol 9. issue 4. 2000-04-11. PMID:10664474. |
1-[1-(2-benzo[b]thiopheneyl)cyclohexyl]piperidine hydrochloride (btcp) and cocaine bind to the neuronal dopamine transporter (dat) to strongly inhibit dopamine (da) reuptake. |
2000-04-11 |
2023-08-12 |
mouse |
| C D Fiorillo, J T William. Selective inhibition by adenosine of mGluR IPSPs in dopamine neurons after cocaine treatment. Journal of neurophysiology. vol 83. issue 3. 2000-04-11. PMID:10712458. |
selective inhibition by adenosine of mglur ipsps in dopamine neurons after cocaine treatment. |
2000-04-11 |
2023-08-12 |
rat |
| C D Fiorillo, J T William. Selective inhibition by adenosine of mGluR IPSPs in dopamine neurons after cocaine treatment. Journal of neurophysiology. vol 83. issue 3. 2000-04-11. PMID:10712458. |
one consequence of repeated cocaine treatment is an increase in extracellular adenosine in the ventral tegmental area (vta), which results in tonic inhibition of synaptic input to dopamine neurons. |
2000-04-11 |
2023-08-12 |
rat |
| L B Li, M E Reit. Interaction of Na+, K+, and Cl- with the binding of amphetamine, octopamine, and tyramine to the human dopamine transporter. Journal of neurochemistry. vol 74. issue 4. 2000-04-11. PMID:10737611. |
in this study, substrate recognition was studied via the inhibition of binding of [3h]win 35,428 [2beta-carbomethoxy-3beta-(4-fluorophenyl)[3h]tropane], a cocaine analogue, to the human dopamine transporter in human embryonic kidney 293 cells. |
2000-04-11 |
2023-08-12 |
human |
| E El Daly, V Chefer, S Sandill, T S Shippenber. Modulation of the neurotoxic effects of methamphetamine by the selective kappa-opioid receptor agonist U69593. Journal of neurochemistry. vol 74. issue 4. 2000-04-11. PMID:10737612. |
kappa-opioid receptor agonists prevent alterations in dopamine neurotransmission that occur in response to repeated cocaine administration. |
2000-04-11 |
2023-08-12 |
mouse |
| M Froimowitz, K M Wu, J Rodrigo, C Georg. Conformational preferences of the potent dopamine reuptake blocker BTCP and its analogs and their incorporation into a pharmacophore model. Journal of computer-aided molecular design. vol 14. issue 2. 2000-04-05. PMID:10721502. |
there is excellent agreement between a 'back-bridged' cocaine analog that is optimal as a dopamine reuptake blocker and the previously proposed biologically active conformer of methylphenidate. |
2000-04-05 |
2023-08-12 |
Not clear |
| C N Haile, G Carey, G B Varty, V L Coffi. The dopamine D(1) receptor agonist SKF-82958 serves as a discriminative stimulus in the rat. European journal of pharmacology. vol 388. issue 2. 2000-03-16. PMID:10666503. |
the dopamine d(2) receptor agonist trans-(+/-)-4,4a,5,6,7,8,8a, 9-octahydro-5-propyl-1h-propyl-1h-pyrazolo[3,4-g]quinoline dihydrochloride (quinpirole) and the indirect dopamine agonist cocaine did not substitute fully for the skf-82958 discriminative stimulus cue. |
2000-03-16 |
2023-08-12 |
rat |
| S J Li, B Biswal, Z Li, R Risinger, C Rainey, J K Cho, B J Salmeron, E A Stei. Cocaine administration decreases functional connectivity in human primary visual and motor cortex as detected by functional MRI. Magnetic resonance in medicine. vol 43. issue 1. 2000-03-14. PMID:10642730. |
it is suggested that the observed changes in low frequency components after acute cocaine administration during a resting, no-task situation may be used as a baseline reference source when assessing the effects of cocaine on task-driven activation or on mesolimbic dopamine pathways. |
2000-03-14 |
2023-08-12 |
human |
| W P Melega, G Lacan, A A Desalles, M E Phelp. Long-term methamphetamine-induced decreases of [(11)C]WIN 35,428 binding in striatum are reduced by GDNF: PET studies in the vervet monkey. Synapse (New York, N.Y.). vol 35. issue 4. 2000-03-13. PMID:10657033. |
win, a cocaine analog that binds to the dopamine transporter (dat), was used to provide an index of striatal dopamine terminal integrity. |
2000-03-13 |
2023-08-12 |
human |
| S Wang, S Sakamuri, I J Enyedy, A P Kozikowski, O Deschaux, B C Bandyopadhyay, S R Tella, W A Zaman, K M Johnso. Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies. Journal of medicinal chemistry. vol 43. issue 3. 2000-03-13. PMID:10669562. |
discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3d-database pharmacophore searching. |
2000-03-13 |
2023-08-12 |
mouse |
| S Wang, S Sakamuri, I J Enyedy, A P Kozikowski, O Deschaux, B C Bandyopadhyay, S R Tella, W A Zaman, K M Johnso. Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies. Journal of medicinal chemistry. vol 43. issue 3. 2000-03-13. PMID:10669562. |
a novel, fairly potent dopamine transporter (dat) inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone (3, k(i) values of 492 and 360 nm in binding affinity and inhibition of dopamine reuptake, respectively), with significant functional antagonism against cocaine and a different in vitro pharmacological profile from cocaine at the three transporter sites (dopamine, serotonin, and norepinephrine) was discovered through 3d-database pharmacophore searching. |
2000-03-13 |
2023-08-12 |
mouse |
| T Sato, S Kitayama, C Mitsuhata, T Ikeda, K Morita, T Doh. Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics. Naunyn-Schmiedeberg's archives of pharmacology. vol 361. issue 2. 2000-03-08. PMID:10685879. |
among the las tested, procaine and other ester-type las inhibited [3h]da uptake and binding of [3h]2-beta-carbomethoxy-3-beta-(4-fluorophenyl)tropane (cft), a cocaine analogue, in cos cells expressing rat dopamine transporter (dat). |
2000-03-08 |
2023-08-12 |
mouse |
| J G Chen, G Rudnic. Permeation and gating residues in serotonin transporter. Proceedings of the National Academy of Sciences of the United States of America. vol 97. issue 3. 2000-03-02. PMID:10655481. |
in net i155c, cocaine enhanced this inactivation, and the substrate, dopamine, apparently protected against inactivation. |
2000-03-02 |
2023-08-12 |
Not clear |
| S W Choi, D R Elmaleh, R N Hanson, A J Fischma. Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands. Journal of medicinal chemistry. vol 43. issue 2. 2000-02-28. PMID:10649976. |
we have undertaken a program to develop cocaine antagonists based on the premise that such compounds should block cocaine binding but permit reuptake of dopamine at the dopamine transporter (dat). |
2000-02-28 |
2023-08-12 |
Not clear |
| S B Caine, S S Negus, N K Mell. Effects of dopamine D(1-like) and D(2-like) agonists on cocaine self-administration in rhesus monkeys: rapid assessment of cocaine dose-effect functions. Psychopharmacology. vol 148. issue 1. 2000-02-25. PMID:10663416. |
effects of dopamine d(1-like) and d(2-like) agonists on cocaine self-administration in rhesus monkeys: rapid assessment of cocaine dose-effect functions. |
2000-02-25 |
2023-08-12 |
monkey |
| S B Caine, S S Negus, N K Mell. Effects of dopamine D(1-like) and D(2-like) agonists on cocaine self-administration in rhesus monkeys: rapid assessment of cocaine dose-effect functions. Psychopharmacology. vol 148. issue 1. 2000-02-25. PMID:10663416. |
the reinforcing effects of cocaine have been most compellingly related to its action as an indirect dopamine agonist. |
2000-02-25 |
2023-08-12 |
monkey |
| J L Katz, S Izenwasser, P Terr. Relationships among dopamine transporter affinities and cocaine-like discriminative-stimulus effects. Psychopharmacology. vol 148. issue 1. 2000-02-25. PMID:10663422. |
the discriminative-stimulus effects of cocaine have been reported to be mediated by indirect agonist actions initiated by the blockade of dopamine uptake, and the potencies of drugs that have discriminative-stimulus effects like cocaine are directly related to their dopamine transporter binding affinities. |
2000-02-25 |
2023-08-12 |
Not clear |
| J L Katz, S Izenwasser, P Terr. Relationships among dopamine transporter affinities and cocaine-like discriminative-stimulus effects. Psychopharmacology. vol 148. issue 1. 2000-02-25. PMID:10663422. |
the binding to the dopamine transporter by cocaine and many of its analogs has been reported to fit better using a two-site model than a one-site model. |
2000-02-25 |
2023-08-12 |
Not clear |
| N Chen, J V Ferrer, J A Javitch, J B Justic. Transport-dependent accessibility of a cytoplasmic loop cysteine in the human dopamine transporter. The Journal of biological chemistry. vol 275. issue 3. 2000-02-24. PMID:10636852. |
reaction of cys-90 or cys-306 with impermeant methanethiosulfonate derivatives enhanced dopamine uptake to a similar extent as the previously observed enhancement of [(3)h]cft binding caused by the same reaction, suggesting that cocaine may bind preferentially to a conformation in the transport cycle. |
2000-02-24 |
2023-08-12 |
human |
| L L Howell, P W Czoty, M J Kuhar, F I Carro. Comparative behavioral pharmacology of cocaine and the selective dopamine uptake inhibitor RTI-113 in the squirrel monkey. The Journal of pharmacology and experimental therapeutics. vol 292. issue 2. 2000-02-22. PMID:10640288. |
comparative behavioral pharmacology of cocaine and the selective dopamine uptake inhibitor rti-113 in the squirrel monkey. |
2000-02-22 |
2023-08-12 |
human |