| Name | dopamine transporter |
|---|---|
| Synonyms | DA transporter; DAT1; DAT; DAT 1; Dopamine transporter; SLC6A3; Sodium dependent dopamine transporter; Dopamine transporters… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 18597947 | Espana RA, Roberts DC, Jones SR: Short-acting cocaine and long-acting GBR-12909 both elicit rapid uptake inhibition following intravenous delivery. Neuroscience. 2008 Jul 31;155(1):250-7. Epub 2008 Jul 1. The current studies sought to better characterize the onset of cocaine-induced DA uptake inhibition and to compare these effects to those obtained with the high-affinity, long-acting DA transporter inhibitor, GBR-12909 (1-(2-bis (4-fluorphenyl)-methoxy)-ethyl)-4-(3-phenyl-propyl) piperazine). |
32(0,1,1,2) | Details |
| 12672246 | Greiner E, Prisinzano T, Johnson II EM, Dersch CM, Marcus J, Partilla JS, Rothman RB, Jacobson AE, Rice KC: Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine. J Med Chem. 2003 Apr 10;46(8):1465-9. |
32(0,1,1,2) | Details |
| 19428788 | Sperlagh B, Windisch K, Ando RD, Sylvester Vizi E: Neurochemical evidence that stimulation of CB1 cannabinoid receptors on GABAergic nerve terminals activates the dopaminergic reward system by increasing release in the rat nucleus accumbens. Neurochem Int. 2009 Jun;54(7):452-7. Epub 2009 Feb 6. The cannabinoid agonist (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo [1,2,3-de]-1,4 -benzoxazin-6-yl]-1-naphthalenylmethanone mesylate (WIN55,212-2, 100 nM) significantly enhanced stimulation-evoked [(3) H] release in the presence of the selective dopamine transporter inhibitor 1-[2-[bis-(4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine dihydrochloride (GBR12909, 100 nM). |
31(0,1,1,1) | Details |
| 15240827 | Czoty PW, Ramanathan CR, Mutschler NH, Makriyannis A, Bergman J: Drug discrimination in methamphetamine-trained monkeys: effects of monoamine transporter inhibitors. J Pharmacol Exp Ther. 2004 Nov;311(2):720-7. Epub 2004 Jul 7. In monkeys discriminating i.m. injections of 0.3 mg/kg MA from saline, methamphetamine (0.01-0.3 mg/kg), and dopamine transporter (DAT) inhibitors, including 1-[2-(bis (4-fluorophenyl)-methoxy) ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909; 1.0-17.8 mg/kg) and its analogs AM2502 (1.0-17.8 mg/kg), AM2506 (1.0-30.0 mg/kg), AM2515 (1.0-17.8 mg/kg), and AM2517 (1.0-5.6 mg/kg), produced dose-related increases in responding on the MA-associated lever and, at the highest doses, full substitution. |
31(0,1,1,1) | Details |
| 17127069 | Gilbert KM, Boos TL, Dersch CM, Greiner E, Jacobson AE, Lewis D, Matecka D, Prisinzano TE, Zhang Y, Rothman RB, Rice KC, Venanzi CA: DAT/SERT selectivity of flexible GBR 12909 analogs modeled using 3D-QSAR methods. Bioorg Med Chem. 2007 Jan 15;15(2):1146-59. Epub 2006 Oct 1. The reuptake inhibitor GBR 12909 (1-{2-[bis (4-fluorophenyl) methoxy] ethyl}-4-(3-phenylpropyl) piperazine, 1) and its analogs have been developed as tools to test the hypothesis that selective dopamine transporter (DAT) inhibitors will be useful therapeutics for cocaine addiction. |
31(0,1,1,1) | Details |
| 11249581 | Preti A: Vanoxerine National Institute on Drug Abuse. Curr Opin Investig Drugs. 2000 Oct;1(2):241-51. Gist-Brocades originally initiated studies of vanoxerine, along with another piperazine, GBR-12935, for the treatment of cocaine dependence. Dopamine transporter occupancy has also been measured. |
4(0,0,0,4) | Details |
| 11689080 | Zhang Y, Joseph DB, Bowen WD, Flippen-Anderson JL, Dersch CM, Rothman RB, Jacobson AE, Rice KC: Synthesis and biological evaluation of tropane-like 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909) analogues. J Med Chem. 2001 Nov 8;44(23):3937-45. We have prepared azabicyclo [3.2.1] derivatives (C-3-substituted tropanes) that bind with high affinity to the dopamine transporter and inhibit reuptake. |
4(0,0,0,4) | Details |
| 12490570 | Kimmel HL, Carroll FI, Kuhar MJ: Withdrawal from repeated cocaine alters dopamine transporter protein turnover in the rat striatum. J Pharmacol Exp Ther. 2003 Jan;304(1):15-21. Transporter binding was measured with [(3) H] GBR12935 [1-(2-[diphenylmethoxy] ethyl)-4-[3-phenylpropyl] piperazine]. |
3(0,0,0,3) | Details |
| 15475185 | Manakova S, Puttonen KA, Raasmaja A, Mannisto PT: The roles of dopamine transporter and Bcl-2 protein in the protection of CV1-P cells from 6-OHDA-induced toxicity. Toxicol Lett. 2004 Dec 1;154(1-2):117-23. The apparent entry of 6-OHDA into fibroblasts was decreased by the DAT inhibitor, 1-(2-bis-(4-fluorophenyl) methoxy) ethyl)-4-(3-phenyl-propyl) piperazine (GBR 12909). |
2(0,0,0,2) | Details |
| 14982963 | Lindsey KP, Wilcox KM, Votaw JR, Goodman MM, Plisson C, Carroll FI, Rice KC, Howell LL: Effects of dopamine transporter inhibitors on cocaine self-administration in rhesus monkeys: relationship to transporter occupancy determined by positron emission tomography neuroimaging. J Pharmacol Exp Ther. 2004 Jun;309(3):959-69. Epub 2004 Feb 24. The drugs studied included a selective DAT inhibitor, [1-(2 [bis (4-fluorophenyl-) methoxy] ethyl)-4-(3-phenylpropyl) piperazine] bimesylate hydrate (GBR 12909); an inhibitor with equal potency at and norepinephrine transporters, [3beta-(4-chlorophenyl) tropane-2beta-(3-phenylisoxazol-5-yl)] HCl (RTI-177); and a nonselective inhibitor of norepinephrinem and serotonin transporters, [(-)-3beta-(3'-methyl-4-chlorophenyl) tropane-2beta-carboxylic acid methyl ester] (RTI-112). |
2(0,0,0,2) | Details |
| 15261288 | Kimura M, Masuda T, Yamada K, Kawakatsu N, Kubota N, Mitani M, Kishii K, Inazu M, Kiuchi Y, Oguchi K, Namiki T: Antioxidative activities of novel diphenylalkyl piperazine derivatives with high affinities for the dopamine transporter. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4287-90. |
162(2,2,2,2) | Details |
| 18845198 | Stepanov V, Jarv J: Kinetic mechanism of dopamine transporter interaction with 1-(2-(bis-(4-fluorophenyl) methoxy) ethyl)-4-(3-phenylpropyl) piperazine (GBR 12909). Neurochem Int. 2008 Dec;53(6-8):370-3. Epub 2008 Sep 18. |
162(2,2,2,2) | Details |
| 12927856 | Kimura M, Masuda T, Yamada K, Mitani M, Kubota N, Kawakatsu N, Kishii K, Inazu M, Kiuchi Y, Oguchi K, Namiki T: Novel diphenylalkyl piperazine derivatives with high affinities for the dopamine transporter. Bioorg Med Chem. 2003 Sep 1;11(18):3953-63. |
82(1,1,1,2) | Details |
| 12213078 | Prisinzano T, Greiner E, Johnson EM 2nd, Dersch CM, Marcus J, Partilla JS, Rothman RB, Jacobson AE, Rice KC: Piperidine analogues of 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909): high affinity ligands for the dopamine transporter. J Med Chem. 2002 Sep 12;45(19):4371-4. |
82(1,1,1,2) | Details |
| 18393401 | Hsin LW, Chang LT, Rothman RB, Dersch CM, Jacobson AE, Rice KC: Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine and 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl) piperazine: role of amino, methoxyl, methyl, methylene, and oxo substituents on affinity for the and serotonin transporters. J Med Chem. 2008 May 8;51(9):2795-806. Epub 2008 Apr 5. Novel derivatives of 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909, 1) and 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl) piperazine (GBR 12935, 2) with various substituents in positions C2 and C3 of the phenylpropyl side chain were synthesized and evaluated for their ability to bind to the dopamine transporter (DAT) and the serotonin transporter (SERT). |
81(1,1,1,1) | Details |
| 11123994 | Zhang Y, Rothman RB, Dersch CM, de Costa BR, Jacobson AE, Rice KC: Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909). J Med Chem. 2000 Dec 14;43(25):4840-9. A series of analogues related to 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl) piperazine (2) and 1- inverted question mark2-[bis (4-fluorophenyl) methoxy] ethyl inverted question mark-4-(3-phenylpropyl) piperazine (3) (GBR 12935 and GBR 12909, respectively), in which the piperazine moiety was replaced by bridged piperazines for structural rigidity, has been designed, synthesized, and evaluated for their ability to bind to the dopamine transporter (DAT) and to inhibit the uptake of (3) H-labeled (DA). |
81(1,1,1,1) | Details |
| 17000468 | Chiasson K, Daoust B, Levesque D, Martinoli MG: D2 agonists, bromocriptine and quinpirole, increase MPP+ -induced toxicity in PC12 cells. Neurotox Res. 2006 Aug;10(1):31-42. On the other hand, 1-{2-[bis-(4-fluorophenyl) methoxy] ethyl}-4-(3-phenylpropyl) piperazine (GBR 12909), a potent inhibitor of the dopamine transporter, partially reversed MPP+ -induced cellular death and completely abolished the increase of cellular death induced by bromocriptine. |
81(1,1,1,1) | Details |
| 16014753 | Desai RI, Kopajtic TA, French D, Newman AH, Katz JL: Relationship between in vivo occupancy at the dopamine transporter and behavioral effects of cocaine, GBR 12909 [1-{2-[bis-(4-fluorophenyl) methoxy] ethyl}-4-(3-phenylpropyl) piperazine], and benztropine analogs. J Pharmacol Exp Ther. 2005 Oct;315(1):397-404. Epub 2005 Jul 13. To better understand these differences, we examined the relationship between locomotor-stimulant effects of cocaine, 1-{2-[bis-(4-fluorophenyl) methoxy] ethyl}-4-(3-phenylpropyl)-piperazine (GBR 12909), and BZT analogs [(3alpha-[bis (4'-fluorophenyl) methoxy]-tropane) (AHN 1-055) and (N-allyl-3alpha-[bis (4'-fluorophenyl) methoxy]-tropane) (AHN 2-005)] and their in vivo displacement of the DA transporter ligand [125I] 3beta-(4-iodophenyl)-tropan-2beta-carboxylic acid isopropyl ester hydrochloride (RTI-121) in striatum. |
40(0,1,2,5) | Details |
| 12646032 | Ghorai SK, Cook C, Davis M, Venkataraman SK, George C, Beardsley PM, Reith ME, Dutta AK: High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl) piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo. J Med Chem. 2003 Mar 27;46(7):1220-8. In our effort to develop high-affinity ligands for the dopamine transporter which might find potential use as cocaine medication, a polar substituent was introduced into the piperidine ring of one of our disubstituted lead analogues derived from 1-[2-(diphenylmethoxy)-ethyl]-4-(3-phenylpropyl) piperazine (GBR 12935). |
34(0,1,1,4) | Details |
| 11882001 | Hsin LW, Dersch CM, Baumann MH, Stafford D, Glowa JR, Rothman RB, Jacobson AE, Rice KC: Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents: chiral -containing derivatives of 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine and 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl) piperazine. J Med Chem. 2002 Mar 14;45(6):1321-9. |
32(0,1,1,2) | Details |
| 12659747 | Kimura M, Masuda T, Yamada K, Mitani M, Kubota N, Kawakatsu N, Kishii K, Inazu M, Kiuchi Y, Oguchi K, Namiki T: Syntheses of novel diphenyl piperazine derivatives and their activities as inhibitors of uptake in the central nervous system. Bioorg Med Chem. 2003 Apr 17;11(8):1621-30. A new series of diphenyl piperazine derivatives containing the phenyl substituted aminopropanol moiety, which were modified at sites between the diphenyl and piperazine moieties, was prepared and evaluated for dopamine transporter binding affinity with [(3) H] GBR12935 in rat striatal membranes. |
32(0,1,1,2) | Details |
| 11020233 | Hinerth MA, Collins HA, Baniecki M, Hanson RN, Waszczak BL: Novel in vivo electrophysiological assay for the effects of cocaine and putative "cocaine antagonists" on dopamine transporter activity of substantia nigra and ventral tegmental area neurons. Synapse. 2000 Dec 1;38(3):305-12. We next evaluated GBR12909, a piperazine analog promoted as a "cocaine antagonist" because of its ability to bind with high affinity to the DAT, while only modestly elevating extracellular levels. |
2(0,0,0,2) | Details |
| 11053528 | Erikson KM, Jones BC, Beard JL: Iron deficiency alters dopamine transporter functioning in rat striatum. . J Nutr. 2000 Nov;130(11):2831-7. Radioligand binding assays with (3) H-1-(2-(diphenylmethoxy)-ethyl)-4-(3-phenylpropyl) piperazine ((3) H-GBR12935) demonstrated that iron deficiency did not alter the affinity of the ligand for the DAT but did significantly decrease the density of the transporter by 30% in caudate putamen and 20% in nucleus accumbens. |
2(0,0,0,2) | Details |
| 17141211 | Middleton LS, Apparsundaram S, King-Pospisil KA, Dwoskin LP: increases dopamine transporter function in rat striatum through a trafficking-independent mechanism. Eur J Pharmacol. 2007 Jan 12;554(2-3):128-36. Epub 2006 Oct 19. To determine whether the increase in V (max) was due to an increase in dopamine transporter density, [(3) H] GBR 12935 (1-(2-[bis (4-fluorophenyl) methoxy] ethyl)-4-(3-phenylpropyl) piperazine dihydrochloride) binding was performed using rat striatal membranes; no differences were found between and saline-control groups at 5, 10 or 40 min post-injection, indicating that did not increase striatal dopamine transporter density; however, [(3) H] GBR 12935 binding assays determine both cell surface and intracellular dopamine transporter. |
2(0,0,0,2) | Details |
| 12438556 | Huotari M, Santha M, Lucas LR, Karayiorgou M, Gogos JA, Mannisto PT: Effect of uptake inhibition on brain catecholamine levels and locomotion in catechol-O-methyltransferase-disrupted mice. J Pharmacol Exp Ther. 2002 Dec;303(3):1309-16. For dopaminergic neurons, uptake by the high-affinity dopamine transporter (DAT) is the most effective mechanism, and the contribution of glial COMT remains secondary under normal conditions. In the present study we have characterized the role of COMT using COMT-deficient mice in conditions where DAT is inhibited by 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl)-piperazine (GBR 12909) or cocaine. |
1(0,0,0,1) | Details |
| 14640559 | Orjales A, Mosquera R, Toledo A, Pumar MC, Garcia N, Cortizo L, Labeaga L, Innerarity A: Syntheses and binding studies of new [(aryl)(aryloxy) methyl] piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for and (NE) transporters. J Med Chem. 2003 Dec 4;46(25):5512-32. In a wide search program toward new, efficient, and fast-acting antidepressant drugs, we have prepared series of new compounds having an (aryl)(aryloxy) methyl moiety linked directly or through a methylene chain to different substituted and unsubstituted cycles (isoquinoline, piperazine, piperidine, tetrahydropyran, or cyclopentane). Some of these racemic mixtures were resolved to their enantiomers and tested for binding to (NE) transporter (NET), (DA) transporter (DAT), and alpha (2) receptor. |
1(0,0,0,1) | Details |
| 12211084 | Thumen A, Qadri F, Sarkar R, Moser A: GBR-12909 effect on outflow depends on phosphorylation in the caudate nucleus of the rat. Synapse. 2002 Nov;46(2):72-8. Modulation of the (DA) transporter inhibitor GBR-12909 effect on DA release by protein kinases and protein phosphatases was studied in slices of the rat caudate nucleus measuring DA outflow in the superfusate of static chambers. These results suggest a complex and strong influence of phosphorylation on GBR-12909 effects on calcium channel-dependent DA outflow at low-affinity piperazine binding sites in slices of the rat caudate nucleus in vitro. |
1(0,0,0,1) | Details |
| 19285542 | Katagiri N, Abe K, Kitabatake M, Utsunomiya I, Horiguchi Y, Hoshi K, Taguchi K: Single administration of increases the extracellular concentration of in rat striatum. Neuroscience. 2009 Jun 2;160(4):820-8. Epub 2009 Mar 12. These results suggest that systemic administration of a single dose of 1-BnTIQ increases striatal extracellular concentration through activation of dopaminergic nigra striatal neurons via the dopamine transporter. This 1-BnTIQ-induced increase in extracellular concentration was also inhibited by pre-treatment with a uptake inhibitor, GBR12909 (1-(2-[bis (4-Fluorophenyl)-4-(3-phenylpropyl) piperazine dihydrochloride). |
1(0,0,0,1) | Details |
| 14612141 | Dutta AK, Zhang S, Kolhatkar R, Reith ME: Dopamine transporter as target for drug development of cocaine dependence medications. Eur J Pharmacol. 2003 Oct 31;479(1-3):93-106. The following categories of compounds are covered: tropane, benztropine, 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR), methylphenidate, mazindol, and phencyclidine analogs. |
2(0,0,0,2) | Details |
| 16339913 | Chalon S, Hall H, Saba W, Garreau L, Dolle F, Halldin C, Emond P, Bottlaender M, Deloye JB, Helfenbein J, Madelmont JC, Bodard S, Mincheva Z, Besnard JC, Guilloteau D: Pharmacological characterization of (E)-N-(4-fluorobut-2-enyl)-2beta-carbomethoxy-3beta-(4'-tolyl) nortropane (LBT-999) as a highly promising fluorinated ligand for the dopamine transporter. J Pharmacol Exp Ther. 2006 Apr;317(1):147-52. Epub 2005 Dec 9. In vitro on rat striatal membrane, [(3) H] LBT-999 bound to a single site with a K (d) of 9 nM, B (max) of 17 pmol/mg protein, and a very high selectivity for the DAT [IC (50) for 1-{2-[bis-(4-fluorophenyl)-methoxy] ethyl}-4-(3-phenylpropyl) piperazine (GBR 12909) and (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl) nortro pane (PE2I): 2.4 and 18 nM, respectively; IC (50) for paroxetine, N,N-dimethyl-2-(2-amino-4-methylphenyl thio) benzylamine, nisoxetine, and desipramine > 1 muM]. |
2(0,0,0,2) | Details |
| 19197004 | Zolkowska D, Jain R, Rothman RB, Partilla JS, Roth BL, Setola V, Prisinzano TE, Baumann MH: Evidence for the involvement of dopamine transporters in behavioral stimulant effects of modafinil. J Pharmacol Exp Ther. 2009 May;329(2):738-46. Epub 2009 Feb 5. Here, we examined the interaction of modafinil with receptors and transporters in vitro and compared pharmacological effects of the drug with those produced by indirect (DA) agonists 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR12909) and (+)-methamphetamine (METH). |
1(0,0,0,1) | Details |
| 11806716 | Dutta AK, Davis MC, Fei XS, Beardsley PM, Cook CD, Reith ME: Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl) piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules. J Med Chem. 2002 Jan 31;45(3):654-62. A series of substituted N-benzyl analogues of the dopamine transporter (DAT) specific compound, 4-[2-(diphenylmethoxy) ethyl]-1-benzylpiperidine were synthesized and biologically characterized. |
1(0,0,0,1) | Details |
| 15142566 | Kimura M, Masuda T, Yamada K, Mitani M, Kubota N, Kawakatsu N, Kishii K, Inazu M, Kiuchi Y, Oguchi K, Namiki T: Efficient asymmetric syntheses, determination of absolute configurations and biological activities of 1-[4,4-bis (4-fluorophenyl) butyl]-4-[2-hydroxy-3-(phenylamino) propyl] pipera zine as a novel potent uptake inhibitor in the central nervous system. Bioorg Med Chem. 2004 Jun 1;12(11):3069-78. In in vitro pharmacological evaluations, 4a.3HCl and 4b.3HCl showed potent dopamine transporter binding affinities, high moderate and weak uptake inhibitory activities, and 4a.3HCl exhibited a more potent and selective uptake inhibition over the or uptake inhibition as compared with 4b.3HCl. |
1(0,0,0,1) | Details |
| 12742518 | Katz JL, Libby TA, Kopajtic T, Husbands SM, Newman AH: Behavioral effects of rimcazole analogues alone and in combination with cocaine. Eur J Pharmacol. 2003 May 9;468(2):109-19. Several sigma receptor ligands have been reported to also have affinity for the dopamine transporter, among them rimcazole (9-[3-(cis-3,5-dimethyl-1-piperazinyl) propyl] carbazole dihydrochloride). However, rimcazole lacks behavioral effects like those of other uptake inhibitors, such as cocaine and GBR 12909 (1-(2-[bis (4-fluorophenyl) methoxy] ethyl)-4-(3-phenylpropyl) piperazine dihydrochloride). |
1(0,0,0,1) | Details |
| 17090704 | Moy LY, Wang SP, Sonsalla PK: Mitochondrial stress-induced efflux and neuronal damage by involves the dopamine transporter. J Pharmacol Exp Ther. 2007 Feb;320(2):747-56. Epub 2006 Nov 7. Pharmacological blockade of the DAT with a series of structurally different inhibitors [cocaine, mazindol, 1-(2-(bis (4-fluophenyl methoxy) ethyl)-4-(3-(4-fluorophenyl)-propyl) piperazine) dimethane sulfonate (GBR 13098) and methyl (-)-3beta-(p-fluorophenyl)-1alphaH,5alphaH-tropane-2beta-carboxylate 1,5-naphthalene (Win 35,428)] attenuated -induced DA overflow in vivo and protected mice against subsequent damage to DA nerve terminals. |
1(0,0,0,1) | Details |
| 19325033 | Zhu J, Mactutus CF, Wallace DR, Booze RM: HIV-1 Tat protein-induced rapid and reversible decrease in [3H] uptake: dissociation of [3H] uptake and [3H] 2beta-carbomethoxy-3-beta-(4-fluorophenyl) tropane (WIN 35,428) binding in rat striatal synaptosomes. J Pharmacol Exp Ther. 2009 Jun;329(3):1071-83. Epub 2009 Mar 26. (DA) transporter (DAT) function is strikingly altered in patients with HIV-1-associated dementia and a history of chronic drug abuse. Rat striatal synaptosomes were incubated with recombinant Tat (1-86) protein, and [(3) H] DA uptake and the binding of [(3) H] 2beta-carbomethoxy-3-beta-(4-fluorophenyl) tropane (WIN 35,428) and [(3) H] 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl)-piperazine (GBR 12935) were determined. |
1(0,0,0,1) | Details |
| 18557608 | Mahaney PE, Gavrin LK, Trybulski EJ, Stack GP, Vu TA, Cohn ST, Ye F, Belardi JK, Santilli AA, Sabatucci JP, Leiter J, Johnston GH, Bray JA, Burroughs KD, Cosmi SA, Leventhal L, Koury EJ, Zhang Y, Mugford CA, Ho DM, Rosenzweig-Lipson SJ, Platt B, Smith VA, Deecher DC: Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective reuptake inhibitors. J Med Chem. 2008 Jul 10;51(13):4038-49. Epub 2008 Jun 17. These efforts led to the discovery of a piperazine-containing analogue, 17g (WY-46824), that exhibited potent reuptake inhibition, excellent selectivity over the serotonin transporter, but no selectivity over the dopamine transporter. Synthesis and testing of a series of cyclohexanol ethylpiperazines identified ( S)-(-)- 17i (WAY-256805), a potent reuptake inhibitor (IC 50 = 82 nM, K i = 50 nM) that exhibited excellent selectivity over both the and dopamine transporters and was efficacious in animal models of depression, pain, and thermoregulatory dysfunction. |
1(0,0,0,1) | Details |
| 15115806 | Champagne FA, Chretien P, Stevenson CW, Zhang TY, Gratton A, Meaney MJ: Variations in nucleus accumbens associated with individual differences in maternal behavior in the rat. J Neurosci. 2004 Apr 28;24(17):4113-23. Dopamine transporter binding in the n. Injection of the selective DA uptake inhibitor GBR 12909 [1-(2-(Bis-(4-fluorophenyl) methoxy) ethyl)-4-(3 phenypropyl) piperazine dihydrochloride] (5 mg/kg, s.c.) increased the DA signal in the n. |
1(0,0,0,1) | Details |
| 15860577 | Nightingale B, Dersch CM, Boos TL, Greiner E, Calhoun WJ, Jacobson AE, Rice KC, Rothman RB: Studies of the biogenic amine transporters. J Pharmacol Exp Ther. 2005 Aug;314(2):906-15. Epub 2005 Apr 28. Identification of a 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR12909) analog that allosterically modulates the serotonin transporter.. Previous studies identified partial inhibitors of (5-HT) transporter and dopamine transporter binding. |
1(0,0,0,1) | Details |
| 14556232 | Villegier AS, Drouin C, Bizot JC, Marien M, Glowinski J, Colpaert F, Tassin JP: Stimulation of postsynaptic alpha1b- and alpha2-adrenergic receptors amplifies -mediated locomotor activity in both rats and mice. Synapse. 2003 Dec 15;50(4):277-84. To test whether NE release could increase DA-mediated locomotor hyperactivity, rats were treated with GBR 12783 (10 mg/kg), a specific inhibitor of the DA transporter, and NE release was enhanced with dexefaroxan (0.63-10 mg/kg), a potent and specific antagonist at alpha2-adrenergic receptors. |
1(0,0,0,1) | Details |
| 12023554 | Baumann MH, Ayestas MA, Sharpe LG, Lewis DB, Rice KC, Rothman RB: Persistent antagonism of methamphetamine-induced release in rats pretreated with GBR12909 decanoate. J Pharmacol Exp Ther. 2002 Jun;301(3):1190-7. At the molecular level, methamphetamine promotes DA release by a nonexocytotic diffusion-exchange process involving DA transporter (DAT) proteins. We have shown that blocking DAT activity with high-affinity DA uptake inhibitors, such as 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR12909), can substantially reduce amphetamine-induced DA release in vivo. |
1(0,0,0,1) | Details |
| 15111235 | Presgraves SP, Ahmed T, Borwege S, Joyce JN: Terminally differentiated SH-SY5Y cells provide a model system for studying neuroprotective effects of agonists. Neurotox Res. 2004;5(8):579-98. We characterized undifferentiated (UN) and three differentiation conditions of the SH-SY5Y neuroblastoma cell line for phenotypic markers of dopaminergic cells, sensitivity to the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridinium ion (MPP+), the requirement to utilize the (DA) transporter (DAT) for MPP+ toxicity, and the neuroprotective effects of pramipexole. RA/TPA differentiated cells evidenced high sensitivity to the effects of MPP+ (0.03 to 3.0 mM), and the effects of MPP+ were blocked with the DAT inhibitor 1-(2-[bis (4-fluorophenyl) methoxy] ethyl)-4-(3-phenylpropyl) piperazine (GBR 12909). |
1(0,0,0,1) | Details |
| 14978248 | Gaffaney JD, Vaughan RA: Uptake inhibitors but not substrates induce protease resistance in extracellular loop two of the dopamine transporter. Mol Pharmacol. 2004 Mar;65(3):692-701. Changes in protease sensitivity of extracellular loop two (EL2) of the dopamine transporter (DAT) during inhibitor and substrate binding were examined using trypsin proteolysis and epitope-specific immunoblotting. However, in the presence of the uptake blockers [2-(diphenylmethoxyl) ethyl]-4-(3phenylpropyl) piperazine (GBR 12909), mazindol, 2beta-carbomethoxy-3beta-(4-flourophenyl) tropane (beta-CFT), nomifensine, benztropine, or (-)-cocaine, 100- to 1000-fold higher concentrations of trypsin were required to produce comparable levels of proteolysis. |
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| 12747792 | Kolhatkar RB, Ghorai SK, George C, Reith ME, Dutta AK: Interaction of cis-(6-benzhydrylpiperidin-3-yl) benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl) piperidin-4-ylmethyl] amine. J Med Chem. 2003 May 22;46(11):2205-15. One of the enantiomers, compound S,S-(-)-19a, exhibited the highest potency for the DAT (IC50 = 11.3 nM) among all the compounds tested and was as potent as GBR 12909 (1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine). All novel compounds were tested for their affinity at the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET) in the brain by measuring their potency in competing for the binding of [3H] WIN 35 428, [3H] and [3H] nisoxetine, respectively. |
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| 14724217 | Choong KC, Shen RY: Methylphenidate restores ventral tegmental area neuron activity in prenatal -exposed rats by augmenting neurotransmission. J Pharmacol Exp Ther. 2004 May;309(2):444-51. Epub 2004 Jan 14. The effect of methylphenidate was mediated by increased extracellular levels of DA instead of because this effect was not altered by the coadministration of prazosin, an alpha (1) receptor antagonist, and was mimicked by the application of DA transporter blockers, nomifensine and 1-2 (-[bis (4-flurophenyl) methoxy] ethyl)-4-(3-phenyl) piperazine dihydrochloride (GBR 12909). |
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| 18606182 | Aksenov MY, Aksenova MV, Silvers JM, Mactutus CF, Booze RM: Different effects of selective uptake inhibitors, GBR 12909 and WIN 35428, on HIV-1 Tat toxicity in rat fetal midbrain neurons. Neurotoxicology. 2008 Nov;29(6):971-7. Epub 2008 Jun 19. In this study, we found that the selective inhibitor of dopamine transporter (DAT) function, 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909, vanoxerine), but not the selective inhibitors of and (SERT and NET) transporters, and nizoxetine, emulated cocaine-mediated enhancement of Tat neurotoxicity in rat fetal midbrain primary cell cultures. |
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| 15496938 | Baumann MH, Clark RD, Budzynski AG, Partilla JS, Blough BE, Rothman RB: N-substituted piperazines abused by humans mimic the molecular mechanism of 3,4-methylenedioxymethamphetamine (MDMA, or 'Ecstasy'). Neuropsychopharmacology. 2005 Mar;30(3):550-60. Recent evidence reveals that drug users are ingesting piperazine analogs, like 1-benzylpiperazine (BZP, or 'A2') and 1-(m-trifluoromethylphenyl) piperazine (TFMPP, or 'Molly'), to mimic psychoactive effects of MDMA. The effects of MDMA, BZP, and TFMPP on transporter-mediated efflux of [3H] and [3H] MPP+ (DA transporter substrate) were determined in synaptosomes. |
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| 15542717 | Baumann MH, Clark RD, Budzynski AG, Partilla JS, Blough BE, Rothman RB: Effects of "Legal X" piperazine analogs on and release in rat brain. Ann N Y Acad Sci. 2004 Oct;1025:189-97. The ability of MDMA, BZP, and TFMPP to stimulate efflux of [3H] and [3H] MPP+ (a DA transporter substrate) was determined in vitro using release assays in synaptosomes. |
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| 11230993 | Rahman S, Engleman E, Simon J, McBride WJ: Negative interaction of dopamine D2 receptor antagonists and GBR 12909 and GBR 12935 uptake inhibitors in the nucleus accumbens. Eur J Pharmacol. 2001 Feb 23;414(1):37-44. Perfusion of the nucleus accumbens for 60 min with the uptake inhibitors, 1-[2-[bis (4-Fluorophenyl) methoxy] ethyl]-4-[3-phenylpropyl] piperazine dihydrochloride (GBR 12909; 100 microm) or 1-[2-(Diphenylmethoxy) ethyl]-4-(3-phenylpropyl)-piperazine dihydrochloride (GBR 12935; 100 microm) alone, increased the extracellular levels of in the nucleus accumbens to 400% and 350% of basal, respectively. |
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| 16385509 | Minuzzi L, Olsen AK, Bender D, Arnfred S, Grant R, Danielsen EH, Cumming P: Quantitative autoradiography of ligands for receptors and transporters in brain of Gottingen minipig: comparison with results in vivo. Synapse. 2006 Mar 15;59(4):211-9. However, well-characterized piperazine and tropane radioligands failed to recognize DAT in pig brain; the two tropane radioligands lacked pharmacological specificity for DAT and SERT in pig brain in vitro and in vivo. |
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| 11578899 | Ishiwata K, Kobayashi T, Kawamura K, Matsuno K, Senda M: [11C] Raclopride binding was reduced in vivo by sigma (1) receptor ligand SA4503 in the mouse brain, while [11C] SA4503 binding was not by raclopride. Nucl Med Biol. 2001 Oct;28(7):787-92. [11C] Raclopride is widely used as a representative D (2)-like receptor ligand in positron emission tomography (PET) studies, and [11C] 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl) piperazine dihydrochloride ([11C] SA4503) is a recently developed selective ligand for mapping sigma (1) receptors in the brain. |
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| 12504872 | Nakai M, Mori A, Watanabe A, Mitsumoto Y: 1-methyl-4-phenylpyridinium (MPP+) decreases mitochondrial oxidation-reduction (REDOX) activity and membrane potential (Deltapsi (m)) in rat striatum. Exp Neurol. 2003 Jan;179(1):103-10. Both measures of mitochondrial dysfunction induced by MPP+ (40 nmol) at 18 h were attenuated, at least in part, by pretreatment with a selective uptake inhibitor GBR-12909 (1-(2-(bis (4-fluorophenyl) methoxy) ethyl)-4-(3-phenylpropyl) piperazine). |
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