| Name | norepinephrine transporter |
|---|---|
| Synonyms | NAT1; NAT1; NET1; NET; Norepinephrine transporter; Norepinephrine transporter protein 1; SLC6A2; SLC6A5… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 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). |
81(1,1,1,1) | 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. Novel compounds were tested for their binding affinity at the and norepinephrine transporter systems in the brain by competing for [(3) H] WIN 35 428, [(3) H] and [(3) H] nisoxetine, respectively. |
1(0,0,0,1) | 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). Newly synthesized compounds were characterized for their binding affinity at the and norepinephrine transporter systems in rat brain. |
1(0,0,0,1) | 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. A series of 4-[2-[bis (4-fluorophenyl) methoxy] ethyl-1-benzylpiperidines were examined for their ability to bind to the dopamine transporter (DAT), the serotonin transporter (SERT), and the norepinephrine transporter (NET). |
1(0,0,0,1) | 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. A series of 4-[2-[bis (4-fluorophenyl) methoxy] ethylpiperidines were examined for their ability to bind to the dopamine transporter (DAT), the norepinephrine transporter, and the serotonin transporter (SERT). |
1(0,0,0,1) | Details |
| 15763140 | Reith ME, Wang LC, Dutta AK: Pharmacological profile of radioligand binding to the norepinephrine transporter: instances of poor indication of functional activity. J Neurosci Methods. 2005 Apr 15;143(1):87-94. Binding assays for the (NE) transporter (NET) with [3H] nisoxetine have generally yielded weak potencies for compounds related to cocaine and 1-(2-(di (4-fluorophenyl)-methoxy)-ethyl)-4-(3-phenylpropyl) piperazine (GBR 12909), as compared with their functional activity in inhibiting NE uptake. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |