Target Validation Information
Target ID T21945
Target Name Sodium-dependent noradrenaline transporter
Target Type
Successful
Drug Potency against Target Trimipramine Drug Info IC50 = 1000 nM [1]
Diethylpropion Drug Info IC50 = 18100 nM [2]
Reboxetine Drug Info IC50 = 8 nM [3]
Phenmetrazine Drug Info EC50 = 50 nM [4]
Desipramine Drug Info IC50 = 3.4 nM [5]
WAY-256805 Drug Info IC50 = 82 nM [6]
R-sibutramine metabolite Drug Info Ki = 66 nM [7]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 21 nM [8]
MDL-28618 Drug Info IC50 = 880 nM [9]
((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine Drug Info IC50 = 46 nM [9]
1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine Drug Info Ki = 747 nM [10]
4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine Drug Info Ki = 1940 nM [8]
1-(2-phenoxyphenyl)piperazine Drug Info Ki = 554 nM [8]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info Ki = 9 nM [8]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 292 nM [10]
POLYGALATENOSIDE B Drug Info IC50 = 6040 nM [11]
2-(2,3-Dihydro-1H-indol-5-yl)-1-methyl-ethylamine Drug Info IC50 = 360 nM [12]
N,N-dimethyl(2-phenoxyphenyl)methanamine Drug Info IC50 = 70 nM [13]
(R)-1-((S)-morpholin-2-yl)-1,2-diphenylethanol Drug Info Ki = 148 nM [14]
Mazindol Drug Info ED50 = 1.5 nM [15]
{2-[3-(Phenylsulfonyl)-1H-indol-4-yl]ethyl}amine Drug Info IC50 = 960 nM [16]
Duloxetine Drug Info Ki = 4.6 nM [17]
D-211B Drug Info Ki = 418 nM [18]
2-((2-iodophenoxy)(phenyl)methyl)morpholine Drug Info Ki = 2.47 nM [19]
NISOXETINE Drug Info IC50 = 6 nM [20]
METHYLENEDIOXYAMPHETAMINE Drug Info IC50 = 266 nM [21]
DOV-216303 Drug Info Ki = 20.3 nM [22]
1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 9.4 nM [23]
PYROVALERONE Drug Info IC50 = 28.3 nM [23]
DOV 21947 Drug Info Ki = 22.8 nM [24]
Bupropion Drug Info Ki = 1900 nM [25]
Nortriptyline Drug Info IC50 = 177 nM [26]
N-(2-oxazolemethyl)milnacipran Drug Info IC50 = 450 nM [27]
PF-3409409 Drug Info Ki = 6 nM [28]
1-(3,4-dichlorophenyl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 72.4 nM [29]
Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine Drug Info Ki = 271 nM [30]
RTI-219 Drug Info IC50 = 750 nM [31]
(R)-Norfluoxetine Drug Info IC50 = 1995 nM [32]
Radaxafine HCl Drug Info IC50 = 1400 nM [33]
3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine Drug Info IC50 = 47 nM [34]
2-Amino-1-(4-methylthiophenyl)propane Drug Info IC50 = 2375 nM [35]
4-(2-(benzyloxy)phenyl)piperidine Drug Info Ki = 76 nM [8]
2-(N-tert-Butylamino)-3',4'-dichloropropiophenone Drug Info Ki = 5400 nM [36]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 74 nM [10]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 18 nM [8]
2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one Drug Info IC50 = 607 nM [37]
1-(3-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 5600 nM [37]
2-(N-Cyclopentylamino)-3'-fluoropropiophenone Drug Info IC50 = 2850 nM [37]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 11 nM [8]
(S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 200 nM [38]
2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran Drug Info IC50 = 2322 nM [39]
Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 840 nM [40]
2-((3-iodophenyl)(o-tolyloxy)methyl)morpholine Drug Info Ki = 27.6 nM [19]
2-(N-tert-Butylamino)propiophenone Drug Info Ki = 5700 nM [36]
2-(N-tert-Butylamino)-3'-chloropentanophenone Drug Info IC50 = 472 nM [36]
2-(N-Pyrrolidinyl)-3'-methoxypropiophenone Drug Info IC50 = 718 nM [37]
2-(N-tert-Butylamino)-3'-chlorooctanophenone Drug Info IC50 = 4890 nM [36]
WIN_35428 Drug Info IC50 = 1230 nM [41]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info Ki = 31 nM [42]
(S)-NORDULOXETINE Drug Info IC50 = 445 nM [43]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 300 nM [44]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine Drug Info Ki = 32 nM [10]
2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 73 nM [44]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 180 nM [42]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 536 nM [10]
2-(Aminomethyl)-5-phenethyltetrahydrofuran Drug Info IC50 = 360 nM [39]
2-Aminomethyl-5-(phenyl)tetrahydrofuran Drug Info IC50 = 23 nM [39]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 2900 nM [38]
1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 54 nM [44]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info Ki = 183 nM [8]
1-(4-fluorophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 171 nM [23]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info Ki = 1710 nM [8]
1-(2-(2-bromophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 35 nM [44]
2-(N-Pyrrolidinyl)-3'-methylpropiophenone Drug Info IC50 = 577 nM [37]
1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one Drug Info IC50 = 2520 nM [37]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine Drug Info Ki = 526 nM [8]
1-(1,4-diphenylbutan-2-yl)piperazine Drug Info IC50 = 48 nM [45]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine Drug Info Ki = 330 nM [10]
1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 130 nM [44]
4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 170 nM [8]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info Ki = 170 nM [8]
4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 115 nM [8]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info Ki = 13 nM [8]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info Ki = 1330 nM [46]
2-(N-Pyrrolidinyl)-3'-fluoropropiophenone Drug Info IC50 = 135 nM [37]
AMIFLAMINE Drug Info IC50 = 650 nM [12]
1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 2540 nM [37]
2-(tert-butylamino)-1-p-tolylpropan-1-one Drug Info IC50 = 2350 nM [37]
1-(3-chlorophenyl)-2-(dimethylamino)propan-1-one Drug Info IC50 = 1520 nM [37]
PF-526014 Drug Info Ki = 12 nM [42]
Bicifadine Drug Info IC50 = 55 nM [47]
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine Drug Info Ki = 104 nM [8]
(R)-DULOXETINE Drug Info IC50 = 13.2 nM [43]
1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 22 nM [44]
4-(2-(phenoxymethyl)phenyl)piperidine Drug Info Ki = 1710 nM [8]
Para-chloroamphetamine Drug Info IC50 = 207 nM [35]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info IC50 = 14 nM [44]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info IC50 = 405 nM [35]
1-(1-phenyl-2-o-tolylethyl)piperazine Drug Info IC50 = 90 nM [44]
2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran Drug Info IC50 = 59 nM [39]
1-(1,2-diphenylethyl)piperazine Drug Info IC50 = 39 nM [44]
1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 46.5 nM [23]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info Ki = 24 nM [46]
1-(2-(2-ethoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 16 nM [44]
2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran Drug Info IC50 = 58 nM [39]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 97 nM [8]
1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 11.7 nM [23]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 5.2 nM [48]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 34 nM [8]
1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 72 nM [44]
2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran Drug Info IC50 = 210 nM [39]
(R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 7500 nM [49]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 1200 nM [49]
2-(tert-Butylamino)-3',4'-dichlorobutyrophenone Drug Info IC50 = 135 nM [36]
1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 19.7 nM [23]
PF-18298 Drug Info Ki = 21 nM [42]
(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info Ki = 58 nM [42]
S-34324 Drug Info Ki = 365 nM [50]
Imipramine Drug Info pKi < 5 [51]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info Ki = 11 nM [46]
D-211A Drug Info Ki = 388 nM [18]
D-257A Drug Info Ki = 954 nM [18]
R-NORDULOXETINE Drug Info IC50 = 188 nM [43]
DIFLUOROBENZTROPINE Drug Info Ki = 844 nM [52]
1-(2-(3-fluorophenoxy)phenyl)piperazine Drug Info Ki = 1720 nM [8]
1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 81 nM [23]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info Ki = 1370 nM [8]
1-(2-(benzyloxy)phenyl)piperazine Drug Info Ki = 168 nM [8]
2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran Drug Info IC50 = 61 nM [39]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info Ki = 9 nM [8]
2-(N-Cyclopentylamino)-3'-bromopropiophenone Drug Info IC50 = 2530 nM [37]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info Ki = 2980 nM [52]
2-(tert-butylamino)-1-m-tolylpropan-1-one Drug Info IC50 = 6200 nM [37]
2-(2'-Aminoethyl)-5-benzyltetrahydrofuran Drug Info IC50 = 347 nM [39]
2-(N-Cyclopentylamino)-3'-methoxypropiophenone Drug Info IC50 = 8200 nM [37]
N-benzyl-N-isobutylpiperidin-4-amine Drug Info Ki = 91 nM [53]
Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine Drug Info Ki = 69 nM [53]
1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine Drug Info Ki = 18 nM [42]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 4400 nM [38]
2-(N,N-Diethylamino)-3'-chloropropiophenone Drug Info Ki = 4476 nM [36]
2-(N-tert-Butylamino)-3'-chloroheptanophenone Drug Info Ki = 4300 nM [36]
2-(tert-Butylamino)-3',4'-dichloropentanophenone Drug Info IC50 = 43 nM [36]
2-(N-tert-Butylamino)-3'-chlorohexanophenone Drug Info Ki = 3190 nM [36]
2-(N-Cyclopropylamino)-3-chloropropiophenone Drug Info Ki = 4000 nM [36]
2-(N-Pyrrolidinyl)-3'-nitropropiophenone Drug Info IC50 = 4100 nM [37]
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info Ki = 2440 nM [10]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [54]
2-(N-Cyclopentylamino)-3'-methylpropiophenone Drug Info IC50 = 8700 nM [37]
1-(2,3-Dihydro-1H-indol-5-ylmethyl)-propylamine Drug Info IC50 = 500 nM [12]
1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 83 nM [23]
2-(N-Cyclopentylamino)-3'-chloropropiophenone Drug Info Ki = 5700 nM [36]
(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine Drug Info IC50 = 1400 nM [38]
4-(2-phenoxyphenyl)piperidine Drug Info Ki = 416 nM [8]
2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran Drug Info IC50 = 92 nM [39]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info Ki = 3 nM [8]
(S)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 24 nM [49]
2pyrrolidin-1-yl-1-phenylpentan-1-one Drug Info IC50 = 56 nM [23]
2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran Drug Info IC50 = 3420 nM [39]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 162 nM [8]
6-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 1900 nM [38]
LITOXETINE Drug Info IC50 = 1400 nM [49]
(R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 772 nM [38]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine Drug Info IC50 = 10500 nM [38]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 17 nM [42]
Levomilnacipran Drug Info IC50 = 100 nM [17]
2-(N-Pyrrolidinyl)-3'-bromopropiophenone Drug Info IC50 = 1180 nM [37]
D-257C Drug Info Ki = 319 nM [18]
1S,2R-milnacipran Drug Info IC50 = 40 nM [55]
(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 1130 nM [56]
D-166A Drug Info Ki = 730 nM [18]
D-254C Drug Info Ki = 170 nM [18]
1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 531 nM [23]
Reboxetine Drug Info Ki = 1.04 nM [57]
(S)-Norfluoxetine Drug Info IC50 = 2806 nM [32]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 30 nM [42]
Desvenalfaxine succinate Drug Info Ki = 558.4 nM [58]
WIN-35065-2 Drug Info IC50 = 920 nM [41]
KF-A5 Drug Info IC50 = 9100 nM [59]
Phentermine Drug Info EC50 = 39.4 nM [60]
Venlafaxine Drug Info Ki = 640 nM [61]
WIN-35066-2 Drug Info Ki = 550 nM [62]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 550 nM [56]
Cis-3-phenoxy-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 5000 nM [40]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info IC50 = 1800 nM [38]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 1200 nM [38]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 160 nM [48]
Action against Disease Model Sibutramine Uptake of 3H-dopamine in rat whole brain synaptosomes IC50: 2000 nM [63] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Extracellular clearance rate pof NET prolonged (sixfold);Amplitude of stimulated release of NET decreased by 55%;Basal extracellular of NET elevated twofold;Tissue content of NET decreased by 55%-75%;Synthesis rate of NET elevated by 70%;Postsynaptic receptors of NET is down-regulated [6]
References
REF 1Uptake inhibition of biogenic amines by newer antidepressant drugs: relevance to the dopamine hypothesis of depression. Psychopharmacology (Berl). 1977 Aug 16;53(3):309-14.
REF 2Uptake and release effects of diethylpropion and its metabolites with biogenic amine transporters. Bioorg Med Chem. 2000 Dec;8(12):2689-92.
REF 3Mirtazapine decreases stimulatory effects of reboxetine on cortisol, adrenocorticotropin and prolactin secretion in healthy male subjects. Neuroendocrinology. 2004 Jan;79(1):54-62.
REF 4Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain. Eur J Pharmacol. 2002 Jun 28;447(1):51-7.
REF 5Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231). J Med Chem. 2010 Jun 10;53(11):4511-21. doi: 10.1021/jm100053t.
REF 6J Med Chem. 2008 Jul 10;51(13):4038-49. Epub 2008 Jun 17.Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.
REF 7The contribution of metabolites to the rapid and potent down-regulation of rat cortical beta-adrenoceptors by the putative antidepressant sibutramine hydrochloride. Neuropharmacology. 1989 Feb;28(2):129-34.
REF 8Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7. Epub 2009 Oct 12.Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
REF 9Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8. Epub 2008 Jul 17.Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.
REF 10Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7. Epub 2009 Dec 6.Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
REF 11J Nat Prod. 2006 Sep;69(9):1305-9.Antidepressant principles of the roots of Polygala tenuifolia.
REF 12J Med Chem. 1986 Aug;29(8):1406-12.Selective monoamine oxidase inhibitors. 3. Cyclic compounds related to 4-aminophenethylamine. Preparation and neuron-selective action of some 5-(2-aminoethyl)-2,3-dihydroindoles.
REF 13Bioorg Med Chem Lett. 2008 Jan 15;18(2):596-9.1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.
REF 14Bioorg Med Chem Lett. 2006 Apr 1;16(7):2022-5. Epub 2006 Jan 18.Discovery of novel and selective tertiary alcohol containing inhibitors of the norepinephrine transporter.
REF 15Studies on the capacity of mazindol and dita to act as uptake inhibitors or releasing agents for 3H-biogenic amines in rat brain tissue slices. Eur J Pharmacol. 1977 Oct 15;45(4):329-33.
REF 16Bioorg Med Chem. 2009 Nov 15;17(22):7802-15. Epub 2009 Sep 18.Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.
REF 17J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
REF 18Bioorg Med Chem. 2008 Mar 15;16(6):2769-78. Epub 2008 Jan 11.Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an exocyclic hydroxyl group: interaction with dopamine, serotonin, and norepinephrine transporters.
REF 19Bioorg Med Chem Lett. 2007 Jan 15;17(2):533-7. Epub 2006 Oct 12.Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER.
REF 20Bioorg Med Chem Lett. 2008 Sep 15;18(18):4929-31. Epub 2008 Aug 22.Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.
REF 21Bioorg Med Chem. 2010 Jun 1;18(11):4009-31. Epub 2010 Apr 13.Synthesis and in vitro toxicity of 4-MTA, its characteristic clandestine synthesis byproducts and related sulfur substituted alpha-alkylthioamphetamines.
REF 22J Clin Pharmacol. 2004 Dec;44(12):1360-7.DOV 216,303, a "triple" reuptake inhibitor: safety, tolerability, and pharmacokinetic profile.
REF 23J Med Chem. 2006 Feb 23;49(4):1420-32.1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.
REF 24Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104.
REF 25BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000. doi: 10.1038/nrd2658.
REF 268-hydroxy-2-(di-n-propylamino)tetralin-responsive 5-hydroxytryptamine4-like receptor expressed in bovine pulmonary artery smooth muscle cells. Mol Pharmacol. 1992 Nov;42(5):817-25.
REF 27Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9. Epub 2008 Jan 9.Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
REF 28Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83. Epub 2009 Jul 2.Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.
REF 29Bioorg Med Chem Lett. 2010 Sep 15;20(18):5567-71. Epub 2010 Aug 17.Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
REF 30Bioorg Med Chem Lett. 2008 Aug 1;18(15):4355-9. Epub 2008 Jun 25.Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.
REF 31J Med Chem. 2007 Jul 26;50(15):3686-95. Epub 2007 Jun 30.Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.
REF 32Bioorg Med Chem. 2009 Jan 1;17(1):337-43. Epub 2008 Nov 5.Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression.
REF 33Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Curr Opin Pharmacol. 2007 Dec;7(6):583-92. Epub 2007 Nov 9.
REF 34Bioorg Med Chem Lett. 2008 Dec 1;18(23):6067-70. Epub 2008 Oct 11.Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
REF 35Eur J Med Chem. 2009 Dec;44(12):4862-88. Epub 2009 Aug 6.Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.
REF 36J Med Chem. 2009 Nov 12;52(21):6768-81.Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction.
REF 37J Med Chem. 2010 Mar 11;53(5):2204-14.Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.
REF 38Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. Epub 2009 Feb 20.Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.
REF 39Bioorg Med Chem. 2009 Mar 1;17(5):2047-68. Epub 2009 Jan 15.2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors.
REF 40Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7. Epub 2008 May 20.Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
REF 41J Med Chem. 1996 Oct 11;39(21):4139-41.3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter.
REF 42Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. Epub 2010 Apr 18.Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
REF 43Bioorg Med Chem. 2009 Oct 1;17(19):6890-7. Epub 2009 Aug 20.Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents fordepression.
REF 44Bioorg Med Chem Lett. 2006 Aug 15;16(16):4345-8. Epub 2006 Jun 5.N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.
REF 45Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53. Epub 2006 Jun 5.Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.
REF 46J Med Chem. 2004 May 6;47(10):2624-34.Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters.
REF 47Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6. Epub 2008 May 23.Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
REF 48Bioorg Med Chem Lett. 2000 Nov 6;10(21):2445-7.3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter.
REF 49Bioorg Med Chem Lett. 2009 Oct 15;19(20):5893-7. Epub 2009 Aug 21.Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.
REF 50J Med Chem. 2005 Mar 24;48(6):2054-71.Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
REF 51Multi-target strategies for the improved treatment of depressive states: Conceptual foundations and neuronal substrates, drug discovery and therapeutic application. Pharmacol Ther. 2006 May;110(2):135-370. Epub 2006 Mar 7.
REF 52J Med Chem. 2006 Oct 19;49(21):6391-9.Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
REF 53Bioorg Med Chem Lett. 2006 May 15;16(10):2714-8. Epub 2006 Feb 23.N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake.
REF 54J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
REF 55J Med Chem. 2008 Nov 27;51(22):7265-72.Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
REF 56J Med Chem. 2010 Jun 24;53(12):4731-48.Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
REF 57J Med Chem. 2009 Jan 8;52(1):62-73.Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomography radioligands for in vivo imaging of the norepinephrine transporter.
REF 58Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65. Epub 2006 May 4.
REF 59Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40. Epub 2007 Sep 10.Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
REF 60Therapeutic potential of monoamine transporter substrates. Curr Top Med Chem. 2006;6(17):1845-59.
REF 61Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 62J Med Chem. 2004 Dec 2;47(25):6401-9.Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
REF 63Effects of sibutramine on the central dopaminergic system in rodents. Neurotox Res. 2001 Jul;3(3):235-47.

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