Target Validation Information
TTD ID T21945
Target Name Norepinephrine transporter (NET)
Type of Target
Successful
Drug Potency against Target Amfepramone Drug Info IC50 = 18100 nM [50]
Bupropion Drug Info Ki = 1900 nM [59]
Desipramine Drug Info IC50 = 3.4 nM [60]
Desvenalfaxine succinate Drug Info Ki = 558.4 nM [56]
Duloxetine Drug Info Ki = 4.6 nM [6]
Imipramine Drug Info pKi < 5 [55]
Levomilnacipran Drug Info IC50 = 100 nM [6]
Mazindol Drug Info ED50 = 1.5 nM [63]
Nortriptyline Drug Info IC50 = 177 nM [52]
Phenmetrazine Drug Info EC50 = 50 nM [48]
Phentermine Drug Info EC50 = 39.4 nM [57]
Reboxetine Drug Info IC50 = 8 nM [53]
Trimipramine Drug Info IC50 = 1000 nM [62]
Venlafaxine Drug Info Ki = 640 nM [49]
Drug Info Ki = 22.8 nM [51]
Bicifadine Drug Info IC50 = 55 nM [20]
DOV-216303 Drug Info Ki = 20.3 nM [3]
R-sibutramine metabolite Drug Info Ki = 66 nM [61]
Spiroglumide Drug Info IC50 = 1400 nM [58]
Drug Info IC50 = 72.4 nM [45]
Drug Info IC50 = 920 nM [47]
((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine Drug Info IC50 = 46 nM [24]
(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine Drug Info IC50 = 1400 nM [31]
(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 1130 nM [43]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 550 nM [43]
(R)-1-((S)-morpholin-2-yl)-1,2-diphenylethanol Drug Info Ki = 148 nM [7]
(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info Ki = 58 nM [42]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 1200 nM [31]
(R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 772 nM [31]
(R)-DULOXETINE Drug Info IC50 = 13.2 nM [35]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 1200 nM [34]
(R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 7500 nM [34]
(R)-Norfluoxetine Drug Info IC50 = 1995 nM [28]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 2900 nM [31]
(S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 200 nM [31]
(S)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 24 nM [34]
(S)-NORDULOXETINE Drug Info IC50 = 445 nM [35]
(S)-Norfluoxetine Drug Info IC50 = 2806 nM [28]
1-(1,2-diphenylethyl)piperazine Drug Info IC50 = 39 nM [10]
1-(1,4-diphenylbutan-2-yl)piperazine Drug Info IC50 = 48 nM [11]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 17 nM [42]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 30 nM [42]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info Ki = 31 nM [42]
1-(1-phenyl-2-o-tolylethyl)piperazine Drug Info IC50 = 90 nM [10]
1-(2,3-Dihydro-1H-indol-5-ylmethyl)-propylamine Drug Info IC50 = 500 nM [46]
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine Drug Info Ki = 104 nM [38]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 180 nM [42]
1-(2-(2-bromophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 35 nM [10]
1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine Drug Info Ki = 747 nM [39]
1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 22 nM [10]
1-(2-(2-ethoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 16 nM [10]
1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 72 nM [10]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine Drug Info Ki = 526 nM [38]
1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine Drug Info Ki = 18 nM [42]
1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 54 nM [10]
1-(2-(3-fluorophenoxy)phenyl)piperazine Drug Info Ki = 1720 nM [38]
1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 130 nM [10]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info Ki = 1710 nM [38]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine Drug Info IC50 = 10500 nM [31]
1-(2-(benzyloxy)phenyl)piperazine Drug Info Ki = 168 nM [38]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info Ki = 183 nM [38]
1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 19.7 nM [8]
1-(2-phenoxyphenyl)piperazine Drug Info Ki = 554 nM [38]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info Ki = 1330 nM [2]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info Ki = 24 nM [2]
1-(3-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 5600 nM [40]
1-(3-chlorophenyl)-2-(dimethylamino)propan-1-one Drug Info IC50 = 1520 nM [40]
1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one Drug Info IC50 = 2520 nM [40]
1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 81 nM [8]
1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 9.4 nM [8]
1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 2540 nM [40]
1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 83 nM [8]
1-(4-fluorophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 171 nM [8]
1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 46.5 nM [8]
1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 531 nM [8]
1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 11.7 nM [8]
1S,2R-milnacipran Drug Info IC50 = 40 nM [27]
2-((2-iodophenoxy)(phenyl)methyl)morpholine Drug Info Ki = 2.47 nM [14]
2-((3-iodophenyl)(o-tolyloxy)methyl)morpholine Drug Info Ki = 27.6 nM [14]
2-(2'-Aminoethyl)-5-benzyltetrahydrofuran Drug Info IC50 = 347 nM [30]
2-(2,3-Dihydro-1H-indol-5-yl)-1-methyl-ethylamine Drug Info IC50 = 360 nM [46]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 74 nM [39]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 536 nM [39]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 292 nM [39]
2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 73 nM [10]
2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran Drug Info IC50 = 3420 nM [30]
2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran Drug Info IC50 = 210 nM [30]
2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran Drug Info IC50 = 58 nM [30]
2-(Aminomethyl)-5-phenethyltetrahydrofuran Drug Info IC50 = 360 nM [30]
2-(N,N-Diethylamino)-3'-chloropropiophenone Drug Info Ki = 4476 nM [36]
2-(N-Cyclopentylamino)-3'-bromopropiophenone Drug Info IC50 = 2530 nM [40]
2-(N-Cyclopentylamino)-3'-chloropropiophenone Drug Info Ki = 5700 nM [36]
2-(N-Cyclopentylamino)-3'-fluoropropiophenone Drug Info IC50 = 2850 nM [40]
2-(N-Cyclopentylamino)-3'-methoxypropiophenone Drug Info IC50 = 8200 nM [40]
2-(N-Cyclopentylamino)-3'-methylpropiophenone Drug Info IC50 = 8700 nM [40]
2-(N-Cyclopropylamino)-3-chloropropiophenone Drug Info Ki = 4000 nM [36]
2-(N-Pyrrolidinyl)-3'-bromopropiophenone Drug Info IC50 = 1180 nM [40]
2-(N-Pyrrolidinyl)-3'-fluoropropiophenone Drug Info IC50 = 135 nM [40]
2-(N-Pyrrolidinyl)-3'-methoxypropiophenone Drug Info IC50 = 718 nM [40]
2-(N-Pyrrolidinyl)-3'-methylpropiophenone Drug Info IC50 = 577 nM [40]
2-(N-Pyrrolidinyl)-3'-nitropropiophenone Drug Info IC50 = 4100 nM [40]
2-(N-tert-Butylamino)-3',4'-dichloropropiophenone Drug Info Ki = 5400 nM [36]
2-(N-tert-Butylamino)-3'-chloroheptanophenone Drug Info Ki = 4300 nM [36]
2-(N-tert-Butylamino)-3'-chlorohexanophenone Drug Info Ki = 3190 nM [36]
2-(N-tert-Butylamino)-3'-chlorooctanophenone Drug Info IC50 = 4890 nM [36]
2-(N-tert-Butylamino)-3'-chloropentanophenone Drug Info IC50 = 472 nM [36]
2-(N-tert-Butylamino)propiophenone Drug Info Ki = 5700 nM [36]
2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one Drug Info IC50 = 607 nM [40]
2-(tert-butylamino)-1-m-tolylpropan-1-one Drug Info IC50 = 6200 nM [40]
2-(tert-butylamino)-1-p-tolylpropan-1-one Drug Info IC50 = 2350 nM [40]
2-(tert-Butylamino)-3',4'-dichlorobutyrophenone Drug Info IC50 = 135 nM [36]
2-(tert-Butylamino)-3',4'-dichloropentanophenone Drug Info IC50 = 43 nM [36]
2-Amino-1-(4-methylthiophenyl)propane Drug Info IC50 = 2375 nM [33]
2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran Drug Info IC50 = 59 nM [30]
2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran Drug Info IC50 = 61 nM [30]
2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran Drug Info IC50 = 92 nM [30]
2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran Drug Info IC50 = 2322 nM [30]
2-Aminomethyl-5-(phenyl)tetrahydrofuran Drug Info IC50 = 23 nM [30]
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info Ki = 2440 nM [39]
2pyrrolidin-1-yl-1-phenylpentan-1-one Drug Info IC50 = 56 nM [8]
3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine Drug Info IC50 = 47 nM [26]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 300 nM [10]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info IC50 = 14 nM [10]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine Drug Info Ki = 330 nM [39]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 5.2 nM [1]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info Ki = 2980 nM [13]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info IC50 = 1800 nM [31]
4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine Drug Info Ki = 1940 nM [38]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info Ki = 3 nM [38]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 34 nM [38]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info Ki = 13 nM [38]
4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 170 nM [38]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 11 nM [38]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 162 nM [38]
4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 115 nM [38]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 21 nM [38]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info Ki = 9 nM [38]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info Ki = 9 nM [38]
4-(2-(benzyloxy)phenyl)piperidine Drug Info Ki = 76 nM [38]
4-(2-(phenoxymethyl)phenyl)piperidine Drug Info Ki = 1710 nM [38]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine Drug Info Ki = 32 nM [39]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 18 nM [38]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 97 nM [38]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info Ki = 170 nM [38]
4-(2-phenoxyphenyl)piperidine Drug Info Ki = 416 nM [38]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info Ki = 1370 nM [38]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [44]
6-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 1900 nM [31]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 4400 nM [31]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 160 nM [1]
AMIFLAMINE Drug Info IC50 = 650 nM [46]
Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine Drug Info Ki = 271 nM [23]
Cis-3-phenoxy-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 5000 nM [21]
D-166A Drug Info Ki = 730 nM [19]
D-211A Drug Info Ki = 388 nM [19]
D-211B Drug Info Ki = 418 nM [19]
D-254C Drug Info Ki = 170 nM [19]
D-257A Drug Info Ki = 954 nM [19]
D-257C Drug Info Ki = 319 nM [19]
Difluorobenztropine Drug Info Ki = 844 nM [13]
Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine Drug Info Ki = 69 nM [9]
KF-A5 Drug Info IC50 = 9100 nM [16]
LITOXETINE Drug Info IC50 = 1400 nM [34]
MDL-28618 Drug Info IC50 = 880 nM [24]
METHYLENEDIOXYAMPHETAMINE Drug Info IC50 = 266 nM [41]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info IC50 = 405 nM [33]
N,N-dimethyl(2-phenoxyphenyl)methanamine Drug Info IC50 = 70 nM [18]
N-(2-oxazolemethyl)milnacipran Drug Info IC50 = 450 nM [17]
N-benzyl-N-isobutylpiperidin-4-amine Drug Info Ki = 91 nM [9]
NISOXETINE Drug Info IC50 = 6 nM [25]
Para-chloroamphetamine Drug Info IC50 = 207 nM [33]
PF-18298 Drug Info Ki = 21 nM [42]
PF-3409409 Drug Info Ki = 6 nM [32]
PF-526014 Drug Info Ki = 12 nM [42]
POLYGALATENOSIDE B Drug Info IC50 = 6040 nM [12]
PYROVALERONE Drug Info IC50 = 28.3 nM [8]
R-NORDULOXETINE Drug Info IC50 = 188 nM [35]
Reboxetine Drug Info Ki = 1.04 nM [29]
RTI-219 Drug Info IC50 = 750 nM [15]
S-34324 Drug Info Ki = 365 nM [5]
Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 840 nM [21]
WAY-256805 Drug Info IC50 = 82 nM [22]
WIN-35066-2 Drug Info Ki = 550 nM [4]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info Ki = 11 nM [2]
[3H]WIN35428 Drug Info IC50 = 1230 nM [47]
{2-[3-(Phenylsulfonyl)-1H-indol-4-yl]ethyl}amine Drug Info IC50 = 960 nM [37]
Action against Disease Model Sibutramine Drug Info Uptake of 3H-dopamine in rat whole brain synaptosomes IC50: 2000 nM [54]
References
REF 1 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. Bioorg Med Chem Lett. 2000 Nov 6;10(21):2445-7.
REF 2 Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters. J Med Chem. 2004 May 6;47(10):2624-34.
REF 3 DOV 216,303, a "triple" reuptake inhibitor: safety, tolerability, and pharmacokinetic profile. J Clin Pharmacol. 2004 Dec;44(12):1360-7.
REF 4 Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl e... J Med Chem. 2004 Dec 2;47(25):6401-9.
REF 5 Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking... J Med Chem. 2005 Mar 24;48(6):2054-71.
REF 6 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 7 Discovery of novel and selective tertiary alcohol containing inhibitors of the norepinephrine transporter. Bioorg Med Chem Lett. 2006 Apr 1;16(7):2022-5.
REF 8 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. J Med Chem. 2006 Feb 23;49(4):1420-32.
REF 9 N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake. Bioorg Med Chem Lett. 2006 May 15;16(10):2714-8.
REF 10 N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4345-8.
REF 11 Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53.
REF 12 Antidepressant principles of the roots of Polygala tenuifolia. J Nat Prod. 2006 Sep;69(9):1305-9.
REF 13 Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogue... J Med Chem. 2006 Oct 19;49(21):6391-9.
REF 14 Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER. Bioorg Med Chem Lett. 2007 Jan 15;17(2):533-7.
REF 15 Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-... J Med Chem. 2007 Jul 26;50(15):3686-95.
REF 16 Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40.
REF 17 Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9.
REF 18 1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity. Bioorg Med Chem Lett. 2008 Jan 15;18(2):596-9.
REF 19 Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an ex... Bioorg Med Chem. 2008 Mar 15;16(6):2769-78.
REF 20 Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6.
REF 21 Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI). Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7.
REF 22 Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors. J Med Chem. 2008 Jul 10;51(13):4038-49.
REF 23 Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modu... Bioorg Med Chem Lett. 2008 Aug 1;18(15):4355-9.
REF 24 Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8.
REF 25 Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4929-31.
REF 26 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. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6067-70.
REF 27 Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropath... J Med Chem. 2008 Nov 27;51(22):7265-72.
REF 28 Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Jan 1;17(1):337-43.
REF 29 Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomogra... J Med Chem. 2009 Jan 8;52(1):62-73.
REF 30 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. Bioorg Med Chem. 2009 Mar 1;17(5):2047-68.
REF 31 Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32.
REF 32 Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more po... Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83.
REF 33 Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents. Eur J Med Chem. 2009 Dec;44(12):4862-88.
REF 34 Bioorg 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 35 Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Oct 1;17(19):6890-7.
REF 36 Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. J Med Chem. 2009 Nov 12;52(21):6768-81.
REF 37 Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(p... Bioorg Med Chem. 2009 Nov 15;17(22):7802-15.
REF 38 Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7.
REF 39 Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agon... Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7.
REF 40 Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation. J Med Chem. 2010 Mar 11;53(5):2204-14.
REF 41 Synthesis and in vitro toxicity of 4-MTA, its characteristic clandestine synthesis byproducts and related sulfur substituted alpha-alkylthioampheta... Bioorg Med Chem. 2010 Jun 1;18(11):4009-31.
REF 42 Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reduc... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92.
REF 43 Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. J Med Chem. 2010 Jun 24;53(12):4731-48.
REF 44 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 45 Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5567-71.
REF 46 Selective monoamine oxidase inhibitors. 3. Cyclic compounds related to 4-aminophenethylamine. Preparation and neuron-selective action of some 5-(2-... J Med Chem. 1986 Aug;29(8):1406-12.
REF 47 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine trans... J Med Chem. 1996 Oct 11;39(21):4139-41.
REF 48 Interaction 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 49 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 50 Uptake and release effects of diethylpropion and its metabolites with biogenic amine transporters. Bioorg Med Chem. 2000 Dec;8(12):2689-92.
REF 51 Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104.
REF 52 8-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 53 Mirtazapine decreases stimulatory effects of reboxetine on cortisol, adrenocorticotropin and prolactin secretion in healthy male subjects. Neuroendocrinology. 2004 Jan;79(1):54-62.
REF 54 Effects of sibutramine on the central dopaminergic system in rodents. Neurotox Res. 2001 Jul;3(3):235-47.
REF 55 Multi-target strategies for the improved treatment of depressive states: Conceptual foundations and neuronal substrates, drug discovery and therape... Pharmacol Ther. 2006 May;110(2):135-370.
REF 56 Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65.
REF 57 Therapeutic potential of monoamine transporter substrates. Curr Top Med Chem. 2006;6(17):1845-59.
REF 58 Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Curr Opin Pharmacol. 2007 Dec;7(6):583-92.
REF 59 BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000.
REF 60 Discovery 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.
REF 61 The 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 62 Uptake 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 63 Studies 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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.