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Hudson S., Kiankarimi M., Eccles W., Mostofi Y.S., Genicot M.J., Dwight W., Fleck B.A., Gogas K., and Wade W.S. Bioorg. Med. Chem. Lett. 18 (2008) 4495
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Personal Communication, Brian Campell, Pfizer Global Research and Development, Groton, Connecticut, USA.
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Dounay A.B., Barta N.S., Bikker J.A., Borosky S.A., Campbell B.M., Crawford T., Denny L., Evans L.M., Gray D.L., Lee P., Lenoir E.A., and Xu W. Bioorg. Med. Chem. Lett. 19 (2009) 1159
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16
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49449095466
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Siracusa M.A., Salerno L., Modica M.N., Pittala V., Romeo G., Amato M.E., Nowak M., Bojarski A.J., Mereghetti I., Cagnotto A., and Mennini T. J. Med. Chem. 51 (2008) 4529
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71749102114
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WO patent 9814433
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Howard, H.R.1
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60849111422
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Collantes, E. M.; Ortwine, D. F. Abstracts of Papers, 238th ACS National Meeting, Washington, DC, United States, March 16-20, 2009; COMP-229.
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22
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71749084957
-
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note
-
1A = 14 nM).
-
-
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23
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71749116350
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Monoamine binding assay: Homogenized paste prepared from HEK293 cell lines expressing human clones for NE, DA, and 5HT transporters was incubated with drug and 50 pM [125I]-RTI-55 for 90 min at rt in PEI coated FlashPlates. Binding was terminated by assay withdraw with plates subsequently counted for beta emissions. Nonspecific binding was determined in the presence of selective inhibitors desipramine, GBR12909 and citalopram.
-
Monoamine binding assay: Homogenized paste prepared from HEK293 cell lines expressing human clones for NE, DA, and 5HT transporters was incubated with drug and 50 pM [125I]-RTI-55 for 90 min at rt in PEI coated FlashPlates. Binding was terminated by assay volume withdraw with plates subsequently counted for beta emissions. Nonspecific binding was determined in the presence of selective inhibitors desipramine, GBR12909 and citalopram.
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24
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38149006973
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1A binding assay according to published protocol:
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1A binding assay according to published protocol:. Graham J.M., Coughenour L.L., Barr B.M., Rock D.L., and Nikam S.S. Bioorg. Med. Chem. Lett. 18 (2008) 489
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25
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12444315980
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Dyck B., Parker J., Phillips T., Carter L., Murphy B., Summers R., Hermann J., Baker T., Cismowski M., Saunders J., and Goodfellow V. Bioorg. Med. Chem. Lett. 21 (2003) 3793
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26
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71749087388
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note
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Aryl piperidine benzyl alcohol 4 was prepared starting from 2-bromobenzaldehyde by the method outlined in Scheme 2.
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27
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71749086968
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note
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3 in MeOH.
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28
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0024547622
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Martin G.E., Elgin Jr. R.J., Mathiasen J.R., Davis C.B., Kesslick J.M., Baldy W.J., Shank R.P., DiStefano D.L., Fedde C.L., and Scott M.K. J. Med. Chem. 42 (1989) 1052
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9144220758
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Richardson T.I., Ornstein P.L., Briner K., Fisher M.J., Backer R.T., Biggers C.K., Clay M.P., Emmerson P.J., Hertel L.W., Hsiung H.M., Husain S., Kahl S.D., Lee J.A., Lindstrom T.D., Martinelli M.J., Mayer J.P., Mullaney J.T., O'Brien T.P., Pawlak J.M., Revell K.D., Shah J., Zgombick J.M., Herr R.J., Melekhov A., Sampson P.B., and King C.-H.R. J. Med. Chem. 47 (2004) 744
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more..
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30
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0034534775
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Komoto T., Hirota H., Otsuka M., Kotake J., Hasegawa S., Koya H., Sato S., and Sakamoto T. Chem. Pharm. Bull. 48 (2000) 1978
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Komoto, T.1
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Hasegawa, S.5
Koya, H.6
Sato, S.7
Sakamoto, T.8
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31
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71749099915
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Compound 14 was purchased from a commercial source
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Compound 14 was purchased from a commercial source.
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34
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0037007703
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Buck E., Song Z.J., Tschaen D., Dormer P.G., Volante R.P., and Reider P.J. Org. Lett. 4 (2002) 1623
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Buck, E.1
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Reider, P.J.6
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35
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71749117423
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1A (FLIPR assay) see Ref. 10a.
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1A (FLIPR assay) see Ref. 10a.
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36
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23944451585
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Monoamine uptake: HEK293 cell lines expressing human clones for NE, DA, and 5HT transporters were used to evaluate monamine reuptake inhibition. Cell suspensions were filter harvested following a 20 minute, RT exposure to tritiated versions of NE (100 nM), DA (50 nM), or 5HT (25 nM) in the presence or absence of test agents. Non-specific uptake was determined in the presence of selective antagonists atomoxetine, GBR12909 and citalopram. (c) HLM assay expressed as apparent intrinsic clearance (uncorrected for microsomal binding): Riley, R. J.; McGinnity, D. F.; Austin, R. P. Drug. Metab. Dispos. 2005, 33, 1304.
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Monoamine uptake: HEK293 cell lines expressing human clones for NE, DA, and 5HT transporters were used to evaluate monamine reuptake inhibition. Cell suspensions were filter harvested following a 20 minute, RT exposure to tritiated versions of NE (100 nM), DA (50 nM), or 5HT (25 nM) in the presence or absence of test agents. Non-specific uptake was determined in the presence of selective antagonists atomoxetine, GBR12909 and citalopram. (c) HLM assay expressed as apparent intrinsic clearance (uncorrected for microsomal binding): Riley, R. J.; McGinnity, D. F.; Austin, R. P. Drug. Metab. Dispos. 2005, 33, 1304.
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38
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71749103961
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note
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1A SEM = 0.6% (n = 4), NET SEM = 1.5% (n = 4). IACUC approved procedures were carried out in compliance with the NIH Guide for the Care and Use of Laboratory Animals (1985).
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