-
1
-
-
47149111966
-
-
Shah U., Boyle C.D., Chackalamannil S., Neustadt B.R., Lindo N., Greenlee W.J., Foster C., Arik L., Zhai Y., Lachowicz J.E., Ng K., Wang S., and Monopoli A. Bioorg. Med. Chem. Lett. 18 (2008) 4199
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 4199
-
-
Shah, U.1
Boyle, C.D.2
Chackalamannil, S.3
Neustadt, B.R.4
Lindo, N.5
Greenlee, W.J.6
Foster, C.7
Arik, L.8
Zhai, Y.9
Lachowicz, J.E.10
Ng, K.11
Wang, S.12
Monopoli, A.13
-
2
-
-
0028183014
-
-
Fredholm B.B., Abbracchio M.P., Burnstock G., Daly J.W., Harden T.K., Jacobson K.A., Leff P., and Williams M. Pharmacol. Rev. 46 (1994) 143
-
(1994)
Pharmacol. Rev.
, vol.46
, pp. 143
-
-
Fredholm, B.B.1
Abbracchio, M.P.2
Burnstock, G.3
Daly, J.W.4
Harden, T.K.5
Jacobson, K.A.6
Leff, P.7
Williams, M.8
-
3
-
-
0025768754
-
-
Ferre S., von Euler G., Johansson B., Fredholm B.B., and Fuxe K. Proc. Natl. Acad. Sci. U.S.A. 88 (1991) 7238
-
(1991)
Proc. Natl. Acad. Sci. U.S.A.
, vol.88
, pp. 7238
-
-
Ferre, S.1
von Euler, G.2
Johansson, B.3
Fredholm, B.B.4
Fuxe, K.5
-
4
-
-
36148955045
-
-
2A Receptors in Parkinson's Disease and Other CNS Disorders.
-
2A Receptors in Parkinson's Disease and Other CNS Disorders.
-
-
-
-
5
-
-
0030075741
-
-
Zocchi C., Ongini E., Conti A., Monopoli A., Negretti A., Baraldi P.G., and Dionisotti S. J. Pharmacol. Exp. Ther. 276 (1996) 398
-
(1996)
J. Pharmacol. Exp. Ther.
, vol.276
, pp. 398
-
-
Zocchi, C.1
Ongini, E.2
Conti, A.3
Monopoli, A.4
Negretti, A.5
Baraldi, P.G.6
Dionisotti, S.7
-
6
-
-
0030004579
-
-
Baraldi P.G., Cacciari B., Spalluto G., Pineda de Villatoro M.J., Zocchi C., Dionisotti S., and Ongini E. J. Med. Chem. 39 (1996) 1164
-
(1996)
J. Med. Chem.
, vol.39
, pp. 1164
-
-
Baraldi, P.G.1
Cacciari, B.2
Spalluto, G.3
Pineda de Villatoro, M.J.4
Zocchi, C.5
Dionisotti, S.6
Ongini, E.7
-
8
-
-
47149113843
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-
1 is necessary to avoid cardiac side-effects.
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1 is necessary to avoid cardiac side-effects.
-
-
-
-
9
-
-
0042626108
-
-
Bara-Jimenez W., Sherzai A., Dimitrova T., Favit A., Bibbiani F., Gillespie M., Morris M.J., Mouradian M.M., and Chase T.N. Neurology 61 (2003) 293
-
(2003)
Neurology
, vol.61
, pp. 293
-
-
Bara-Jimenez, W.1
Sherzai, A.2
Dimitrova, T.3
Favit, A.4
Bibbiani, F.5
Gillespie, M.6
Morris, M.J.7
Mouradian, M.M.8
Chase, T.N.9
-
11
-
-
0023929951
-
-
Francis J.E., Cash W.D., Psychoyos S., Ghai G., Wenk P., Friedmann R.C., Atkins C., Warren V., Furness P., Hyun J.L., Stone G.A., Desai M., and Williams M. J. Med. Chem. 31 (1988) 1014
-
(1988)
J. Med. Chem.
, vol.31
, pp. 1014
-
-
Francis, J.E.1
Cash, W.D.2
Psychoyos, S.3
Ghai, G.4
Wenk, P.5
Friedmann, R.C.6
Atkins, C.7
Warren, V.8
Furness, P.9
Hyun, J.L.10
Stone, G.A.11
Desai, M.12
Williams, M.13
-
12
-
-
0025306964
-
-
Sarges R., Howard H.R., Browne R.G., Lebel L.A., Seymour P.A., and Koe B.K. J. Med. Chem. 33 (1990) 2240
-
(1990)
J. Med. Chem.
, vol.33
, pp. 2240
-
-
Sarges, R.1
Howard, H.R.2
Browne, R.G.3
Lebel, L.A.4
Seymour, P.A.5
Koe, B.K.6
-
13
-
-
0037011899
-
-
Baraldi P.G., Cacciari B., Romagnoli R., Spalluto G., Monopoli A., Ongini E., Varani K., and Borea P.A. J. Med. Chem. 45 (2002) 115
-
(2002)
J. Med. Chem.
, vol.45
, pp. 115
-
-
Baraldi, P.G.1
Cacciari, B.2
Romagnoli, R.3
Spalluto, G.4
Monopoli, A.5
Ongini, E.6
Varani, K.7
Borea, P.A.8
-
14
-
-
33846903864
-
-
Neustadt B.R., Hao J., Lindo N., Greenlee W.J., Stamford A.W., Tulshian D., Ongini E., Hunter J., Monopoli A., Bertorelli R., Foster C., Arik L., Lachowicz J., Ng K., and Feng K.-I. Bioorg. Med. Chem. Lett. 17 (2007) 1376
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 1376
-
-
Neustadt, B.R.1
Hao, J.2
Lindo, N.3
Greenlee, W.J.4
Stamford, A.W.5
Tulshian, D.6
Ongini, E.7
Hunter, J.8
Monopoli, A.9
Bertorelli, R.10
Foster, C.11
Arik, L.12
Lachowicz, J.13
Ng, K.14
Feng, K.-I.15
-
15
-
-
33847063396
-
-
Silverman L.S., Caldwell J.P., Greenlee W.J., Kiselgof E., Matasi J.J., Tulshian D.B., Arik L., Foster C., Bertorelli R., Monopoli A., and Ongini E. Bioorg. Med. Chem. Lett. 17 (2007) 1659
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 1659
-
-
Silverman, L.S.1
Caldwell, J.P.2
Greenlee, W.J.3
Kiselgof, E.4
Matasi, J.J.5
Tulshian, D.B.6
Arik, L.7
Foster, C.8
Bertorelli, R.9
Monopoli, A.10
Ongini, E.11
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16
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47149105269
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note
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All compounds in this publication were isolated and tested in free base form.
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17
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47149110030
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note
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Intermediate 2a is commercially available from Aldrich Chemical Company, Inc., Milwaukee, WI.
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18
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13944274827
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2A receptors did not differ from affinity for the human receptor
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2A receptors did not differ from affinity for the human receptor
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(2005)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 1333
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Matasi, J.J.1
Caldwell, J.P.2
Hao, J.3
Neustadt, B.4
Arik, L.5
Foster, C.6
Lachowicz, J.7
Tulshian, D.8
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19
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0033136333
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Procedure described in: %CV values typically range from 10 to 30 in this assay (n = 2)
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Procedure described in:. Cox K.A., Dunn-Meynell K., Korfmacher W.A., Broske L., Nomeir A.A., Lin C.-C., Cayen M.N., and Barr W.H. Drug Discovery Today 4 (1999) 232 %CV values typically range from 10 to 30 in this assay (n = 2)
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(1999)
Drug Discovery Today
, vol.4
, pp. 232
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Cox, K.A.1
Dunn-Meynell, K.2
Korfmacher, W.A.3
Broske, L.4
Nomeir, A.A.5
Lin, C.-C.6
Cayen, M.N.7
Barr, W.H.8
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20
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47149105669
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Inhibition of haloperidol-induced catalepsy is an in vivo assay used to evaluate Parkinson's drugs (>30% inhibition is considered to be active in this assay)
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Inhibition of haloperidol-induced catalepsy is an in vivo assay used to evaluate Parkinson's drugs (>30% inhibition is considered to be active in this assay)
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22
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22844440107
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Procedure described in:
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Procedure described in:. Matasi J.J., Caldwell J.P., Zhang H., Fawzi A., Cohen-Williams M.E., Varty G.B., and Tulshian D.B. Bioorg. Med. Chem. Lett. 15 (2005) 3670
-
(2005)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 3670
-
-
Matasi, J.J.1
Caldwell, J.P.2
Zhang, H.3
Fawzi, A.4
Cohen-Williams, M.E.5
Varty, G.B.6
Tulshian, D.B.7
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23
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0035289779
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The nephelometric (light scattering) method was used to determine the kinetic solubility of compounds. The test compound (1.0 mg) was dissolved in DMSO at 25 mM.A serial dilution into DMSO was performed and 3 μl of the compound in DMSO at various concentrations was added to the buffer (10 mM phosphate, pH 7.4). Presence of precipitate was detected by nephelometry. Solubility was defined as the highest concentration of material that did not scatter light
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The nephelometric (light scattering) method was used to determine the kinetic solubility of compounds. The test compound (1.0 mg) was dissolved in DMSO at 25 mM.A serial dilution into DMSO was performed and 3 μl of the compound in DMSO at various concentrations was added to the buffer (10 mM phosphate, pH 7.4). Presence of precipitate was detected by nephelometry. Solubility was defined as the highest concentration of material that did not scatter light. Lipinski C.A., Lombardo F., Dominy B.W., and Feeney P.J. Adv. Drug Delivery Rev. 46 (2001) 3
-
(2001)
Adv. Drug Delivery Rev.
, vol.46
, pp. 3
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Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
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24
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0023638005
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Tetrahydroisoquinolines 2i, 2j, and 10 were synthesized as described in: Intermediates 2e-2g are commercially available from Acros Organics, Morris Plains, NJ
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Tetrahydroisoquinolines 2i, 2j, and 10 were synthesized as described in:. Sall D.J., and Grunewald G.L. J. Med. Chem. 30 (1987) 2208 Intermediates 2e-2g are commercially available from Acros Organics, Morris Plains, NJ
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(1987)
J. Med. Chem.
, vol.30
, pp. 2208
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Sall, D.J.1
Grunewald, G.L.2
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25
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84980225877
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Benzazepine 2m was synthesized as described in: The unsubstituted intermediate 2l is commercially available from Scientific Exchange, Inc., Center Ossipee, NH
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Benzazepine 2m was synthesized as described in:. Pecherer B., Sunbury R.C., and Brossi A. J. Heterocycl. Chem. 8 (1971) 779 The unsubstituted intermediate 2l is commercially available from Scientific Exchange, Inc., Center Ossipee, NH
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(1971)
J. Heterocycl. Chem.
, vol.8
, pp. 779
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Pecherer, B.1
Sunbury, R.C.2
Brossi, A.3
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26
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0021235467
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The synthesis of intermediate 2r is reported in the following reference:
-
The synthesis of intermediate 2r is reported in the following reference:. Shiozawa A., Ichikawa Y.-I., Ishikawa M., Kogo Y., Kurashige S., Miyazaki H., Yamanaka H., and Sakamoto T. Chem. Pharm. Bull. 32 (1984) 995
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(1984)
Chem. Pharm. Bull.
, vol.32
, pp. 995
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-
Shiozawa, A.1
Ichikawa, Y.-I.2
Ishikawa, M.3
Kogo, Y.4
Kurashige, S.5
Miyazaki, H.6
Yamanaka, H.7
Sakamoto, T.8
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27
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0021203034
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The synthesis of intermediate 2s is reported in the following reference:
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The synthesis of intermediate 2s is reported in the following reference:. Shiozawa A., Ichikawa Y.-I., Komuro C., Kurashige S., Miyazaki H., Yamanaka H., and Sakamoto T. Chem. Pharm. Bull. 32 (1984) 2522
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(1984)
Chem. Pharm. Bull.
, vol.32
, pp. 2522
-
-
Shiozawa, A.1
Ichikawa, Y.-I.2
Komuro, C.3
Kurashige, S.4
Miyazaki, H.5
Yamanaka, H.6
Sakamoto, T.7
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29
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0035012876
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Cyclization of 13 to form a 3-nitrotetrahydronaphthyridine is reported in:
-
Cyclization of 13 to form a 3-nitrotetrahydronaphthyridine is reported in:. Harling J.D., Harrington F.P., and Thompson M. Synth. Commun. 31 (2001) 787
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(2001)
Synth. Commun.
, vol.31
, pp. 787
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-
Harling, J.D.1
Harrington, F.P.2
Thompson, M.3
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30
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0036150226
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The synthesis of intermediate 2w is reported in:
-
The synthesis of intermediate 2w is reported in:. Fukui H., Inoguchi K., and Nakano J. Heterocycles 56 (2002) 257
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(2002)
Heterocycles
, vol.56
, pp. 257
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Fukui, H.1
Inoguchi, K.2
Nakano, J.3
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31
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47149110583
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The synthesis of intermediate 2x is described in: Ashton, W. T.; Caldwell, C. G.; Duffy, J. L.; Mathvink, R. J.; Wang, L.; Weber, A. E. WO Patent 2004069162, 2004.
-
The synthesis of intermediate 2x is described in: Ashton, W. T.; Caldwell, C. G.; Duffy, J. L.; Mathvink, R. J.; Wang, L.; Weber, A. E. WO Patent 2004069162, 2004.
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