-
1
-
-
0026586557
-
-
1 Lloyd, K.C., Raybould, H.E., Tache, Y. and Walsh, J.H. Am. J. Physiol. 1992, 262, 747; Kovacs, T.O., Walsh, J.H., Maxwell, V., Wong, H.C., Azuma, T. and Katt, E. Gastroenterology 1989, 97, 1406.
-
(1992)
Am. J. Physiol.
, vol.262
, pp. 747
-
-
Lloyd, K.C.1
Raybould, H.E.2
Tache, Y.3
Walsh, J.H.4
-
2
-
-
0024337187
-
-
1 Lloyd, K.C., Raybould, H.E., Tache, Y. and Walsh, J.H. Am. J. Physiol. 1992, 262, 747; Kovacs, T.O., Walsh, J.H., Maxwell, V., Wong, H.C., Azuma, T. and Katt, E. Gastroenterology 1989, 97, 1406.
-
(1989)
Gastroenterology
, vol.97
, pp. 1406
-
-
Kovacs, T.O.1
Walsh, J.H.2
Maxwell, V.3
Wong, H.C.4
Azuma, T.5
Katt, E.6
-
4
-
-
0024529827
-
-
3 Bock, M.G., DiPardo, R.M., Evans, B.E., Rittle, K.E., Whitter, W.L., Veber, D.F., Anderson, P.S. and Freidinger, R.M. J. Med. Chem. 1989, 32, 13.
-
(1989)
J. Med. Chem.
, vol.32
, pp. 13
-
-
Bock, M.G.1
DiPardo, R.M.2
Evans, B.E.3
Rittle, K.E.4
Whitter, W.L.5
Veber, D.F.6
Anderson, P.S.7
Freidinger, R.M.8
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5
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-
0026508095
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-
Bs were determined by the average of two experiments, each at a single concentration. For full experimental details of pharmacological assays see: Patel, M. and Spraggs, C.F. Br. J. Pharmacol. 1992, 106, 275.
-
(1992)
Br. J. Pharmacol.
, vol.106
, pp. 275
-
-
Patel, M.1
Spraggs, C.F.2
-
6
-
-
0027724267
-
-
5 The same observation was made by workers at Merck in the 1,4-benzodiazepinone series: Bock, M.G., DiPardo, R.M., Evans, B.E., Rittle, K.E., Whitter, W.L., Garsky, V.M., Gilbert, K.F., Leighton, J.L., Carson, K.L., Mellin, E.C., Veber, D.F., Chang, R.S.L., Lotti, V.J., Freedman, S.B., Smith, A.J., Patel, S., Anderson, P.S. and Freidinger, R.M. J. Med. Chem. 1993, 36, 4276.
-
(1993)
J. Med. Chem.
, vol.36
, pp. 4276
-
-
Bock, M.G.1
DiPardo, R.M.2
Evans, B.E.3
Rittle, K.E.4
Whitter, W.L.5
Garsky, V.M.6
Gilbert, K.F.7
Leighton, J.L.8
Carson, K.L.9
Mellin, E.C.10
Veber, D.F.11
Chang, R.S.L.12
Lotti, V.J.13
Freedman, S.B.14
Smith, A.J.15
Patel, S.16
Anderson, P.S.17
Freidinger, R.M.18
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7
-
-
0017619105
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-
and references therein
-
6 For the general procedure see: Hedges, A.R. and Parsons, M.E. J. Physiol. 1977, 267, 181 and references therein.
-
(1977)
J. Physiol.
, vol.267
, pp. 181
-
-
Hedges, A.R.1
Parsons, M.E.2
-
8
-
-
0017095638
-
-
7 Elliott, H.W. Br. J. Anaesth. 1976, 48, 1017; Ruelius, H.W. J. Clin. Psychiatry 1978, 39, 11; Shutz, H., "Biotransformation" in Benzodiazepines, Springer-Verlag: Berlin, 1982; pp 4-11.
-
(1976)
Br. J. Anaesth.
, pp. 1017
-
-
Elliott, H.W.1
-
9
-
-
0018161039
-
-
7 Elliott, H.W. Br. J. Anaesth. 1976, 48, 1017; Ruelius, H.W. J. Clin. Psychiatry 1978, 39, 11; Shutz, H., "Biotransformation" in Benzodiazepines, Springer-Verlag: Berlin, 1982; pp 4-11.
-
(1978)
J. Clin. Psychiatry
, vol.39
, pp. 11
-
-
Ruelius, H.W.1
-
10
-
-
0011385713
-
Biotransformation
-
Springer-Verlag: Berlin
-
7 Elliott, H.W. Br. J. Anaesth. 1976, 48, 1017; Ruelius, H.W. J. Clin. Psychiatry 1978, 39, 11; Shutz, H., "Biotransformation" in Benzodiazepines, Springer-Verlag: Berlin, 1982; pp 4-11.
-
(1982)
Benzodiazepines
, pp. 4-11
-
-
Shutz, H.1
-
11
-
-
0011477273
-
-
Pharmacokinetic Protocol: Each rat received a single oral or intravenous dose equivalent to 3 mg/kg bodyweight. Blood was collected under anaesthesia at 0, 5, 15, 30, 45 min, and 1, 1.5, 2, 4, 6, 8, 10, 12 and 24 h post dosing (two rats per time point). The blood samples were placed in heparinised tubes and centrifuged to separate the plasma. Plasma samples were extracted by solid phase extraction with C8 cartridges. The extracts were analysed by HPLC using an Inertsil ODS column with UV detection
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8 Pharmacokinetic Protocol: Each rat received a single oral or intravenous dose equivalent to 3 mg/kg bodyweight. Blood was collected under anaesthesia at 0, 5, 15, 30, 45 min, and 1, 1.5, 2, 4, 6, 8, 10, 12 and 24 h post dosing (two rats per time point). The blood samples were placed in heparinised tubes and centrifuged to separate the plasma. Plasma samples were extracted by solid phase extraction with C8 cartridges. The extracts were analysed by HPLC using an Inertsil ODS column with UV detection.
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-
-
-
12
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-
0028180562
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9 Denyer, J., Gray, J., Wong, M., Stolz, M. and Tate, S. Eur. J. Pharm. (Mol. Pharmacology Sec.) 1994, 268, 29.
-
(1994)
Eur. J. Pharm. (Mol. Pharmacology Sec.)
, vol.268
, pp. 29
-
-
Denyer, J.1
Gray, J.2
Wong, M.3
Stolz, M.4
Tate, S.5
-
13
-
-
0027156051
-
-
10 Ulrich, C.D., Ferber, I., Holicky, E., Hadac, E., Buell, G. and Miller, L.J. Biochem. Biophys. Res. Commun. 1993, 193, 204.
-
(1993)
Biochem. Biophys. Res. Commun.
, vol.193
, pp. 204
-
-
Ulrich, C.D.1
Ferber, I.2
Holicky, E.3
Hadac, E.4
Buell, G.5
Miller, L.J.6
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14
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-
0011475146
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-
Except for 7, pKis were determined in triplicate in a single experiment
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11 Except for 7, pKis were determined in triplicate in a single experiment.
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15
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0028314649
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12 Similar substituants, but located at C-5, were found to be beneficial in the 1,4-benzodiazepine series: Showell, G.A., Bourrain, S., Neduvelil, J.G., Fletcher, S.R., Baker, R., Watt, A.P., Fletcher, A.E., Freedman, S.B., Kemp, J.A., Marshall, G.R., Patel, S., Smith, A.J. and Matassa, V.G. J. Med. Chem. 1994, 37, 719.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 719
-
-
Showell, G.A.1
Bourrain, S.2
Neduvelil, J.G.3
Fletcher, S.R.4
Baker, R.5
Watt, A.P.6
Fletcher, A.E.7
Freedman, S.B.8
Kemp, J.A.9
Marshall, G.R.10
Patel, S.11
Smith, A.J.12
Matassa, V.G.13
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16
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0027377367
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-
13 The same observation was made independently by workers at Merck in the 1,4-benzodiazepinone series: Chambers, M.S., Hobbs, S.C., Fletcher, S.R., Matassa, V.G., Mitchell, P.J., Watt, A.P., Baker, R., Freedman, S.B., Patel, S. and Smith, A.J. Bioorg. and Med. Chem. Lett. 1993, 3, 1919.
-
(1993)
Bioorg. and Med. Chem. Lett.
, vol.3
, pp. 1919
-
-
Chambers, M.S.1
Hobbs, S.C.2
Fletcher, S.R.3
Matassa, V.G.4
Mitchell, P.J.5
Watt, A.P.6
Baker, R.7
Freedman, S.B.8
Patel, S.9
Smith, A.J.10
-
17
-
-
0028871552
-
-
Patent Application WO 94/13648
-
14 Armour, D.R., Box, P.C. and Shah, P. Patent Application WO 94/13648; Sherrill, R.G. and Sugg, E.E. J. Org. Chem. 1995, 60, 730.
-
-
-
Armour, D.R.1
Box, P.C.2
Shah, P.3
-
18
-
-
0028871552
-
-
14 Armour, D.R., Box, P.C. and Shah, P. Patent Application WO 94/13648; Sherrill, R.G. and Sugg, E.E. J. Org. Chem. 1995, 60, 730.
-
(1995)
J. Org. Chem.
, vol.60
, pp. 730
-
-
Sherrill, R.G.1
Sugg, E.E.2
-
19
-
-
0011385575
-
-
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