-
2
-
-
33845981826
-
-
B.Q. Wei, T.S. Mikkelsen, M.K. McKinney, E.S. Lander, and B.F. Cravatt J. Biol. Chem. 281 2006 36569
-
(2006)
J. Biol. Chem.
, vol.281
, pp. 36569
-
-
Wei, B.Q.1
Mikkelsen, T.S.2
McKinney, M.K.3
Lander, E.S.4
Cravatt, B.F.5
-
3
-
-
0027078685
-
-
W.A. Devane, L. Hanus, A. Breuer, R.G. Pertwee, L.A. Stevenson, G. Griffin, D. Gibson, A. Mandelbaum, A. Etinger, and R. Mechoulam Science 258 1992 1946
-
(1992)
Science
, vol.258
, pp. 1946
-
-
Devane, W.A.1
Hanus, L.2
Breuer, A.3
Pertwee, R.G.4
Stevenson, L.A.5
Griffin, G.6
Gibson, D.7
Mandelbaum, A.8
Etinger, A.9
Mechoulam, R.10
-
5
-
-
11244328917
-
-
J. Lo Verme, J. Fu, G. Astarita, G. La Rana, R. Russo, A. Calignano, and D. Piomelli Mol. Pharmacol. 67 2005 15
-
(2005)
Mol. Pharmacol.
, vol.67
, pp. 15
-
-
Lo Verme, J.1
Fu, J.2
Astarita, G.3
La Rana, G.4
Russo, R.5
Calignano, A.6
Piomelli, D.7
-
9
-
-
0035979244
-
-
B.F. Cravatt, K. Demarest, M.P. Patricelli, M.H. Bracey, D.K. Giang, B.R. Martin, and A.H. Lichtman Proc. Natl. Acad. Sci. U.S.A. 98 2001 9371
-
(2001)
Proc. Natl. Acad. Sci. U.S.A.
, vol.98
, pp. 9371
-
-
Cravatt, B.F.1
Demarest, K.2
Patricelli, M.P.3
Bracey, M.H.4
Giang, D.K.5
Martin, B.R.6
Lichtman, A.H.7
-
10
-
-
79952966932
-
-
F.J. Pavon, A. Serrano, M. Romero-Cuevas, M. Alonso, and F.R. de Fonseca Drug Disc. Today: Dis. Mech. 7 2011 e175 e183
-
(2011)
Drug Disc. Today: Dis. Mech.
, vol.7
-
-
Pavon, F.J.1
Serrano, A.2
Romero-Cuevas, M.3
Alonso, M.4
De Fonseca, F.R.5
-
11
-
-
0035979244
-
-
B.F. Cravatt, K. Demarest, M.P. Patricelli, M.H. Bracey, D.K. Giang, B.R. Martin, and A.H. Lichtman PNAS 98 2001 9371
-
(2001)
PNAS
, vol.98
, pp. 9371
-
-
Cravatt, B.F.1
Demarest, K.2
Patricelli, M.P.3
Bracey, M.H.4
Giang, D.K.5
Martin, B.R.6
Lichtman, A.H.7
-
12
-
-
49849094981
-
-
J.M. Keith, R. Apodaca, W. Xiao, M. Seierstad, K. Pattabiraman, J. Wu, M. Webb, M.J. Karbarz, S. Brown, S. Wilson, B. Scott, C.-S. Tham, L. Luo, J. Palmer, M. Wennerholm, S. Chaplan, and J.G. Breitenbucher Bioorg. Med. Chem. Lett. 18 2008 4838
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 4838
-
-
Keith, J.M.1
Apodaca, R.2
Xiao, W.3
Seierstad, M.4
Pattabiraman, K.5
Wu, J.6
Webb, M.7
Karbarz, M.J.8
Brown, S.9
Wilson, S.10
Scott, B.11
Tham, C.-S.12
Luo, L.13
Palmer, J.14
Wennerholm, M.15
Chaplan, S.16
Breitenbucher, J.G.17
-
13
-
-
64749114255
-
-
K. Ahn, D.S. Johnson, M. Mileni, D. Beidler, J.Z. Long, M.K. McKinney, E. Weerapana, N. Sadagopan, M. Liimatta, S.E. Smith, S. Lazerwith, C. Stiff, S. Kamtekar, K. Bhattacharya, Y. Zhang, S. Swaney, K.V. Becelaere, R.C. Stevens, and B.F. Cravatt Chem. Bio. 16 2009 411
-
(2009)
Chem. Bio.
, vol.16
, pp. 411
-
-
Ahn, K.1
Johnson, D.S.2
Mileni, M.3
Beidler, D.4
Long, J.Z.5
McKinney, M.K.6
Weerapana, E.7
Sadagopan, N.8
Liimatta, M.9
Smith, S.E.10
Lazerwith, S.11
Stiff, C.12
Kamtekar, S.13
Bhattacharya, K.14
Zhang, Y.15
Swaney, S.16
Becelaere, K.V.17
Stevens, R.C.18
Cravatt, B.F.19
-
14
-
-
79951518976
-
-
D.S. Johnson, C. Stiff, S. Lazerwith, S. Kesten, L. Fay, M. Morris, D. Beidler, M. Liimatta, S. Smith, N. Sadagopan, S. Bhattachar, S. Kesten, D. Dudley, T.K. Nomanbhoy, B.F. Cravatt, and K. Ahn ACS Med. Chem. Lett. 2 2011 91
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 91
-
-
Johnson, D.S.1
Stiff, C.2
Lazerwith, S.3
Kesten, S.4
Fay, L.5
Morris, M.6
Beidler, D.7
Liimatta, M.8
Smith, S.9
Sadagopan, N.10
Bhattachar, S.11
Kesten, S.12
Dudley, D.13
Nomanbhoy, T.K.14
Cravatt, B.F.15
Ahn, K.16
-
15
-
-
79959506821
-
-
K. Ahn, S.E. Smith, M.B. Liimatta, D. Beidler, N. Sadagopan, D.T. Dudley, T. Young, P. Wren, Y. Zhang, S. Swaney, K. Van Becelaere, J.L. Blankman, D.K. Nomura, S.N. Bhattachar, C. Stiff, T.K. Nomanbhoy, E. Weerapana, D.S. Johnson, and B.F. Cravatt J. Pharmacol. Exp. Ther. 338 2011 114
-
(2011)
J. Pharmacol. Exp. Ther.
, vol.338
, pp. 114
-
-
Ahn, K.1
Smith, S.E.2
Liimatta, M.B.3
Beidler, D.4
Sadagopan, N.5
Dudley, D.T.6
Young, T.7
Wren, P.8
Zhang, Y.9
Swaney, S.10
Van Becelaere, K.11
Blankman, J.L.12
Nomura, D.K.13
Bhattachar, S.N.14
Stiff, C.15
Nomanbhoy, T.K.16
Weerapana, E.17
Johnson, D.S.18
Cravatt, B.F.19
-
16
-
-
84858954657
-
-
G.L. Li, H. Winter, R. Arends, G.W. Jay, V. Le, T. Young, and J.P. Huggins Br. J. Clin. Pharmacol. 73 2012 706
-
(2012)
Br. J. Clin. Pharmacol.
, vol.73
, pp. 706
-
-
Li, G.L.1
Winter, H.2
Arends, R.3
Jay, G.W.4
Le, V.5
Young, T.6
Huggins, J.P.7
-
17
-
-
65349167368
-
-
D.S. Johnson, K. Ahn, S. Kesten, S.E. Lazerwith, Y. Song, M. Morris, L. Fay, T. Gregory, C. Stiff, J.B. Dunbar, M. Liimatta, D. Beidler, S. Smith, T.K. Nomanbhoy, and B.F. Cravatt Bioorg. Med. Chem. Lett. 19 2009 2865
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 2865
-
-
Johnson, D.S.1
Ahn, K.2
Kesten, S.3
Lazerwith, S.E.4
Song, Y.5
Morris, M.6
Fay, L.7
Gregory, T.8
Stiff, C.9
Dunbar, J.B.10
Liimatta, M.11
Beidler, D.12
Smith, S.13
Nomanbhoy, T.K.14
Cravatt, B.F.15
-
18
-
-
84867369139
-
-
J.M. Keith, R. Apodaca, M. Tichenor, W. Xiao, W. Jones, J. Pierce, M. Seierstad, J. Palmer, M. Webb, M.J. Karbarz, B. Scott, S. Wilson, L. Luo, M. Wennerholm, L. Chang, S. Brown, M. Rizzolio, R. Rynberg, S. Chaplan, and J.G. Breitenbucher ACS Med. Chem. Lett. 3 2012 823 827
-
(2012)
ACS Med. Chem. Lett.
, vol.3
, pp. 823-827
-
-
Keith, J.M.1
Apodaca, R.2
Tichenor, M.3
Xiao, W.4
Jones, W.5
Pierce, J.6
Seierstad, M.7
Palmer, J.8
Webb, M.9
Karbarz, M.J.10
Scott, B.11
Wilson, S.12
Luo, L.13
Wennerholm, M.14
Chang, L.15
Brown, S.16
Rizzolio, M.17
Rynberg, R.18
Chaplan, S.19
Breitenbucher, J.G.20
more..
-
19
-
-
80054791082
-
-
M.J. Meyers, S.A. Long, M.J. Pelc, J.L. Wang, S.J. Bowen, B.A. Schweitzer, M.V. Wilcox, J. McDonald, S.E. Smith, S. Foltin, J. Rumsey, Y.-S. Yang, M.C. Walker, S. Kamtekar, D. Beidler, and A. Thorarensen Bioorg. Med. Chem. Lett. 21 2011 6545
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 6545
-
-
Meyers, M.J.1
Long, S.A.2
Pelc, M.J.3
Wang, J.L.4
Bowen, S.J.5
Schweitzer, B.A.6
Wilcox, M.V.7
McDonald, J.8
Smith, S.E.9
Foltin, S.10
Rumsey, J.11
Yang, Y.-S.12
Walker, M.C.13
Kamtekar, S.14
Beidler, D.15
Thorarensen, A.16
-
20
-
-
80054778775
-
-
M.J. Meyers, S.A. Long, M.J. Pelc, J.L. Wang, S.J. Bowen, M.C. Walker, B.A. Schweitzer, H.M. Madsen, R.E. Tenbrink, J. McDonald, S.E. Smith, S. Foltin, D. Beidler, and A. Thorarensen Bioorg. Med. Chem. Lett. 21 2011 6538
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 6538
-
-
Meyers, M.J.1
Long, S.A.2
Pelc, M.J.3
Wang, J.L.4
Bowen, S.J.5
Walker, M.C.6
Schweitzer, B.A.7
Madsen, H.M.8
Tenbrink, R.E.9
McDonald, J.10
Smith, S.E.11
Foltin, S.12
Beidler, D.13
Thorarensen, A.14
-
21
-
-
79953283871
-
-
D.J. Gustin, Z. Ma, X. Min, Y. Li, C. Hedberg, C. Guimaraes, A.C. Porter, M. Lindstrom, D. Lester-Zeiner, G. Xu, T.J. Carlson, S. Xiao, C. Meleza, R. Connors, Z. Wang, and F. Kayser Bioorg. Med. Chem. Lett. 21 2011 2492
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 2492
-
-
Gustin, D.J.1
Ma, Z.2
Min, X.3
Li, Y.4
Hedberg, C.5
Guimaraes, C.6
Porter, A.C.7
Lindstrom, M.8
Lester-Zeiner, D.9
Xu, G.10
Carlson, T.J.11
Xiao, S.12
Meleza, C.13
Connors, R.14
Wang, Z.15
Kayser, F.16
-
22
-
-
54049105756
-
-
Note: this intermediate has since become commercially available
-
J. Burkhard, and E.M. Carreira Org. Lett. 10 2008 3525 Note: this intermediate has since become commercially available
-
(2008)
Org. Lett.
, vol.10
, pp. 3525
-
-
Burkhard, J.1
Carreira, E.M.2
-
24
-
-
84867369139
-
-
JNJ-40355003 will give almost complete inhibition of FAAH in rat brain out to about 12 h (10 mg/kg, p.o.; 90% FAAH inhibition at 12 h), and gives robust increases in AEA, PEA and OEA. JNJ-40355003 is consistently effective in the Chung model at lower doses, but the artificially high dose is used to ensure maximum efficacy
-
JNJ-40355003 will give almost complete inhibition of FAAH in rat brain out to about 12 h (10 mg/kg, p.o.; 90% FAAH inhibition at 12 h), and gives robust increases in AEA, PEA and OEA. JNJ-40355003 is consistently effective in the Chung model at lower doses, but the artificially high dose is used to ensure maximum efficacy J.M. Keith, R. Apodaca, M. Tichenor, W. Xiao, W. Jones, J. Pierce, M. Seierstad, J. Palmer, M. Webb, M. Karbarz, B. Scott, S. Wilson, L. Luo, M. Wennerholm, L. Chang, S. Brown, M. Rizzolio, R. Rynberg, S. Chaplan, and J.G. Breitenbucher ACS Med. Chem. Lett. 3 2012 823
-
(2012)
ACS Med. Chem. Lett.
, vol.3
, pp. 823
-
-
Keith, J.M.1
Apodaca, R.2
Tichenor, M.3
Xiao, W.4
Jones, W.5
Pierce, J.6
Seierstad, M.7
Palmer, J.8
Webb, M.9
Karbarz, M.10
Scott, B.11
Wilson, S.12
Luo, L.13
Wennerholm, M.14
Chang, L.15
Brown, S.16
Rizzolio, M.17
Rynberg, R.18
Chaplan, S.19
Breitenbucher, J.G.20
more..
-
25
-
-
20144377098
-
-
D.L. Boger, H. Miyauchi, W. Du, C. Hardouin, R.A. Fecik, H. Cheng, I. Hwang, M.P. Hedrick, D. Leung, O. Acevedo, C.R. Guimaraes, W.L. Jorgensen, and B.F. Cravatt J. Med. Chem. 48 2005 1849
-
(2005)
J. Med. Chem.
, vol.48
, pp. 1849
-
-
Boger, D.L.1
Miyauchi, H.2
Du, W.3
Hardouin, C.4
Fecik, R.A.5
Cheng, H.6
Hwang, I.7
Hedrick, M.P.8
Leung, D.9
Acevedo, O.10
Guimaraes, C.R.11
Jorgensen, W.L.12
Cravatt, B.F.13
-
26
-
-
33847783305
-
-
F.A. Romero, W. Du, I. Hwang, T.J. Rayl, F.S. Kimball, D. Leung, H.S. Hoover, R.L. Apodaca, J.G. Breitenbucher, B.F. Cravatt, and D.L. Boger J. Med. Chem. 50 2007 1058
-
(2007)
J. Med. Chem.
, vol.50
, pp. 1058
-
-
Romero, F.A.1
Du, W.2
Hwang, I.3
Rayl, T.J.4
Kimball, F.S.5
Leung, D.6
Hoover, H.S.7
Apodaca, R.L.8
Breitenbucher, J.G.9
Cravatt, B.F.10
Boger, D.L.11
-
27
-
-
68049090031
-
-
M. Mileni, J. Garfunkle, J.K. DeMartino, B.F. Cravatt, D.L. Boger, and R.C. Stevens J. Am. Chem. Soc. 131 2009 10497
-
(2009)
J. Am. Chem. Soc.
, vol.131
, pp. 10497
-
-
Mileni, M.1
Garfunkle, J.2
Demartino, J.K.3
Cravatt, B.F.4
Boger, D.L.5
Stevens, R.C.6
|