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A. Hall et al. / Bioorg. Med. Chem. Lett. 18 (2008) 3392–3399
9. Naganawa, A.; Matsui, T.; Ima, M.; Saito, T.; Murota,
Acknowledgment
M.; Aratani, Y.; Kijima, H.; Yamamoto, H.; Maruyama,
T.; Ohuchida, S.; Nakai, H.; Toda, M. Bioorg. Med.
Chem. 2006, 16, 7121.
We thank Alan K. Bristow for stability studies con-
ducted with compound 10a and for formulation devel-
opment for compounds 10a and b.
10. McKeown, S. C.; Hall, A.; Giblin, G. M. P.; Lorthioir, O.;
Blunt, R.; Lewell, X. Q.; Wilson, R. J.; Brown, S. H.;
Chowdhury, A.; Coleman, T.; Watson, S. P.; Chessell, I.
P.; Pipe, A.; Clayton, N.; Goldsmith, P. Bioorg. Med.
Chem. Lett. 2006, 16, 4767.
References and notes
11. Logarithm (base 10) of the distribution coefficient (D),
where D is the ratio of equilibrium concentrations of all
species of a compound partitioned between n-octanol and
water (buffered to pH 7.4). All values are measured.
12. Complete Freund’s Adjuvant model of inflammatory pain
was used. See Ref. 2a.
13. A series of dibenzoxazepines has been reported to dem-
onstrate analgesic efficacy in the mouse phenylbenzoqui-
none-induced writing model when dosed intragastrically
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0.9% (w/v) saline containing 2% (v/v) DMSO and 20% (w/
v) Kleptose. Compounds 6j, 8h and 9a were dissolved in
0.9% (w/v) saline containing 2% (v/v) DMSO and 10% (w/
v) Kleptose at. Compounds 8i and 8k were dissolved in
0.9% (w/v) saline containing 2% (v/v) DMSO, 20% (w/v)
Kleptose with a molar equivalent NaOH. All formulations
were made at a concentration of 0.1 mg free compound/
mL and were filtered with 0.22 lm Millex-GV filter prior
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saline containing 2% (v/v) DMSO and 20% (w/v) Kleptose
and administered as an intravenous infusion over 18 h at a
dose rate of 5 mL/kg/h (0.518 mg/kg/h) to a male Sprague–
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