in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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182 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ transduction signal enzymes<br />
PLC<br />
❚ phospholipase c<br />
Source<br />
Substrate<br />
Measured product<br />
Detection method<br />
Bacillus cereus<br />
glycero-phosphoethanolam<strong>in</strong>e (GPE)<br />
(100 nM)<br />
diacylglycerol (DAG)<br />
fluorimetry<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Ref. 2837<br />
Q 3 weeks<br />
Reference<br />
D609 (IC 50 : 5.2 µM)<br />
Amtmann, E. (1996) Drugs Exp. Cl<strong>in</strong>. Res., 22: 287-294.<br />
<br />
<br />
<br />
❚ ATPases<br />
<br />
<br />
<br />
<br />
ATPase (Na + /K + )<br />
Ref. 2009<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Diversity profile<br />
BioPr<strong>in</strong>t ® profile<br />
Source<br />
porc<strong>in</strong>e cerebral cortex<br />
Substrate<br />
ATP (2 mM)<br />
Measured product Pi<br />
Detection method photometry<br />
Reference<br />
ouaba<strong>in</strong> (IC 50 : 215 nM)<br />
Fiske, C.M. and Subbarow, Y. (1925) J. Biol. Chem., 66: 375-400.<br />
enzyme activity (% of control)<br />
<br />
100<br />
<br />
<br />
<br />
<br />
50<br />
ouaba<strong>in</strong><br />
melitt<strong>in</strong><br />
0<br />
buffal<strong>in</strong><br />
-9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
ATPase (H + /K + )<br />
Ref. 0445<br />
Q 4 weeks<br />
Source<br />
rabbit stomach fundus<br />
Substrate<br />
pNPP (2 mM)<br />
Measured product pNP<br />
Detection method photometry<br />
Reference<br />
omeprazole (IC 50 : 2.4 µM)<br />
Dantzig, H. et al. (1991) Biochem. Pharmacol., 42: 2019-2026.<br />
<br />
<br />
-10 -9 -8 -7 -6 -5 -4<br />
<br />
-11 -10 -9 -8 -7 -6<br />
-12 -11 -10 -6<br />
-9 -8 -7<br />
<br />
<br />
<br />
<br />
❚ Miscellaneous enzymes<br />
<br />
<br />
acetyl CoA synthetase<br />
Source<br />
yeast<br />
Substrate<br />
[ 14 C]acetate (50 µM)<br />
Measured product [ 14 C]acetyl CoA<br />
Detection method sc<strong>in</strong>tillation count<strong>in</strong>g<br />
Reference<br />
p-HMB (IC 50 : 350 µM)<br />
Ref. 0388<br />
Q 4 weeks<br />
Focke, M. et al. (1990) FEBS Lett., 261: 106-108.<br />
enzyme activity (% of control)<br />
<br />
100<br />
50<br />
0<br />
-5 -3<br />
-4<br />
log [drug] (M)<br />
p-HMB<br />
arg<strong>in</strong>ase 1<br />
Ref. 3117<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant (E. coli)<br />
Substrate<br />
thioarg<strong>in</strong><strong>in</strong>e (1 mM)<br />
Measured product thiol group<br />
Detection method photometry<br />
Reference<br />
BEC (IC 50 : 850 nM)<br />
Han, S. and Viola, R.E. (2001) Anal. Biochem., 295: 117-119.<br />
<br />
<br />
-10 -9 -8 -7 -6 -5 -4<br />
<br />
-11 -10 -9 -8 -7 -6<br />
-12 -11 -10 -6<br />
-9 -8 -7
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