in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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96 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ Na + channels<br />
Na + - site 2 - antagonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0169<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Profile<br />
High-throughput profile<br />
Diversity profile<br />
BioPr<strong>in</strong>t ® profile<br />
Organ safety profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
rat cerebral cortex<br />
[ 3 H]batrachotox<strong>in</strong><strong>in</strong> (10 nM)<br />
91 nM<br />
veratrid<strong>in</strong>e (300 µM)<br />
veratrid<strong>in</strong>e (IC 50 : 4.5 µM)<br />
Brown, G.B. (1986) J. Neurosci., 6: 2064-2070.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
0<br />
-10 -9 -8 -7 -6 -5 -4 -3<br />
log [drug] (M)<br />
veratrid<strong>in</strong>e<br />
tetrodotox<strong>in</strong><br />
lidoca<strong>in</strong>e<br />
Na +<br />
cellul ar<br />
Ref. 0219 Activator effect<br />
Ref. 0220 Inhibitor effect<br />
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Source<br />
SK-N-SH cells<br />
Measured product 22 Na uptake<br />
Detection method sc<strong>in</strong>tillation count<strong>in</strong>g<br />
Activator effect Control veratrid<strong>in</strong>e (0.1 mM)<br />
Reference veratrid<strong>in</strong>e (EC 50 : 7 µM)<br />
Inhibitor effect Stimulant veratrid<strong>in</strong>e (100 µM)<br />
Reference tetrodotox<strong>in</strong> (IC 50 : 6 nM)<br />
Jacques, Y. et al. (1978) J. Biol. Chem., 253: 7383-7392..<br />
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[Solvent] must be kept 0.1%<br />
Na V 1.5 (automated patch-clamp)<br />
cellul ar<br />
Ref. 2393<br />
Q 2 weeks<br />
electrophysiology<br />
Source<br />
Na V 1.5 HEK-293 cell l<strong>in</strong>e<br />
Test concentration 0.1, 1, and 10 µM<br />
Detection method automated whole-cell patch-clamp<br />
Reference<br />
tetraca<strong>in</strong>e (IC 50 : 2.5 µM)<br />
Krafte, D. et al. (1995) J. Mol. Cell Cardiol. 27:823-830<br />
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Na V 1.5 (conventional patch-clamp)<br />
cellul ar<br />
Ref. 1938<br />
Q 2 weeks<br />
electrophysiology<br />
Source<br />
Na V 1.5 HEK-293 cell l<strong>in</strong>e<br />
Test concentration 10 µM<br />
Detection method conventional whole-cell patch-clamp<br />
Reference<br />
tetraca<strong>in</strong>e (IC 50 : 4.0 µM)<br />
Krafte, D. et al. (1995) J. Mol. Cell Cardiol. 27:823-830<br />
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❚<br />
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transient receptor potential channels<br />
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TRPM8<br />
cellul ar<br />
Ref. 3316<br />
Ref. 3317<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Measured product <strong>in</strong>tracellular [Ca 2+ ]<br />
Detection method fluorimetry<br />
Agonist effect Control icil<strong>in</strong> (3 µM)<br />
Reference icil<strong>in</strong> (EC 50 : 63 nM)<br />
Antagonist effect Stimulant icil<strong>in</strong> (100 nM)<br />
Reference BCTC (IC 50 : 1400 nM)<br />
Behrendt, H.J., (2004) Br. J. Pharmacol., 141: 737-745.<br />
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[Solvent] must be kept 0.1%
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