in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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186 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ monoam<strong>in</strong>e & neurotransmitter release<br />
5-HT release (activator effect)<br />
cellul ar<br />
Ref. 0459<br />
[CUSTOM OFFER]<br />
Source<br />
Tracer<br />
Control<br />
Measured product<br />
Detection method<br />
Reference<br />
rat bra<strong>in</strong> synaptosomes<br />
[ 3 H]5-HT<br />
fenfluram<strong>in</strong>e (0.1 mM)<br />
[ 3 H]5-HT release from synaptosomes<br />
sc<strong>in</strong>tillation count<strong>in</strong>g<br />
fenfluram<strong>in</strong>e (EC 50 : 470 nM)<br />
Bonanno, G. et al. (1994) J. Neurochem., 63: 1163-1166.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
5-HT release (<strong>in</strong>hibitor effect)<br />
100<br />
cellul ar<br />
Ref. 0286<br />
[CUSTOM OFFER]<br />
Source<br />
rat mast cells<br />
Tracer<br />
[ 3 H]5-HT (0.2 µCi)<br />
Stimulant<br />
compound 48/80 (0.1 µg/mL)<br />
Measured product 5-HT (endogenous)<br />
Detection method sc<strong>in</strong>tillation count<strong>in</strong>g<br />
Reference<br />
SCG (IC 50 : 4 µM)<br />
[Solvent] must be kept ≤ 0.1%<br />
Theoharides, T.C. et al. (1985) Biochem. Pharmacol., 34: 1389-1398.<br />
5-HT release (% of control)<br />
50<br />
0<br />
-7 -6 -5 -4 -3<br />
log [drug] (M)<br />
SGC<br />
❚ Ion transport systems<br />
Ca 2+ - ATPase pump<br />
cellul ar<br />
Ref. 0216<br />
[CUSTOM OFFER]<br />
Source<br />
rat liver membrane vesicles<br />
Substrate<br />
ATP (1 mM)<br />
Tracer<br />
45 Ca (0.1 µCi)<br />
Measured product<br />
45 Ca uptake<br />
Detection method sc<strong>in</strong>tillation count<strong>in</strong>g<br />
Reference<br />
thapsigarg<strong>in</strong> (IC 50 : 400 nM)<br />
Jean, T. and Klee, C.B. (1986) J. Biol. Chem., 261: 16414-16420.<br />
45 Ca uptake (% of control)<br />
100<br />
50<br />
0<br />
-8 -7 -6 -5<br />
log [drug] (M)<br />
thapsigarg<strong>in</strong><br />
Na + /K + - ATPase pump<br />
100<br />
cellul ar<br />
Ref. 0221<br />
[CUSTOM OFFER]<br />
Source<br />
A7r5 cells<br />
Substrate<br />
endogenous ATP<br />
Tracer<br />
86 Rb (0.1 µCi)<br />
Measured product<br />
86 Rb uptake<br />
Detection method sc<strong>in</strong>tillation count<strong>in</strong>g<br />
Reference<br />
ouaba<strong>in</strong> (IC 50 : 200 µM)<br />
[Solvent] must be kept ≤ 0.3%<br />
Chassande, O. et al. (1988) Eur. J. Biochem., 171: 425-433.<br />
86 Rb uptake (% of control)<br />
50<br />
0<br />
-6 -5 -4 -3<br />
log [drug] (M)<br />
ouaba<strong>in</strong><br />
Na + /Ca 2+ antiport<br />
cellul ar<br />
Ref. 0222<br />
[CUSTOM OFFER]<br />
Source<br />
bov<strong>in</strong>e heart membrane vesicles<br />
Tracer<br />
45 Ca (0.5 µCi)<br />
Measured product<br />
45 Ca uptake<br />
Detection method sc<strong>in</strong>tillation count<strong>in</strong>g<br />
Reference<br />
2’,4’ dichlorobenzamil (IC 50 : 20 µM)<br />
Slaughter, R.S. et al. (1988) Biochemistry, 27: 2403-2409.
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