in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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19<br />
adrenergic ❚<br />
alpha 2C - antagonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0016<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
BioPr<strong>in</strong>t ® profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
[ 3 H]RX 821002 (2 nM)<br />
0.95 nM<br />
(-)ep<strong>in</strong>ephr<strong>in</strong>e (100 µM)<br />
yohimb<strong>in</strong>e (IC 50 : 1.9 nM)<br />
Devedjian, J.-C. et al. (1994) Eur. J. Pharmacol., 252: 43-49.<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<br />
log [drug] (M)<br />
yohimb<strong>in</strong>e<br />
RX 821002<br />
prazos<strong>in</strong><br />
oxymetazol<strong>in</strong>e<br />
<strong>Cerep</strong><br />
services<br />
<br />
Receptors<br />
[GPCRs]<br />
alpha 2C - agonist radioligand<br />
Source<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Ligand<br />
[ 3 H](-)ep<strong>in</strong>ephr<strong>in</strong>e (1 nM)<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Kd<br />
0.9 nM<br />
Ref. 1682<br />
Non specific RX 821002 (1 µM)<br />
Q 3 weeks<br />
Reference ep<strong>in</strong>ephr<strong>in</strong>e (IC 50 : 2.87 nM)<br />
Included <strong>in</strong>:<br />
Organ safety profile<br />
Bylund, D.B. et al. (1992) Mol. Pharmacol., 42: 1-5.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
0<br />
-11 -10 -9 -8 -7 -6 -5<br />
log [drug] (M)<br />
ep<strong>in</strong>ephr<strong>in</strong>e<br />
oxymetazol<strong>in</strong>e<br />
RX 821002<br />
prazos<strong>in</strong><br />
Ion<br />
channels<br />
Transporters<br />
alpha 2C<br />
cellul ar<br />
Ref. 1736<br />
Ref. 1737<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Agonist effect<br />
Antagonist effect<br />
Cellular functional GPCR profile<br />
Source<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control ep<strong>in</strong>ephr<strong>in</strong>e (1 µM)<br />
Reference ep<strong>in</strong>ephr<strong>in</strong>e (EC 50 : 2.6 nM)<br />
Antagonist effect Stimulant ep<strong>in</strong>ephr<strong>in</strong>e (100 nM)<br />
Reference rauwolsc<strong>in</strong>e (IC 50 : 55 nM)<br />
Regan, J.W. et al. (1988) Biochem., 85: 6301-6305.<br />
cAMP modulation (% of control)<br />
100<br />
50<br />
0<br />
-12 -11<br />
-10 -9 -8 -7 -6 -5<br />
log [agonist] (M)<br />
ep<strong>in</strong>ephr<strong>in</strong>e<br />
oxymetazol<strong>in</strong>e<br />
clonid<strong>in</strong>e<br />
UK 14,304<br />
100<br />
50<br />
0<br />
-9 -8 -7 -6 -5<br />
-10 -4<br />
log [antagonist] (M)<br />
rauwolsc<strong>in</strong>e<br />
yohimb<strong>in</strong>e<br />
prazos<strong>in</strong><br />
RX 821002<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
beta 1 - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0018<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 />
human recomb<strong>in</strong>ant (HEK-293 cells)<br />
[ 3 H](-)CGP 12177 (0.15 nM)<br />
0.39 nM<br />
alprenolol (50 µM)<br />
atenolol (IC 50 : 278 nM)<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
-12 -11<br />
100<br />
-10 -9 -8 -7 -6 -5<br />
50<br />
-9 -8 -7 -6 -5<br />
-10 -4<br />
0<br />
-10 -9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
Lev<strong>in</strong>, M.C. et al. (2002) J. Biol.Chem., 277: 30429-30435.<br />
[CUSTOM OFFER] rat heart model (Ref. 0017), please contact us at customresearch@cerep.com<br />
atenolol<br />
CGP 20712A<br />
propranolol<br />
ICI 118551<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
beta 1<br />
cellul ar<br />
Ref. 1605<br />
Ref. 1606<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Agonist effect<br />
Antagonist effect<br />
Cellular functional GPCR profile<br />
Source<br />
human recomb<strong>in</strong>ant (HEK-293 cells)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control isoproterenol (100 nM)<br />
Reference isoproterenol (EC 50 : 0.3 nM)<br />
Antagonist effect Stimulant isoproterenol (1 nM)<br />
Reference atenolol (IC 50 : 150 nM)<br />
Frielle, T. et al. (1987) Proc. Natl. Acad. Sci. USA, 84: 7920-7924.<br />
cAMP modulation (% of control)<br />
100<br />
100<br />
50<br />
50<br />
0<br />
0<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3 -9 -8 -7 -6 -5 -4<br />
log [agonist] (M)<br />
log [antagonist] (M)<br />
isoproterenol<br />
atenolol<br />
norep<strong>in</strong>ephr<strong>in</strong>e<br />
propranolol<br />
xamoterol<br />
CGP 20712A<br />
salbutamol<br />
ICI 118551<br />
[Solvent] must be kept ≤ 0.3%<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
beta 1 - <strong>in</strong>verse agonist effect<br />
cellul ar<br />
Ref. 2377<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant (HEK-293 cells)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Control<br />
ICI 118551 (10 µM)<br />
Reference ICI 118551 (EC 50 : 93.8 nM)<br />
[Solvent] must be kept ≤ 0.3%<br />
Lattion, A.L. et al. (1999) FEBS Lett., 457: 302-306.<br />
<br />
<br />
<br />
-12 -11 -10 -9 -8 -7 -6 -5<br />
-9 -8 -7 -6 -5<br />
-10 -4<br />
<br />
<br />
<br />
<br />
<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex