in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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33<br />
dopam<strong>in</strong>e ❚<br />
D 2S - antagonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0046<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Profile<br />
High-throughput profile<br />
Diversity 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]methylspiperone (0.3 nM)<br />
0.15 nM<br />
(+)butaclamol (10 µM)<br />
(+)butaclamol (IC 50 : 1.64 nM)<br />
Grandy, D.K. et al. (1989) Proc. Natl. Acad. Sci. USA, 86: 9762-9766.<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 />
(+)butaclamol<br />
dopam<strong>in</strong>e<br />
SCH 23390<br />
clozap<strong>in</strong>e<br />
<strong>Cerep</strong><br />
services<br />
<br />
Receptors<br />
[GPCRs]<br />
D 2S - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 1322<br />
Q 3 weeks<br />
Included <strong>in</strong>:<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]7-OH-DPAT (1 nM)<br />
0.68 nM<br />
butaclamol (10 µM)<br />
7-OH-DPAT (IC 50 : 0.95 nM)<br />
Grandy, D.K. et al. (1989) Proc. Natl. Acad. Sci. USA, 86: 9762-9766.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
0<br />
7-OH-DPAT<br />
dopam<strong>in</strong>e<br />
spiperone<br />
haloperidol<br />
-10 -9 -8 -7 -6<br />
log [drug] (M)<br />
Ion<br />
channels<br />
Transporters<br />
D 2S<br />
cellul ar<br />
Ref. 2566<br />
Ref. 2569<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
human recomb<strong>in</strong>ant (HEK-293 cells)<br />
Measured product impedance<br />
Detection method cellular dielectric spectroscopy<br />
Agonist effect Control dopam<strong>in</strong>e (3 µM)<br />
Reference dopam<strong>in</strong>e (EC 50 : 2.1 nM)<br />
Antagonist effect Stimulant dopam<strong>in</strong>e (30 nM)<br />
Reference butaclamol (IC 50 : 30.5 nM)<br />
Payne, S.L. et al. (2002) J. Neurochem., 82: 1106-1117.<br />
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[Solvent] must be kept 0.1%<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
D 2L - antagonist radioligand<br />
Source<br />
human recomb<strong>in</strong>ant (HEK-293 cells)<br />
Ligand<br />
[ 3 H]methylspiperone (0.3 nM)<br />
Kd<br />
0.1 nM<br />
Non specific butaclamol (10 µM)<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Reference butaclamol (IC 50 : 2.9 nM)<br />
Ref. 1405<br />
Q 3 weeks<br />
Hall, D.A. and Strange, P.G. (1997) Brit. J. Pharmacol., 121: 731-736.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
<br />
100<br />
<br />
50<br />
<br />
<br />
0<br />
-11 -10 -9 -8 -7 -6 -5 -4 -3<br />
log [drug] (M)<br />
butaclamol<br />
dopam<strong>in</strong>e<br />
clozap<strong>in</strong>e<br />
SCH 23390<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
D 2<br />
tissue<br />
Ref. 0310<br />
Q 4 weeks<br />
Source<br />
rabbit ear artery (field-stimulated)<br />
Agonist qu<strong>in</strong>pirole (pD 2 = 7.3)<br />
Antagonist (-)sulpiride (pA 2 = 7.5)<br />
Test concentrations 3 concentrations, n=2 (2 tissues)<br />
for both activities<br />
[Solvent] must be kept ≤ 0.1%<br />
Ste<strong>in</strong>sland, O.S. and Hieble, J.P. (1978) Science, 199: 443-445.<br />
tension (% of control)<br />
100<br />
50<br />
0<br />
-9 -8 -7 -6<br />
log [agonist] (M)<br />
(-)sulpiride<br />
none<br />
30 nM<br />
100 nM<br />
300 nM<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
D 3 - antagonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0048<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
High-throughput profile<br />
Diversity profile<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]methylspiperone (0.3 nM)<br />
0.085 nM<br />
(+)butaclamol (10 µM)<br />
(+)butaclamol (IC 50 : 1.4 nM)<br />
Mackenzie, R.G. et al. (1994) Eur. J. Pharmacol., 266: 79-85.<br />
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Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex