in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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seroton<strong>in</strong> ❚<br />
69<br />
5-HT 1A<br />
cellul ar<br />
Ref. 2093<br />
Ref. 2101<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control 8-OH-DPAT (100 nM)<br />
Reference 8-OH-DPAT (EC 50 : 0.85 nM)<br />
Antagonist effect Stimulant 8-OH-DPAT (10 nM)<br />
Reference WAY 100635 (IC 50 : 20.5 nM)<br />
Newman-Tancredi, A. et al. (2001) Brit. J. Pharmacol., 132: 518-524.<br />
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α<br />
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[Solvent] must be kept 0.3%<br />
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<strong>Cerep</strong><br />
services<br />
<br />
Receptors<br />
[GPCRs]<br />
5-HT 1B - antagonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0132<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Profile<br />
High-throughput 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 />
[ 125 I]CYP (0.1 nM) (+ 30 µM (-)propranolol)<br />
0.16 nM<br />
seroton<strong>in</strong> (10 µM)<br />
seroton<strong>in</strong> (IC 50 : 10 nM)<br />
Hoyer, D. et al. (1985) Eur. J. Pharmacol., 118: 1-12.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
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100<br />
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50 <br />
<br />
seroton<strong>in</strong><br />
ketanser<strong>in</strong><br />
<br />
0<br />
8-OH-DPAT<br />
MDL 72222<br />
-10 -9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
Ion<br />
channels<br />
Transporters<br />
5-HT 1B<br />
cellul ar<br />
Ref. 2600<br />
Ref. 2604<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
CHO cells (endogenous)<br />
Measured product impedance<br />
Detection method cellular dielectric spectroscopy<br />
Agonist effect Control seroton<strong>in</strong> (1 µM)<br />
Reference seroton<strong>in</strong> (EC 50 : 5.3 nM)<br />
Antagonist effect Stimulant seroton<strong>in</strong> (30 nM)<br />
Reference GR 127935 (IC 50 : 9.18 nM)<br />
Giles, H. et al. (1996) Brit. J. Pharmacol., 117: 1119-1126.<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 />
5-HT 1D - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 1974<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 />
rat recomb<strong>in</strong>ant (CHO cells)<br />
[ 3 H]seroton<strong>in</strong> (1 nM)<br />
0.5 nM<br />
seroton<strong>in</strong> (10 µM)<br />
seroton<strong>in</strong> (IC 50 : 1.82 nM)<br />
Wurch T. et al. (1997) J. Neurochem., 68: 410-418.<br />
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Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
5-HT 1D<br />
cellul ar<br />
Ref. 2496<br />
Ref. 2499<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Agonist effect<br />
Antagonist effect<br />
Cellular functional GPCR profile<br />
Source<br />
rat recomb<strong>in</strong>ant (CHO cells)<br />
Measured product impedance<br />
Detection method cellular dielectric spectroscopy<br />
Agonist effect Control seroton<strong>in</strong> (100 nM)<br />
Reference seroton<strong>in</strong> (EC 50 : 0.6 nM)<br />
Antagonist effect Stimulant seroton<strong>in</strong> (3 nM)<br />
Reference methiothep<strong>in</strong> (IC 50 : 408 nM)<br />
Wurch, T. et al. (1997) J. Neurochem., 68: 410-418.<br />
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[Solvent] must be kept 0.1%<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
5-HT 2A - antagonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0135<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Profile<br />
High-throughput 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]ketanser<strong>in</strong> (0.5 nM)<br />
0.6 nM<br />
ketanser<strong>in</strong> (1 µM)<br />
ketanser<strong>in</strong> (IC 50 : 0.73 nM)<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
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50<br />
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0<br />
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-11 -10 -9 -8 -7 -6 -5 -4 -3<br />
log [drug] (M)<br />
Bonhaus, D.W. et al. (1995) Brit. J. Pharmacol., 115: 622-628.<br />
[Custom offer] rat bra<strong>in</strong> model (Ref. 0134), please contact us at customresearch@cerep.com<br />
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ketanser<strong>in</strong><br />
seroton<strong>in</strong><br />
8-OH-DPAT<br />
MDL 72222<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex