in vitro PHARMACOLOGY 2011 CATALOG - Cerep

dopamine ❚
35
D 5
cellul ar
Ref. 1688
Ref. 1689
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (GH4 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control dopamine (1 µM)
Reference dopamine (EC 50 : 21 nM)
Antagonist effect Stimulant dopamine (50 nM)
Reference SCH 23390 (IC 50 : 0.6 nM)
Sunahara, R.K. et al. (1991) Nature, 350: 614-619.
cAMP modulation (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3
log [agonist] (M)
log [antagonist] (M)
dopamine
SCH 23390
SKF 88393
L-741,626
7-OH-DPAT
L-745,870
bromocryptine
GR 103691
❚ See other dopamine assays, page 104
Cerep
services
Receptors
[GPCRs]
-13
-12 -11 -10 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6
Ion
channels
-9 -8 -7 -6 -5
-10 -4
❚ endothelin
-12 -11 -10 -9 -8 -7 -6
-12 -11
-10 -9 -8 -7 -6 -5
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
Transporters
ET A - agonist radioligand
binding
Ref. 0054
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]endothelin-1 (0.03 nM)
0.03 nM
endothelin-1 (100 nM)
endothelin-1 (IC 50 : 0.038 nM)
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
endothelin-1
endothelin-3
sarafotoxin S6c
BQ-788
Buchan, K.W. et al. (1994) Brit. J. Pharmacol., 112: 1251-1257.
[CUSTOM OFFER] rat A-10 cells model (Ref. 0053), please contact us at customresearch@cerep.com
Kinases
Epigenetic &
DNA-related
enzymes
ET A
cellul ar
Ref. 1264
Ref. 2257
Q 3 weeks
Agonist effect
Antagonist effect
Source
SK-N-MC cells (endogenous)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control endothelin-1 (100 nM)
Reference endothelin-1 (EC 50 : 1.1 nM)
Antagonist effect Stimulant endothelin-1 (10 nM)
Reference BQ-123 (IC 50 : 0.37 nM)
Heinroth-Hoffmann, I. et al. (1998) Brit. J. Pharmacol., 125: 1202-1211.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
endothelin-1
BQ-123
endothelin-3
FR 139317
sarafotoxin S6c
BQ-788
BQ-3020
PD 142,893
[Solvent] must be kept ≤ 0.1%
Other
enzymes
Specialized
cellular
assays
ET A
Source
rat aorta (endothelium-denuded)
100-12 -11 -10 -9 -8 -7
-11 -10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4
tissue
Ref. 0311
Q 4 weeks
Agonist endothelin-1 (pD 2 = 8.9)
Antagonist BQ-123
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Warner, T.D. et al. (1993) Brit. J. Pharmacol., 110: 777-782.
tension (% of max.)
-12 -11
-12 -11
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-10 -9 -8 -7
log [agonist] (M)
Standard
profiles
Testing
conditions
ET B - agonist radioligand
binding
Ref. 0056
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]endothelin-1 (0.03 nM)
0.04 nM
endothelin-1 (0.1 µM)
endothelin-3 (IC 50 : 0.0154 nM)
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
endothelin-3
endothelin-1
sarafotoxin S6c
BQ-788
Fuchs, S. et al. (2001) Mol. Med., 7: 115-124.
[CUSTOM OFFER] rat cerebellum model (Ref. 0055), please contact us at customresearch@cerep.com
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information
Assay list
& index