in vitro PHARMACOLOGY 2011 CATALOG - Cerep

adrenergic ❚
21
beta 3
cellul ar
Ref. 2189
Ref. 0020
Q 3 weeks
Agonist effect
Antagonist effect
Source
SK-N-MC cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control isoproterenol (100 µM)
Reference isoproterenol (EC 50 : 2.7 µM)
Antagonist effect Stimulant isoproterenol (5 µM)
Reference cyanopindolol (IC 50 : 300 nM)
Curran, P.K. and Fishman, P.H. (1996) Cell signal., 8: 355-364.
[Solvent] must be kept 0.3%
Cerep
services
Receptors
[GPCRs]
beta 3
tissue
Ref. 0300
Q 4 weeks
Source
rat colon (precontracted with 30 mM KCl)
Agonist isoproterenol (pD 2 = 6.6)
Antagonist (-)cyanopindolol (pA 2 = 8.8)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
McLaughlin, D.P. and Macdonald, A. (1990) Brit. J. Pharmacol., 101: 569-574.
tension (% of control)
100
50
(-)cyanopindolol
none
0.1 µM
0
1 µM
10 µM
-10 -9 -8 -7 -6 -5 -4 -3
log [agonist] (M)
Ion
channels
Transporters
❚ Angiotensin II
Kinases
AT 1 - antagonist radioligand
binding
Ref. 0024
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 (HEK-293 cells)
[ 125 I][Sar 1 ,Ile 8 ]-AT-II (0.05 nM)
0.05 nM
angiotensin-II (10 µM)
saralasin (IC 50 : 0.63 nM)
Le, M.T. et al. (2005) Eur. J. Pharmacol., 513: 35-45.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
saralasin
ZD 7155
angiotensin-II
PD 123319
Epigenetic &
DNA-related
enzymes
Other
enzymes
AT 1
cellul ar
Ref. 1912
Ref. 1913
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control angiotensin-II (100 nM)
Reference angiotensin-II (EC 50 : 0.85 nM)
Antagonist effect Stimulant angiotensin-II (3 nM)
Reference saralasin (IC 50 : 16.8 nM)
Martin, M.M. et al. (2001) Mol. Endocrinol. 15: 281-293.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11
-10 -9 -8 -7 -6 -5
log [agonist] (M)
angiotensin-II
angiotensin-I
CGP 42112A
100
[Solvent] must be kept ≤ 0.1%
50
0
-11 -10 -9 -8 -7
-12 -6
log [antagonist] (M)
saralasin
ZD 7255
[Sar 1 ,leu 8 ]-AT-II
PD 123319
Specialized
cellular
assays
Standard
profiles
AT 1
tissue
Ref. 0301
Q 4 weeks
Source
rabbit aorta
Agonist angiotensin-II (pD 2 = 8.9)
Antagonist saralasin (pA 2 = 9.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Pendleton, G.G. et al. (1989) J. Pharmacol. Exp. Ther., 248: 637-643.
tension (% of max.)
-12 -11
-12 -11
-12 -11
100-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-10 -9 -8 -7
log [agonist] (M)
-11 -10 -9 -8 -7 -6 -5 -4 -3
-9 -8 -7 -6 -5 -4
saralasin
none
3 nM
10 nM
30 nM
Testing
conditions
Ordering
information
-11 -10
-9 -8 -7 -6 -5 -4
For further details and updated information on assays:
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Assay list
& index