in vitro PHARMACOLOGY 2011 CATALOG - Cerep

101
❚ purinergic channels
Cerep
services
P2X - agonist radioligand
binding
Ref. 0127
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat urinary bladder
[ 3 H]α,β-MeATP (3 nM)
2.6 nM
α,β-MeATP (10 µM)
α,β-MeATP (IC 50 : 3.5 nM)
Bo, X. and Burnstock, G. (1990) Brit. J. Pharmacol., 101: 291-296.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
α,β-MeATP
suramin
adenosine
Receptors
Ion
channels
P2X
tissue
Ref. 0332
Q 4 weeks
Source
rabbit ear artery (endothelium-denuded)
Agonist α,βMeATP (pD 2 = 6.9)
Antagonist suramin (pA 2 = 4.9)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
O’Connor, S.E. et al. (1990) Brit. J. Pharmacol., 101: 640-644.
❚ serotonin channels
5-HT 3 - antagonist radioligand
binding
Ref. 0411
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
5-HT 3
tissue
Ref. 0335
Q 4 weeks
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]BRL 43694 (0.5 nM)
1.15 nM
MDL 72222 (10 µM)
MDL 72222 (IC 50 : 10 nM)
Hope, A.G. et al. (1996) Brit. J. Pharmacol., 118: 1237-1245.
Source
selected cerep assays
guinea-pig colon
Agonist serotonin (pD 2 = 5.6)
Antagonist MDL 72222 (pA 2 = 5.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Butler, A. et al. (1990) Brit. J. Pharmacol., 101: 591-598.
tension (% of max.)
100
50
0
-9 -8 -7 -6 -5 -4
log [agonist] (M)
suramin
none
30 µM
100 µM
300 µM
❚ See other Purinergic assays, pp.67 and 90
specific binding (% of control)
tension (% of max.)
100
50
0
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
-8 -7 -6 -5 -4
log [agonist] (M)
MDL 72222
serotonin
8-OH-DPAT
ketanserin
MDL 72222
none
1 µM
3 µM
10 µM
❚ See other Serotonin assays, pp. 69, 90 and 105
❚ binding assays
Binding assays are developed according to the competition assay principle. There are three assay formats used: filtration, scintillation proximity
assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified). Large batches of
cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are quality controlled before use.
❚ tissue bioassays
Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and
ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory,
gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the contractile
activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in the tissue used.
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index