in vitro PHARMACOLOGY 2011 CATALOG - Cerep

voltage-gated channels [K + channels] ❚
95
K ATP
tissue
Source
rat aorta (precontracted with 20 mM KCl)
Agonist cromakalim (pD 2 = 7.2)
Antagonist glibenclamide (pA 2 = 7.4)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
tension (% of control)
100
50
0
glibenclamide
none
0.1 µM
0.3 µM
1 µM
Cerep
services
Ref. 0340
Q 4 weeks
[Solvent] must be kept ≤ 0.1%
Newgreen, D.T. et al. (1990) Brit. J. Pharmacol., 100: 605-613.
-9 -8 -7 -6 -5
log [agonist] (M)
Receptors
K V - antagonist radioligand
binding
Ref. 0166
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]α-dendrotoxin (0.01 nM)
0.04 nM
α-dendrotoxin (50 nM)
α-dendrotoxin (IC 50 : 0.1 nM)
Sorensen, R.G. and Blaustein, M.P. (1989) Mol. Pharmacol., 36: 689-698.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
α-dendrotoxin
charybdotoxin
apamin
glibenclamide
Ion
channels
Transporters
SK Ca - antagonist radioligand
binding
Ref. 0167
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]apamin (7 pM)
7 pM
apamin (100 nM)
apamin (IC 50 : 0.0091 nM)
Hugues, M. et al. (1982) J. Biol. Chem., 257: 2762-2769.
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
apamin
charybdotoxin
glibenclamide
Kinases
Epigenetic &
DNA-related
enzymes
selected cerep assays
❚ ion channel patch-clamp assays
Electrophysiological assays are developed using both conventional (manual) and automated patch-clamp (Qpatch) to measure agonist,
antagonist and modulator effect of compounds.
The automated patch-clamp system is based on planar glass-coated silicon chips with micro-etched patch-clamp holes. It performs a true
giga-ohm seal patch-clamp, which is the principle used in conventional patch-clamp. Mammalian cell lines (HEK-293 or CHO-K1) stably
expressing various ion channel genes are used. The automated patch-clamp performs multiple independent patch-clamp experiments in
parallel in a disposable electrode array.
❚ 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.
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index