in vitro PHARMACOLOGY 2011 CATALOG - Cerep

17
alpha 1B - antagonist radioligand
binding
Ref. 1633
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]prazosin (0.15 nM)
0.055 nM
phentolamine (10 µM)
prazosin (IC 50 : 0.25 nM)
specific binding (% of control)
100
50
0
-12
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Ford, A.P.D.W. et al. (1997) Brit. J. Pharmacol., 121: 1127-1135.
[CUSTOM OFFER] rat liver model (Ref. 0010), please contact us at customresearch@cerep.com
adrenergic ❚
prazosin
BMY7378
oxymetazoline
phenylephrine
Cerep
services
Receptors
[GPCRs]
alpha 1B
cellul ar
Ref. 1901
Ref. 1902
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control epinephrine (10 µM)
Reference epinephrine (EC 50 : 207 nM)
Antagonist effect Stimulant epinephrine (1 µM)
Reference L765314 (IC 50 : 24 nM)
Schwinn, D.A. et al. (1995) J. Pharmacol. Exp. Ther., 272: 134-142.
cAMP modulation (% of control)
100
100
50
50
0
0
-9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
epinephrine
L765314
norepinephrine
prazosin
M6434
BMY7378
phenylephrine
corynanthine
Ion
channels
Transporters
alpha 1D - antagonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]prazosin (0.2 nM)
binding
Kd
0.15 nM
Ref. 1942
Non specific phentolamine (10 µM)
Q 3 weeks
Reference prazosin (IC 50 : 0.38 nM)
Included in:
Organ safety profile
Kenny, B.A. et al. (1995) Brit. J. Pharmacol., 115: 981-986.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
prazosin
WB 4101
BMY7378
oxymetazoline
Kinases
Epigenetic &
DNA-related
enzymes
alpha 2 (non-selective) - antagonist radioligand
binding
Ref. 0011
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]RX 821002 (0.5 nM)
0.38 nM
(-)epinephrine (100 µM)
yohimbine (IC 50 : 58.7 nM)
Uhlen, S. and Wikberg, J.E. (1991) Pharmacol. Toxicol., 69: 341-350.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
yohimbine
RX 821002
oxymetazoline
prazosin
Other
enzymes
Specialized
cellular
assays
selected cerep assays
❚ 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.
❚ cellular Functional GPCR assays
Functional GPCR assays are cell-based assays to measure agonist-like, inverse agonist, antagonist and modulator activity of compounds.
Various technologies are used: TR-FRET to determine cAMP concentration and IP1 levels, real time fluorescence to monitor calcium flux,
cellular dielectric spectroscopy to measure impedance modulation. Large batches of cells, from which whole cells are frozen and stored
for functional assays, are produced in-house. Cells are quality controlled before use. A novel patented host cell line was designed and
constructed for Gi protein coupled receptors.
❚ 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.
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index