in vitro PHARMACOLOGY 2011 CATALOG - Cerep

neuropeptide y ❚
57
Y 1
cellul ar
Ref. 2206
Ref. 2207
Q 3 weeks
Agonist effect
Antagonist effect
Source
SK-N-MC cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control NPY (10 nM)
Reference NPY (EC 50 : 0.25 nM)
Antagonist effect Stimulant NPY (1 nM)
Reference BIBP 3226 (IC 50 : 125 nM)
Wieland, H.A. et al. (1995) J. Pharmacol. Exp. Ther., 275: 143-149.
[Solvent] must be kept 0.3%
Cerep
services
Receptors
[GPCRs]
Y 1
tissue
Ref. 0324
Q 4 weeks
Source
rabbit vas deferens (field-stimulated)
Agonist [Leu 31 ,Pro 34 ]-NPY (pD 2 = 8.1)
Antagonist BIBP 3226
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Doods, H. and Krause, J. (1991) Eur. J. Pharmacol., 204: 101-103.
tension (% of control)
100
50
[Leu 31 ,Pro 34 ]-NPY
0
NPY-(13-36)
-11 -10 -9 -8 -7 -6
log [agonist] (M)
Ion
channels
Transporters
Y 2 - agonist radioligand
binding
Ref. 0107
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
KAN-TS cells
[ 125 I]peptide YY (0.015 nM)
0.01 nM
NPY (1 µM)
NPY (IC 50 : 0.08 nM)
Fuhlendorff, J. et al. (1990) Proc. Natl. Acad. Sci. USA, 87: 182-186.
Kinases
Epigenetic &
DNA-related
enzymes
Y 2
tissue
Ref. 0325
Q 4 weeks
Source
rat vas deferens (field-stimulated)
Agonist NPY-(13-36) (pD 2 = 7.7)
Antagonist BIIE 0246
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Doods, H. and Krause, J. (1991) Eur. J. Pharmacol., 204: 101-103.
tension (% of control)
100
50
0
-10 -9 -8 -7 -6
log [agonist] (M)
NPY-(13-36)
[Leu 31 ,Pro 34 ]-NPY
Other
enzymes
Specialized
cellular
assays
Y 3
tissue
Ref. 0326
Q 4 weeks
Source
rat colon
Agonist NPY (pD 2 = 7)
Antagonist not available
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Dumont, Y. et al. (1993) Eur. J. Pharmacol., 238: 37-45.
tension (% of max.)
100
50
0
-9 -8 -7 -6
log [agonist] (M)
Standard
profiles
Testing
conditions
❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
available?
For some binding assays two models are available using either agonist or antagonist as radioligand.
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas
the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore,
it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding
of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists.
The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information
about its functional activity at the receptor.
Ordering
information
Assay list
& index