in vitro PHARMACOLOGY 2011 CATALOG - Cerep

51
M 2 - antagonist radioligand
binding
Ref. 0093
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
M 2 - agonist radioligand
binding
Ref. 1626
Q 3 weeks
Included in:
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]AF-DX 384 (2 nM)
4.6 nM
atropine (1 µM)
methoctramine (IC 50 : 32 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Dorje, F. et al. (1991) J. Pharmacol. Exp. Ther., 256: 727-733.
[Custom offer] rat heart model (Ref. 0092), please contact us at customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]oxotremorine-M (1.5 nM)
1.4 nM
atropine (1 µM)
acetylcholine (IC 50 : 3 nM)
Van den Beukel, I. et al. (1997) J. Pharmacol. Exp. Ther., 281: 1113-1119.
muscarinic ❚
methoctramine
atropine
4-DAMP
pirenzepine
Cerep
services
Receptors
[GPCRs]
Ion
channels
Transporters
M 2
cellul ar
Ref. 1658
Ref. 1659
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 acetylcholine (10 µM)
Reference acetylcholine (EC 50 : 107 nM)
Antagonist effect Stimulant acetylcholine (1 µM)
Reference methoctramine (IC 50 : 197 nM)
Michal, P. et al. (2001) Brit. J. Pharmacol., 132: 1217-1228.
cAMP modulation (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-12 -11 -4 -10 -4
log [agonist] (M)
acetylcholine
oxotremorine
metoclopramide
carbachol
100
50
0
log [antagonist] (M)
methoctramine
atropine
4-DAMP
pirenzepine
Kinases
Epigenetic &
DNA-related
enzymes
M 2 - inverse agonist effect
cellul ar
Ref. 2411
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
Control
Reference
[Solvent] must be kept ≤ 0.3%
human recombinant (CHO cells)
tropicamide (10 µM)
tropicamide (EC 50 : 210 nM)
Nelson, C.P. et al. (2006) J. Pharmacol. Exp. Ther, 316: 279-288.
-12 -11
-12 -11
-11 -10
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
Other
enzymes
Specialized
cellular
assays
M 2
tissue
Ref. 0319
Q 4 weeks
Source
guinea-pig left atrium (electrically paced)
Agonist carbachol (pD 2 = 6.4)
Antagonist methoctramine (pA 2 = 6.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Eglen, R.M. et al. (1988) Brit. J. Pharmacol., 95: 1031-1038.
tension (% of control)
100
50
0
-8 -6 -7 -5
log [agonist] (M)
methoctramine
none
0.1 µM
0.3 µM
1 µM
Standard
profiles
Testing
conditions
M 3 - antagonist radioligand
binding
Ref. 0095
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]4-DAMP (0.2 nM)
0.5 nM
atropine (1 µM)
4-DAMP (IC 50 : 0.46 nM)
Peralta, E.G. et al. (1987) Embo. J., 6: 3923-3929.
specific binding (% of control)
100
50
0
-12
-11
-10 -9 -8 -7 -6 -5
log [drug] (M)
4-DAMP
atropine
pirenzepine
methoctramine
Ordering
information
Assay list
& index