in vitro PHARMACOLOGY 2011 CATALOG - Cerep

64 in vitro pharmacology 2011 catalog
❚ prostanoid
EP 1 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]PGE 2 (1.5 nM)
Kd
1.5 nM
Non specific PGE 2 (10 µM)
binding
Reference PGE 2 (IC 50 : 1.4 nM)
Ref. 0440
Q 3 weeks
Sharif, N.A. and Davis, T.L. (2002) J. Pharm. Pharmacol., 54: 539-547.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
PGE2
AH 6809
butaprost
AH 23848
EP 1
cellul ar
Ref. 2053
Ref. 2054
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control PGE 2 (100 nM)
Reference PGE 2 (EC 50 : 0.88 nM)
Antagonist effect Stimulant PGE 2 (3 nM)
Reference SC 51322 (IC 50 : 53.7 nM)
Ungrin, M.D. et al. (1999) Analytical Biochem., 272: 34-42.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
PGE2
17-phenyl PGE2
PGF2α
U 44069
100
[Solvent] must be kept ≤ 0.1%
50
0
-9 -8 -7 -6 -5
log [antagonist] (M)
SC 51322
AL 8810
AH 23848
AH 6809
EP 2 - agonist radioligand
binding
Ref. 1955
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]PGE 2 (3 nM)
3 nM
PGE 2 (10 µM)
PGE 2 (IC 50 : 1.7 nM)
Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293.
-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
EP 2
cellul ar
Ref. 1956
Ref. 1957
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control PGE 2 (10 µM)
Reference PGE 2 (EC 50 : 100 nM)
Antagonist effect Stimulant PGE 2 (300 nM)
Reference AH 6809 (IC 50 : 3.9 µM)
Wilson, R.J. et al. (2004) Eur. J. Pharmacol., 501: 49-58.
cAMP modulation (% of control)
100
100
50
50
0
0
-9 -8 -7 -6 -5
-8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
PGE2
AH 6809
butaprost
AH 23848
AH 13205
U 44069
[Solvent] must be kept ≤ 0.3%
EP 3 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]PGE 2 (0.5 nM)
Kd
0.8 nM
Non specific PGE 2 (1 µM)
binding
Reference sulprostone (IC 50 : 2.9 nM)
Ref. 2774
Q 3 weeks
Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293.
-12 -11
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
EP 3
cellul ar
Ref. 2577
Ref. 2578
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control sulprostone (10 nM)
Reference sulprostone (EC 50 : 0.058 nM)
Antagonist effect Stimulant sulprostone (0.1 nM)
Reference unavailable
Asboth, G. et al. (1996) Endocrinol., 137: 2572-2579.
[Solvent] must be kept 0.1%