in vitro PHARMACOLOGY 2011 CATALOG - Cerep

-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
bombesin ❚
23
BB 1
cellul ar
Ref. 2846
Ref. 2852
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control neuromedin B (10 nM)
Reference neuromedin B (EC 50 : 0.007 nM)
Antagonist effect Stimulant neuromedin B (0.1 nM)
Reference PD 168368 (IC 50 : 200 nM)
Mason, S. et al. (2002) Eur. J. Pharmacol., 438: 25-34.
[Solvent] must be kept 0.1%
Cerep
services
Receptors
[GPCRs]
BB 1
tissue
Ref. 0303
Q 4 weeks
Source
rat urinary bladder
Agonist bombesin (pD 2 = 7.9)
Antagonist not available
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rouissi, N. et al. (1991) Brit. J. Pharmacol., 103: 1141-1147.
tension (% of max.)
100
50
0
-9 -7
-10 -8
log [agonist] (M)
Ion
channels
Transporters
BB 2 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I][Tyr 4 ]bombesin (0.04 nM)
binding
Kd
0.04 nM
Ref. 1986
Non specific bombesin (1 µM)
Q 3 weeks
Reference GRP (IC 50 : 0.041 nM)
Included in:
Organ safety profile
Ashnood, V. et al. (1998) Bio. Med. Chem. Lett., 8: 2589-2594.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
GRP
bombesin
neuromedin B
ICI 216,140
Kinases
Epigenetic &
DNA-related
enzymes
BB 2
cellul ar
Ref. 1915
Ref. 1916
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control GRP (3 nM)
Reference GRP (EC 50 : 0.015 nM)
Antagonist effect Stimulant GRP (0.1 nM)
Reference ICI 216,140 (IC 50 : 510 nM)
Mason, S. et al. (2002) Eur. J. Pharmacol., 438: 25-34.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-13 -12 -11 -10 -9 -8 -7
-9 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
GRP
ICI 216,140
Bn(6-14)
bombesin
neuromedin B
[Solvent] must be kept ≤ 0.1%
Other
enzymes
Specialized
cellular
assays
BB 3 - agonist radioligand
binding
Ref. 0472
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]Bn(6-14) (0.1 nM)
0.16 nM
Bn(6-14) (1 µM)
Bn(6-14) (IC 50 : 8.5 nM)
Mantey, S.A. et al. (1997) J. Biol. Chem., 272: 26062-26071.
-11 -10
-12 -11
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-12 -11
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10 -9 -8 -7 -6 -5 -4 -3
-13 -12
-11 -10 -9 -8 -7
Standard
profiles
Testing
conditions
BB 3
cellul ar
Ref. 1319
Ref. 1764
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control Bn(6-14) (1 µM)
Reference Bn(6-14) (EC 50 : 9.7 nM)
Antagonist effect Stimulant Bn(6-14) (30 nM)
Reference unavailable
Weber, D. et al. (2003) J. Med. Chem., 46: 1918-1930.
Ca 2+ mobilization (% of control)
100
50
0
-10
-9 -8 -7 -6 -5
log [agonist] (M)
Bn(6-14)
bombesin
neuromedin B
GRP
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
Ordering
information
Assay list
& index
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4