in vitro PHARMACOLOGY 2011 CATALOG - Cerep

41
❚ Growth hormone-releasing hormone
Cerep
services
GHRH
cellul ar
Ref. 2236
Ref. 2238
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
50
50
Measured product cAMP
Detection method HTRF
0
0
Agonist effect Control human GHRF(1-29) (10 nM)
Reference human GHRF(1-29) (EC
log [agonist] (M)
50 : 0.3 nM)
human GHRH(1-29)
Antagonist effect Stimulant human GHRF(1-29) (1 nM)
GHRF(1-29)
glucagon
Reference [N-acetyl-Tyr 1 ,D-Arg 2 ]-GHRF
secretin
(IC 50 : 16 nM)
[Solvent] must be kept ≤ 0.3%
Gaudreau, P. et al. (1992) J. Med. Chem., 32: 1864-1869.
cAMP modulation (% of control)
100
-10 -9 -8
-12 -11 -10 -9 -8 -7 -6
-11 -10
-9 -8 -7 -6 -5 -4
100
log [antagonist] (M)
[N-acetyl-Tyr 1 ,D-Arg 2 ]-GHRF
JV-1-36
JV-1-38
[des-His 1 -Glu 9 ]-glucagon amide
❚ For Growth factors assays, see "Other receptors", page 87
Receptors
[GPCRs]
Ion
channels
❚ Histamine
H 1 - antagonist radioligand
binding
Ref. 0870
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]pyrilamine (1 nM)
1.7 nM
pyrilamine (1 µM)
pyrilamine (IC 50 : 2.2 nM)
Smit, M.J. et al. (1996) Brit. J. Pharmacol., 117: 1071-1080.
-12 -11
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
log [drug] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4 -3
pyrilamine
histamine
cimetidine
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
H 1 - antagonist radioligand
Source
guinea-pig cerebellum
Ligand
[ 3 H]pyrilamine (0.5 nM)
Kd
0.37 nM
Non specific triprolidine (100 µM)
binding
Reference pyrilamine (IC 50 : 0.39 nM)
Ref. 0077
Q 3 weeks
Dini, S. et al. (1991) Agents and Actions, 33: 181-184.
α
Other
enzymes
Specialized
cellular
assays
H 1
cellul ar
Ref. 2542
Ref. 2543
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control histamine (10 µM)
Reference histamine (EC 50 : 47 nM)
Antagonist effect Stimulant histamine (300 nM)
Reference pyrilamine (IC 50 : 5.7 nM)
Miller, T.R. et al. (1999) J. Biomol. Screen., 4: 249-258.
α
[Solvent] must be kept 0.1%
Standard
profiles
Testing
conditions
H 1
tissue
Ref. 0316
Q 4 weeks
Source
guinea-pig trachea
Agonist 2-PEA (pD 2 = 4.9)
Antagonist pyrilamine (pA 2 = 9.4)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rappen-Cremer, E. et al. (1989) Agents and Actions, 28: 218-223.
tension (% of max.)
100
50
pyrilamine
none
1 nM
0
3 nM
10 nM
-7 -6 -5 -4
log [agonist] (M)
Ordering
information
Assay list
& index