in vitro PHARMACOLOGY 2011 CATALOG - Cerep

68 in vitro pharmacology 2011 catalog
❚ purinergic
P2Y 6
cellul ar
Ref. 2166
Ref. 2169
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (1321N1 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control UDP (1 µM)
Reference UDP (EC 50 : 13 nM)
Antagonist effect Stimulant UDP (100 nM)
Reference unavailable
Li, Q. et al. (1998) Mol. Pharmacol., 54: 541-546.
Ca 2+ mobilization (% of control)
100
50
0
-9 -8 -7 -6 -5
-10 -4
log [agonist] (M)
UDP
2MeSADP
UTP
MRS 2365
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
❚ See other Purinergic assays, pp. 90 and 101
-11 -10
-9 -8 -7 -6 -5 -4
❚ relaxin
-12 -11
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
RXFP1 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I]H2 relaxin (0.02 nM)
Kd
0.23 nM
Non specific H2 relaxin (100 nM)
binding
Reference H2 relaxin (IC 50 : 1.1 nM)
Ref. 2058
Q 3 weeks
Halls, M.L. et al. (2005) J. Pharm. Exp. Ther., 313: 677-687.
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
H2 relaxin
INSL3
INSL5
relaxin 3B chain
RXFP1
cellul ar
Ref. 2130
Ref. 2131
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control H2 relaxin (100 nM)
Reference H2 relaxin (EC 50 : 3 nM)
Antagonist effect Stimulant H2 relaxin (10 nM)
Reference unavailable
Wilkinson, T.N. et al. (2005) BMC Evol. Biol., 5: 14.
[Solvent] must be kept 0.3%
❚ serotonin
5-HT (non-selective) - agonist radioligand
binding
Ref. 0129
Q 3 weeks
Included in:
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]serotonin (2.5 nM)
2.5 nM
serotonin (10 µM)
serotonin (IC 50 : 1.3 nM)
Peroutka, S.J. and Snyder, S.H. (1979) Mol. Pharmacol., 16: 687-699.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
serotonin
8-OH-DPAT
ketanserin
MDL 72222
5-HT 1A - agonist radioligand
binding
Ref. 0131
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]8-OH-DPAT (0.3 nM)
0.5 nM
8-OH-DPAT (10 µM)
8-OH-DPAT (IC 50 : 0.36 nM)
Mulheron, J.G. et al. (1994) J. Biol. Chem., 269: 12954-12962.
specific binding (% of control)
100
50
8-OH-DPAT
serotonin
ketanserin
0
MDL 72222
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)