in vitro PHARMACOLOGY 2011 CATALOG - Cerep

72 in vitro pharmacology 2011 catalog
❚ serotonin
5-HT 4e - antagonist radioligand
binding
Ref. 0501
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]GR 113808 (0.3 nM)
0.15 nM
serotonin (100 µM)
serotonin (IC 50 : 170 nM)
Mialet, J. et al. (2000) Brit. J. Pharmacol., 129: 771-781.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
serotonin
GR 113808
ketanserin
8-OH-DPAT
5-HT 4e
cellul ar
Ref. 1044
Ref. 1045
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 serotonin (1 µM)
Reference serotonin (EC 50 : 5.2 nM)
Antagonist effect Stimulant serotonin (30 nM)
Reference GR 113808 (IC 50 : 0.3 nM)
Mialet, J. et al. (2000) Brit. J. Pharmacol., 129: 771-781.
cAMP modulation (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3
log [agonist] (M)
log [antagonist] (M)
serotonin
GR 113808
RS 67506
ketanserin
cisapride
5-CT
5-HT 4
tissue
Ref. 0336
Q 4 weeks
Source
guinea-pig colon
Agonist serotonin (pD 2 = 7.1)
Antagonist GR 113808 (pA 2 = 9.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Gale, J.D. et al. (1994) Brit. J. Pharmacol., 111: 332-338.
tension (% of max.)
-12 -11
-12 -11
-11 -10 -9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7
100
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5 -4
GR 113808
none
1 nM
3 nM
0
10 nM
-9 -8 -7 -6 -5 -4
log [agonist] (M)
5-HT 5a - agonist radioligand
binding
Ref. 0140
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]LSD (1.5 nM)
1.5 nM
serotonin (100 µM)
serotonin (IC 50 : 120 nM)
Rees, S. et al. (1994) FEBS Lett., 355: 242-246.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
serotonin
methiothepin
8-OH-DPAT
ketanserin
5-HT 6 - agonist radioligand
binding
Ref. 0142
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]LSD (2 nM)
1.8 nM
serotonin (100 µM)
serotonin (IC 50 : 150 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Monsma, F.J. et al. (1993) Mol. Pharmacol., 43: 320-327.
[custom offer] rat cDNA model (Ref. 0141), please contact us at customresearch@cerep.com
serotonin
methiothepin
MDL 72222
8-OH-DPAT
5-HT 6
cellul ar
Ref. 1627
Ref. 1628
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 serotonin (10 µM)
Reference serotonin (EC 50 : 20 nM)
Antagonist effect Stimulant serotonin (100 nM)
Reference methiothepin (IC 50 : 65 nM)
Kohen, R. et al. (1996) J. Neurochem., 66: 47-56.
cAMP modulation (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
serotonin
5-methoxytryptamine
5-CT
100
50
0
-10 -9 -8 -7 -6 -5
log [antagonist] (M)
methiothepin
SB 285585
Ro 046790
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7