in vitro PHARMACOLOGY 2011 CATALOG - Cerep

32 in vitro pharmacology 2011 catalog
❚ corticotropin releasing factor
CRF 2a - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I]sauvagine (0.1 nM)
binding
Kd
0.05 nM
Ref. 2036
Non specific urocortine (1 µM)
Q 3 weeks
Reference sauvagine (IC 50 : 1.1 nM)
Included in:
Organ safety profile
Dautzenberg, F.M. et al. (2001) J. Pharmacol. Exp. Ther., 296: 113-120.
α
CRF 2a
cellul ar
Ref. 2085
Ref. 2086
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control human CRF (1 µM)
Reference human CRF (EC 50 : 11 nM)
Antagonist effect Stimulant human CRF (30 nM)
Reference astressin (IC 50 : 22 nM)
Dautzenberg, F.M. et al. (2001) J. Pharmacol. Exp. Ther., 296: 113-120.
cAMP modulation (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
-10 -9 -8 -7 -6 -5
log [agonist] (M)
human CRF
sauvagine
urocortin
urotensin-I
100
[Solvent] must be kept ≤ 0.3%
50
0
log [antagonist] (M)
astressin
α-helical-CRF
-11 -10 -9 -8 -7 -6 -5 -4
❚ For Cytokine assays, see "Other receptors", page 83
-12 -11 -10 -9 -8 -7
-13 -12 -11 -10 -9 -8
-11 -10 -9 -8 -7 -6 -5 -4
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4
❚ dopamine
D 1 - antagonist radioligand
binding
Ref. 0044
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 (CHO cells)
[ 3 H]SCH 23390 (0.3 nM)
0.2 nM
SCH 23390 (1 µM)
SCH 23390 (IC 50 : 0.242 nM)
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Zhou, Q.-Y. et al. (1990) Nature, 347: 76-80.
[CUSTOM OFFER] rat striatum model (Ref. 0043), please contact us at customresearch@cerep.com
SCH 23390
A68930
dopamine
SKF 82958
D 1
cellul ar
Ref. 1685
Ref. 1686
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 dopamine (10 µM)
Reference dopamine (EC 50 : 58 nM)
Antagonist effect Stimulant dopamine (300 nM)
Reference SCH 23390 (IC 50 : 1.7 nM)
Zhou, Q.-Y. et al. (1990) Nature, 347: 76-80.
cAMP modulation (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
dopamine
7-OH-DPAT
A68930
bromocriptyne
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
log [antagonist] (M)
SCH 23390
L-741,626
L-745,870
GR 103691
D 1
tissue
Ref. 0309
Q 4 weeks
Source
rabbit splenic artery
(precontracted with 0.1 µM U-46619)
Agonist SKF 82958 (pD 2 = 6.7)
Antagonist SCH 23390
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Zanzottera, D. et al. (1998) Brit. J. Pharmacol., 123: 730-736.
tension (% of control)
-13
100
50 -12 -11 -10 -9 -8 -7 -6 -5
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-9 -8 -7 -6 -5
-10 -4
0
-8 -7 -6 -5
log [agonist] (M)