in vitro PHARMACOLOGY 2011 CATALOG - Cerep

60 in vitro pharmacology 2011 catalog
❚ opioid and opioid-like
kappa (KOP)
cellul ar
Ref. 2071
Ref. 2072
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
rat recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control U 50488 (1 µM)
Reference U 50488 (EC 50 : 1.1 nM)
Antagonist effect Stimulant U 50488 (100 nM)
Reference nor-BNI (IC 50 : 9.2 nM)
Avidor-Reiss, T. et al. (1995) FEBS Lett., 361: 70-74.
cAMP modulation (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
U 50488
U 69593
DAMGO
DPDPE
100
50
0
log [antagonist] (M)
nor-BNI
naloxone
naltrexone
DGNTI
kappa (KOP)
tissue
Ref. 0329
Q 4 weeks
Source
rabbit vas deferens (field-stimulated)
Agonist U 69593 (pD 2 = 7.8)
Antagonist nor-BNI (pA 2 = 10.8)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Oka, T. et al. (1980) Eur. J. Pharmacol., 73: 235-236.
tension (% of control)
-12 -11
-12 -11
-11 -10
100-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
-10 -9 -8 -7 -6
log [agonist] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
nor-BNI
none
0.1 nM
0.3 nM
1 nM
mu (MOP) - antagonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]diprenorphine (0.4 nM)
Kd
0.14 nM
Non specific naltrexone (1 µM)
binding
Reference naltrexone (IC 50 : 1.1 nM)
Ref. 1666
Q 3 weeks
Zhang, S. et al. (1998) J. Pharmacol. Exp. Ther., 286: 136-141.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
naltrexone
DAMGO
U 50488
DPDPE
mu (MOP) - agonist radioligand
binding
Ref. 0118
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
mu (MOP)
cellul ar
Ref. 1392
Ref. 1393
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]DAMGO (0.5 nM)
0.35 nM
naloxone (10 µM)
DAMGO (IC 50 : 0.537 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
Wang, J.-B. et al. (1994) FEBS Lett., 338: 217-222.
[Custom offer] rat brain model (Ref. 0117), please contact us at customresearch@cerep.com
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control DAMGO (1 µM)
Reference DAMGO (EC 50 : 2.8 nM)
Antagonist effect Stimulant DAMGO (30 nM)
Reference CTOP (IC 50 : 335 nM)
Wang, J.B. et al. (1994) FEBS Lett., 338: 217-222.
cAMP modulation (% of control)
100
50
0
log [agonist] (M)
DAMGO
DPDPE
fentanyl
morphine
100
[Solvent] must be kept ≤ 0.3%
DAMGO
naloxone
U 50488
DPDPE
-12 -11 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6 -5
50
0
log [antagonist] (M)
CTOP
naltrexone
naltrindole
naloxone
mu (MOP)
tissue
Ref. 0330
Q 4 weeks
Source
guinea-pig ileum (field-stimulated)
Agonist DAMGO (pD 2 = 8.3)
Antagonist naloxone (pA 2 = 8.8)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Hutchinson, M. et al. (1975) Brit. J. Pharmacol., 55: 541-546.
tension (% of control)
-12 -11
-12 -11
-11 -10
100-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
log [agonist] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
naloxone
none
3 nM
10 nM
30 nM