in vitro PHARMACOLOGY 2011 CATALOG - Cerep

52 in vitro pharmacology 2011 catalog
❚ muscarinic
M 3
cellul ar
Ref. 1243
Ref. 1244
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control acetylcholine (1 µM)
Reference acetylcholine (EC 50 : 10 nM)
Antagonist effect Stimulant acetylcholine (10 nM)
Reference 4-DAMP (IC 50 : 3.6 nM)
Sur, C. et al. (2003) Proc. Natl. Acad. Sci. USA, 100: 13674-13679.
Ca 2+ mobilization (% of control)
100
50
0
log [agonist] (M)
acetylcholine
oxotremorine-M
carbachol
100
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
4-DAMP
atropine
pirenzepine
M 3
tissue
Ref. 0320
Q 4 weeks
Source
guinea-pig ileum
Agonist carbachol (pD 2 = 6.6)
Antagonist 4-DAMP (pA 2 = 9.2)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Clague, R.U. et al. (1985) Brit. J. Pharmacol., 86: 163-170.
tension (% of max.)
100
50
0
-9 -8 -7 -6 -5 -4
log [agonist] (M)
4-DAMP
none
3 nM
10 nM
30 nM
M 4 - antagonist radioligand
binding
Ref. 0096
Q 3 weeks
Included in:
High-throughput profile
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]4-DAMP (0.2 nM)
0.32 nM
atropine (1 µM)
4-DAMP (IC 50 : 0.53 nM)
Dorje, F. et al. (1991) J. Pharmacol. Exp. Ther., 256: 727-733.
specific binding (% of control)
100
50
0
-12
-11
4-DAMP
atropine
pirenzepine
methoctramine
-10 -9 -8 -7 -6 -5
log [drug] (M)
M 4 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]oxotremorine-M (6 nM)
binding
Kd
4.6 nM
Ref. 1619
Non specific atropine (1 µM)
Q 3 weeks
Reference acetylcholine (IC 50 : 20 nM)
Included in:
Organ safety profile
Van den Beukel, I. et al. (1997) J. Pharmacol. Exp. Ther., 281: 1113-1119.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
acetylcholine
oxotremorine
carbachol
atropine
M 4
cellul ar
Ref. 1670
Ref. 1671
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 acetylcholine (10 µM)
Reference acetylcholine (EC 50 : 33 nM)
Antagonist effect Stimulant acetylcholine (300 nM)
Reference PD 102807 (IC 50 : 280 nM)
Olianas, M.C. and Onali, P. (1999) Life Sc., 65: 2233-2240.
[Solvent] must be kept 0.3%
M 4 - inverse agonist effect
cellul ar
Ref. 2412
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
Control
Reference
[Solvent] must be kept ≤ 0.3%
human recombinant (CHO cells)
tropicamide (10 µM)
tropicamide (EC 50 : 122 nM)
Jakubik, J. et al. (1995) FEBS Lett., 377: 275-279.