in vitro PHARMACOLOGY 2011 CATALOG - Cerep

50 in vitro pharmacology 2011 catalog
❚ motilin
motilin
cellul ar
Ref. 1321 Agonist effect
Ref. 1894 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control motilin (3 nM)
Reference motilin (EC 50 : 0.011 nM)
Antagonist effect Stimulant motilin (0.3 nM)
Reference unavailable
Dass, N.B. et al. (2003) Brit. J. Pharmacol. 140: 948-954.
Ca 2+ mobilization (% of control)
100
50
0
-13
-12 -11
log [agonist] (M)
motilin
[Nleu 13 ]-motilin
erythromycin
-10 -9 -8 -7 -6 -5
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
-11 -10
-9 -8 -7 -6 -5 -4
❚ muscarinic
-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
M (non-selective) - antagonist radioligand
binding
Ref. 0089
Q 3 weeks
Included in:
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]QNB (0.05 nM)
0.01 nM
atropine (1 µM)
atropine (IC 50 : 0.45 nM)
Richards, M.H. (1990) Brit. J. Pharmacol., 99: 753-761.
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
atropine
4-DAMP
methoctramine
pirenzepine
M 1 - antagonist radioligand
binding
Ref. 0091
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]pirenzepine (2 nM)
13 nM
atropine (1 µM)
pirenzepine (IC 50 : 22 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
-12 -4
log [drug] (M)
Dorje, F. et al. (1991) J. Pharmacol. Exp. Ther., 256: 727-733.
[Custom offer] rat brain model (Ref. 0090), please contact us at customresearch@cerep.com
pirenzepine
methoctramine
atropine
4-DAMP
M 1
cellul ar
Ref. 1262
Ref. 1474
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 (100 nM)
Reference acetylcholine (EC 50 : 0.76 nM)
Antagonist effect Stimulant acetylcholine (3 nM)
Reference pirenzepine (IC 50 : 96 nM)
Sur, C. et al. (2003) Proc. Natl. Acad. Sci. USA, 100: 13674-13679.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
acetylcholine
pirenzepine
carbachol
atropine
4-DAMP
methoctramine
[Solvent] must be kept ≤ 0.1%
M 1
tissue
Ref. 0318
Q 4 weeks
Source
rabbit vas deferens (field-stimulated)
Agonist McN-A-343 (pD 2 = 6.4)
Antagonist pirenzepine (pA 2 = 8.2)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Eltze, M. (1988) Eur. J. Pharmacol., 151: 205-221.
tension (% of control)
100
-11 -10 -9 -8 -7 -6 -5 -4
-1350
-12 -11 -10 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6
-9 -8 -7 -6 -5
-10 -4
-12 -11 -10 -9 -8 -7 -6
0
-12 -11 -10 -9 -8 -7 -6 -5
-8 -7 -6 -5 -4
log [agonist] (M)
pirenzepine
none
10 nM
-12 -11 -10 -9 -8 -7 30 -6nM-5 -4 -3
100 nM
For further details and updated information on assays:
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Assay developed in 2010 New assay conditions Human Q Standard turnaround time