in vitro PHARMACOLOGY 2011 CATALOG - Cerep

91
❚ Sigma
Cerep
services
sigma (non-selective) - agonist radioligand
binding
Ref. 0146
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]DTG (8 nM)
29 nM
haloperidol (10 µM)
haloperidol (IC 50 : 48 nM)
Shirayama, Y. et al. (1993) Eur. J. Pharmacol., 237: 117-126.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
haloperidol
(+)3-PPP
(+)pentazocine
(+)SKF 10,047
Receptors
[Other
receptors]
Ion
channels
sigma (non-selective)
tissue
Ref. 0337
Q 4 weeks
Source
guinea-pig vas deferens (field-stimulated)
Agonist (+)SKF 10,047 (pD 2 = 4.7)
Antagonist rimcazole
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Vaupel, D.B. and Su, T.P. (1987) Eur. J. Pharmacol., 139: 125-128.
tension (% of max.)
100
50
0
-6 -5 -4
log [agonist] (M)
Transporters
Kinases
sigma 1 - agonist radioligand
Source
Jurkat cells (endogenous)
Ligand
[ 3 H](+)pentazocine (15 nM)
binding
Kd
37 nM
Ref. 0889
Non specific haloperidol (10 µM)
Q 3 weeks
Reference haloperidol (IC 50 : 11.4 nM)
Included in:
Organ safety profile
Ganapathy, M.E. et al. (1999) J. Pharmacol. Exp. Ther., 289: 251-260.
sigma 2 - agonist radioligand
-10 -9 -8 -7 -6 -5 -4 -3
100
-11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
50
-13 -12 -11 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6
-10
haloperidol
(+)3-PPP
-10 -9 -8 -7 -6 -5 -4
0
(+)SKF 10,047
-3
-11 -12 - 10 -11 -9 -10-8 -9 -7-8 -7 -6 -6-5 -5 -4 -4
log [drug] (M)
-9 -8 -7 -12 -11 -10 -6 -5
-11 -10 -9 -8 -7 -6 -5 -4
[Custom offer] guinea-pig brain model (Ref. 0147), please contact us at customresearch@cerep.com
Source
rat cerebral cortex
Ligand
[ 3 H]DTG (5 nM) (+ 300 nM (+)pentazocine)
binding
Kd
32 nM
Ref. 0148
Non specific haloperidol (10 µM)
Q 3 weeks
Reference haloperidol (IC 50 : 120 nM)
Included in:
Organ safety profile
Bowen, W.D. et al. (1993) Mol. Neuropharmacol., 3: 117-126.
specific binding (% of control)
specific binding (% of control)
100
50
haloperidol
0
(+)3-PPP
(+)SKF 10,047
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
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Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index