in vitro PHARMACOLOGY 2011 CATALOG - Cerep

104 in vitro pharmacology 2011 catalog
❚ dopamine
dopamine transporter - antagonist radioligand
binding
Ref. 0052
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
dopamine uptake
cellul ar
Ref. 0394
Q 3 weeks
❚ gaba
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]BTCP (4 nM)
4.5 nM
BTCP (10 µM)
BTCP (IC 50 : 7.1 nM)
specific binding (% of control)
100
50
0
-11 - 10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
Pristupa, Z.B. et al. (1994) Mol. Pharmacol., 45: 125-135.
[Custom offer] rat striatum model (Ref. 0051), please contact us at customresearch@cerep.com
Source
rat striatum synaptosomes
Tracer
[ 3 H]DA (0.2 µCi/ml)
Measured product [ 3 H]DA incorporation into synaptosomes
Detection method scintillation counting
Reference GBR 12909 (IC 50 : 3 nM)
Janowsky, A. et al. (1986) J. Neurochem., 46: 1272-1276.
GABA transporter - antagonist radioligand
binding
Ref. 0060
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
❚ norepinephrine
rat cerebral cortex
Ligand
[ 3 H]GABA (10 nM) (+ 10 µM isoguvacine)
(+ 10 µM baclofen)
Kd 4.6 µM
Non specific GABA (1 mM)
Reference nipecotic acid (IC 50 : 4.9 µM)
Shank, R.P. et al. (1990) J. Neurochem., 54: 2007-2015.
DA uptake (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
BTCP
GBR 12909
nomifensine
dopamine
GBR 12909
❚ See other dopamine assays, page 32
specific binding (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
nipecotic acid
GABA
muscimol
baclofen
❚ See other gaba assays, pp. 38, 84, and 97
norepinephrine transporter - antagonist radioligand
binding
Ref. 0355
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]nisoxetine (1 nM)
2.9 nM
desipramine (1 µM)
protriptyline (IC 50 : 5.4 nM)
Pacholczyk, T. et al. (1991) Nature, 350: 350-354.
specific binding (% of control)
100
50
0
-11 - 10 -9 -8 -7 -6 -5
log [drug] (M)
protriptyline
desipramine
imipramine
GBR 12909
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