in vitro PHARMACOLOGY 2011 CATALOG - Cerep

86 in vitro pharmacology 2011 catalog
❚ gaba
Cl – channel (GABA-gated) - antagonist radioligand
binding
Ref. 0170
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 35 S]TBPS (3 nM)
14.6 nM
picrotoxinin (20 µM)
picrotoxinin (IC 50 : 150 nM)
Lewin, A.H. et al. (1989) Mol. Pharmacol., 35: 189-194.
specific binding (% of control)
100
50
picrotoxinin
muscimol
0
GABA
-9 -8 -7 -6 -5 -4
log [drug] (M)
❚ See other GABA assays pp. 38, 97 and 104
❚ Glutamate
AMPA - agonist radioligand
binding
Ref. 0064
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]AMPA (8 nM)
82 nM
L-glutamate (1 mM)
L-glutamate (IC 50 : 535 nM)
Murphy, D.E. et al. (1987) Neurochem. Res., 12: 775-781.
specific binding (% of control)
100
50
0
-8 -7 -6 -5 -4
log [drug] (M)
L-glutamate
kainic acid
CGS 19755
kainate - agonist radioligand
binding
Ref. 0065
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]kainic acid (5 nM)
19 nM
L-glutamate (1 mM)
kainic acid (IC 50 : 40 nM)
Monaghan, D.T. and Cotman, C.W. (1982) Brain Res., 252: 91-100.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
kainic acid
L-glutamate
CGS 19755
NMDA - antagonist radioligand
binding
Ref. 0066
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]CGP 39653 (5 nM)
23 nM
L-glutamate (100 µM)
CGS 19755 (IC 50 : 550 nM)
Sills, M.A. et al. (1991) Eur. J. Pharmacol., 192: 19-24.
specific binding (% of control)
100
50
CGS 19755
L-glutamate
0
kainic acid
-9 -8 -7 -6 -5 -4
log [drug] (M)
PCP - antagonist radioligand
binding
Ref. 0124
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]TCP (10 nM)
13 nM
MK 801 (10 µM)
MK 801 (IC 50 : 5.3 nM)
Vignon, J. et al. (1986) Brain Res., 378: 133-141.
For further details and updated information on assays:
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