in vitro PHARMACOLOGY 2011 CATALOG - Cerep

179
❚ Monoamine & neurotransmitter synthesis
& metabolism
Cerep
services
Receptors
acetylcholinesterase
Ref. 0363
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
human recombinant (HEK-293 cells)
Substrate
AMTCh (50 µM)
Measured product thio-conjugate
Detection method photometry
Reference
neostigmine (IC 50 : 35 nM)
[Solvent] must be kept ≤ 0.1%
Ellman, G.L. et al. (1961) Biochem. Pharmacol., 7: 88-95.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
neostigmine
physostigmine
tacrine
darepezil
Ion
channels
Transporters
COMT (catechol-O-methyl transferase)
Ref. 0457
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
porcine liver
esculetin (1 µM)
scopoletin
fluorimetry
Ro 41-0960 (IC 50 : 30 nM)
Muller-Enoch, D. et al. (1976) Z. Naturforsch., 31: 280-284.
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
Kinases
Epigenetic &
DNA-related
enzymes
GABA transaminase
Ref. 0461
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
Source
rat brain
Substrate
GABA (9 mM) + α-ketoglutarate (9 mM)
Measured product succinic semialdehyde
Detection method fluorimetry
Reference
AoAA (IC 50 : 200 nM)
Lösher, W. (1981) J. Neurochem., 36: 1521-1527.
enzyme activity (% of control)
100
50
AoAA
γ-acetylenic
0
GABA
-9 -8 -7 -6 -5 -4 -3
log [drug] (M)
Other
enzymes
Specialized
cellular
assays
HNMT (histamine N-methyl transferase)
Source
rat kidney
Substrate
[ 14 C]S-adenosyl-L-methionin (4 µM)
+ histamine (300 µM)
Ref. 0463
Measured product [ 14 C]histamine
Q 6 weeks
Detection method scintillation counting
Included in:
Reference
SKF-91488 (IC 50 : 34 µM)
Organ safety profile
De Santi C. et al. (1998) Xenobiotica, 28: 571-577.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
SKF-91488
0
-7 -6 -5 -4 -3
log [drug] (M)
Standard
profiles
Testing
conditions
MAO-A
Ref. 0191
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human placenta
Substrate
kynuramine (0.15 mM)
Measured product 4-OHquinoline
Detection method photometry
Reference
clorgyline (IC 50 : 37 nM)
Weyler, W. and Salach, J.I. (1985) J. Biol. Chem., 260: 13199-13207.
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
Ordering
information
Assay list
& index