in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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56 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ neuromed<strong>in</strong> U<br />
NMU2 - agonist radioligand<br />
Source<br />
human recomb<strong>in</strong>ant (HEK-293 cells)<br />
Ligand<br />
[ 125 I]NMU-8 (porc<strong>in</strong>e) (0.05 nM)<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Kd<br />
0.057 nM<br />
Ref. 0991<br />
Non specific NMU-8 (porc<strong>in</strong>e) (100 nM)<br />
Q 3 weeks<br />
Reference NMU-8 (porc<strong>in</strong>e) (IC 50 : 0.22 nM)<br />
Included <strong>in</strong>:<br />
Organ safety profile<br />
Funes, S. et al. (2002) Peptides, 23: 1607-1615.<br />
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❚ neuropeptide s<br />
NPS<br />
cellul ar<br />
Ref. 3291<br />
Ref. 3292<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
human recomb<strong>in</strong>ant (HEK-293 cells)<br />
Measured product <strong>in</strong>tracellular [Ca 2+ ]<br />
Detection method fluorimetry<br />
Agonist effect Control NPS (1 µM)<br />
Reference NPS (EC 50 : 3.7 nM)<br />
Antagonist effect Stimulant NPS (300 nM)<br />
Reference unavailable<br />
Xu, Y.L., et al. (2004) Neuron., 43: 487-497.<br />
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[Solvent] must be kept 0.1%<br />
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❚ neuropeptide w / neuropeptide B<br />
NPBW1<br />
cellul ar<br />
Ref. 2845<br />
Ref. 2851<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control NPB29 (100 nM)<br />
Reference NPB29 (EC 50 : 0.08 nM)<br />
Antagonist effect Stimulant NPB29 (1 nM)<br />
Reference unavailable<br />
Shimomura, Y., (2002) J. Biol. Chem., 277: 35826-35832.<br />
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❚ neuropeptide y<br />
Y (non-selective) - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0105<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Diversity profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
rat cerebral cortex<br />
[ 125 I]peptide YY (0.05 nM)<br />
0.1 nM<br />
NPY (1 µM)<br />
NPY (IC 50 : 0.46 nM)<br />
Goldste<strong>in</strong>, M. et al. (1986) Progr. Bra<strong>in</strong> Res., 68: 331-335.<br />
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Y 1 - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0106<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Profile<br />
High-throughput profile<br />
BioPr<strong>in</strong>t ® profile<br />
Organ safety profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
SK-N-MC cells (endogenous)<br />
[ 125 I]peptide YY (0.025 nM)<br />
0.06 nM<br />
NPY (1 µM)<br />
NPY (IC 50 : 0.079 nM)<br />
Wieland, H. A. et al. (1995) J. Pharmacol. Exp. Ther., 275: 143-149.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
0<br />
-12 -11 -10 -9 -8 -7 -6 -5<br />
log [drug] (M)<br />
NPY<br />
[Leu 31 , Pro 34 ]-NPY<br />
BIBP 3226
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