in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
You also want an ePaper? Increase the reach of your titles
YUMPU automatically turns print PDFs into web optimized ePapers that Google loves.
62 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ orex<strong>in</strong><br />
OX 2 - agonist radioligand<br />
Source<br />
human recomb<strong>in</strong>ant (HEK-293 cells)<br />
Ligand<br />
[ 125 I]orex<strong>in</strong>-A (0.04 nM)<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Kd<br />
0.2 nM<br />
Ref. 1988<br />
Non specific orex<strong>in</strong>-B (1 µM)<br />
Q 3 weeks<br />
Reference orex<strong>in</strong>-B (IC 50 : 0.21 nM)<br />
Included <strong>in</strong>:<br />
Organ safety profile<br />
Wieland, H.A. et al. (2002) Eur. J. Biochem., 269: 1128-1135.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
OX 2<br />
cellul ar<br />
Ref. 2349<br />
Ref. 2350<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 orex<strong>in</strong>-B (1 µM)<br />
Reference orex<strong>in</strong>-B (EC 50 : 3.7 nM)<br />
Antagonist effect Stimulant orex<strong>in</strong>-B (10 nM)<br />
Reference unavailable<br />
Ammoun, S. et al. (2003) J. Pharmacol. Exp. Ther., 305: 507-514.<br />
Ca 2+ mobilization (% of control)<br />
100<br />
antagonist effect:<br />
50<br />
no graph available<br />
0<br />
-9 -8 -7 -6 <br />
-11 -10 <br />
log [agonist] (M)<br />
orex<strong>in</strong>-B <br />
orex<strong>in</strong>-A<br />
[Ala 11 ,D-Leu 15 ]-orex<strong>in</strong>-B<br />
<br />
[Solvent] must be kept ≤ 0.3%<br />
❚ orphans (class a)<br />
GPR119<br />
cellul ar<br />
Ref. 3297<br />
Ref. 3299<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
HIT-T15 cells (endogenous)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control AR231453 (10 µM)<br />
Reference AR231453 (EC 50 : 71 nM)<br />
Antagonist effect Stimulant AR231453 (300 nM)<br />
Reference unavailable<br />
Chu, Z.L et al.(2008) Endocr<strong>in</strong>ology, 149: 2038-2047.<br />
-12 -11<br />
-12 -11<br />
<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
<br />
<br />
-12 -11<br />
-10 -9 -8 -7<br />
-10 -9 -8 -7<br />
-10 -9 -8 -7 -6 -5<br />
-9 -8 -7 -6 -5<br />
-10 -4<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
-11 -10<br />
-9 -8 -7 -6 -5 -4<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3<br />
<br />
<br />
<br />
<br />
❚ parathyroid hormone<br />
PTH1<br />
cellul ar<br />
Ref. 2660<br />
Ref. 2661<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
SaOS2 cells (endogenous)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control PTHrP (1-34) (1 µM)<br />
Reference PTHrP (1-34) (EC 50 : 1.7 nM)<br />
Antagonist effect Stimulant PTHrP (1-34) (10 nM)<br />
Reference PTHrP (7-34) (IC 50 : 84 nM)<br />
Orloff, J.J. et al. (1992) Endocr<strong>in</strong>ol., 131: 1603-1611.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
[Solvent] must be kept 0.3%<br />
❚ platelet activat<strong>in</strong>g factor<br />
PAF - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0915<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
BioPr<strong>in</strong>t ® profile<br />
Organ safety profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
[ 3 H]C 16 -PAF (1.5 nM)<br />
1.5 nM<br />
WEB 2086 (10 µM)<br />
C 16 -PAF (IC 50 : 2.4 nM)<br />
Fukunaga, K. et al. (2001) J.Biol.Chem., 276: 43025-43030.<br />
<br />
<br />
<br />
<br />
<br />
<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
<br />
100<br />
<br />
<br />
50<br />
0<br />
C 16-PAF<br />
WEB 2086<br />
-12 -11 -10 -9 -8 -7 -6 -5<br />
log [drug] (M)