in vitro PHARMACOLOGY 2011 CATALOG - Cerep

54 in vitro pharmacology 2011 catalog
❚ neurokinin
NK 1
tissue
Ref. 0321
Q 4 weeks
Source
rabbit pulmonary artery
(precontracted with 0.1 µM norepinephrine)
Agonist [Sar 9 ,Met(O 2 ) 11 ]-SP (pD 2 = 9.8)
Antagonist spantide II
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Emonds-Alt, X. et al. (1993) Eur. J. Pharmacol., 250: 403-413.
tension (% of control)
100
50
0
-12 -11 -10 -9
log [agonist] (M)
NK 1
tissue gpcr
Ref. 0624
Q 4 weeks
Source
guinea-pig ileum
Agonist [Sar 9 ,Met(O 2 ) 11 ]-SP (pD 2 = 8.5)
Antagonist spantide II
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Emonds-Alt, X. et al. (1993) Eur. J. Pharmacol., 250: 403-413.
tension (% of max.)
100
50
0
-11 -10 -9 -8 -7 -6
log [agonist] (M)
NK 2 - agonist radioligand
binding
Ref. 0102
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)
[ 125 I]NKA (0.1 nM)
0.12 nM
[Nleu 10 ]-NKA (4-10) (300 nM)
[Nleu 10 ]-NKA (4-10) (IC 50 : 2.7 nM)
Aharony, D. et al. (1993) Mol. Pharmacol, 44: 356-363.
NK 2
cellul ar
Ref. 1251
Ref. 1765
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control [Nleu 10 ]-NKA (4-10) (1 µM)
Reference [Nleu 10 ]-NKA(4-10)(EC 50 : 1.5 nM)
Antagonist effect Stimulant [Nleu 10 ]-NKA (4-10) (10 nM)
Reference GR 159897 (IC 50 : 15.7 nM)
Subramamian, N. et al. (1994) Biochem. Biophys. Res. Commun., 200: 1512-1520.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
[Nleu 10 ]-NKA (4-10)
NKB
[Sar 9 ,Met(O 2 ) 11 ]-SP
senktide
100
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
GR 159897
SR 48968
SB 222200
spantide II
NK 2
tissue
Ref. 0322
Q 4 weeks
Source
rabbit pulmonary artery
(endothelium-denuded)
Agonist [bAla 8 ]-NKA (4-10) (pD 2 = 8.2)
Antagonist SR 48968 (pA 2 = 10.3)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Emonds-Alt, X. et al. (1993) Regul. Peptides, 46: 31-36.
tension (% of max.)
-12 -11
-12 -11
-11 -10 -9 -8 -7 -6 -5 -4
100-12 -11 -10 -9 -8 -7
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-10 -9 -8 -7 -6
log [agonist] (M)
SR 48968
none
0.1 nM
0.3 nM
1 nM
NK 3 - antagonist radioligand
binding
Ref. 0104
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]SR 142801 (0.4 nM)
0.47 nM
SB 222200 (10 µM)
SB 222200 (IC 50 : 8.8 nM)
Sarau, H.M. et al. (1997) J. Pharmacol. Exp. Ther., 281: 1303-1311.
specific binding (% of control)
100
50
0
SB 222200
senktide
[Sar 9 ,Met (O 2
) 11 ]-SP
SR 48968
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4