in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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70 in vitro pharmacology 2011 catalog ❚ serotonin 5-HT 2A - agonist radioligand binding Ref. 0471 Q 3 weeks Included in: BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (HEK-293 cells) [ 125 I](±)DOI (0.1 nM) 0.3 nM (±)DOI (1 µM) (±)DOI (IC 50 : 0.27 nM) Bryant, H.U. et al. (1996) Life Sci., 15: 1259-1268. specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 log [drug] (M) (+)DOI - serotonin mesulergine ketanserin 5-HT 2A cellul ar Ref. 3196 Ref. 3198 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source human recombinant (HEK-293 cells) Measured product IP 1 Detection method HTRF Agonist effect Control serotonin (10 µM) Reference serotonin (EC 50 : 27 nM) Antagonist effect Stimulant serotonin (100 nM) Reference ketanserin (IC 50 : 24.2 nM) Porter, R.H.P. et al.(1999) Brit. J. Pharmacol., 128: 13-20. Ca 2+ mobilization (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [agonist] (M) serotonin (±)DOI 5-methoxytryptamine BW 723C86 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [antagonist] (M) ketanserin mesulergine SB 206553 SB 204741 5-HT 2A tissue Ref. 0334 Q 4 weeks Source rabbit aorta (endothelium-denuded) Agonist serotonin (pD 2 = 6.5) Antagonist ketanserin (pA 2 = 8.7) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Rinaldi-Carmona, M. et al. (1992) J. Pharmacol. Exp. Ther., 262: 759-768. tension (% of max.) -12 -11 100 50 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 0 -8 -7 -6 -5 -4 -3 log [agonist] (M) ketanserin none 3 nM 10 nM 30 nM 5-HT 2B - antagonist radioligand Source human recombinant (CHO cells) Ligand [ 3 H]mesulergine (2 nM) Kd 2.4 nM Non specific mesulergine (10 µM) binding Reference mesulergine (IC 50 : 2.35 nM) Ref. 1609 Q 3 weeks Kursar, J.D. et al. (1994) Mol. Pharmacol., 46: 227-234. specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) mesulergine SB 206553 SB 204741 ketanserin selected cerep assays ❚ binding assays -10 -9 -8 -7 -6 -5 -4 -3 -11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 Binding assays are developed according to the competition assay principle. There are three assay formats -13 -12 used: -11 -10filtration, -9 -8 -7 -6scintillation -5 -10 -9 -8 -7 -6 proximity assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified). Large batches of cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are -10 -9 -8 -7 -6 -5 -4 quality controlled before use. -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 ❚ cellular Functional GPCR assays -12 -11 -10 -9 -8 -7 -6 -5 Functional GPCR assays are cell-based assays to measure agonist-like, inverse agonist, antagonist and modulator -11 -10 -9 activity -8 -7 -6of -5compounds. -4 Various technologies are used: TR-FRET to determine cAMP concentration and IP1 levels, real time fluorescence to monitor calcium flux, cellular dielectric spectroscopy to measure impedance modulation. Large batches of cells, from which whole cells are frozen and stored for functional assays, are produced in-house. Cells are quality controlled before use. A novel patented host cell line was designed and constructed for Gi protein coupled receptors. ❚ tissue bioassays Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory, gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the contractile activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in the tissue used.
71 serotonin ❚ 5-HT 2B - agonist radioligand binding Ref. 1333 Q 3 weeks Included in: ExpresS Profile High-throughput profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I](±)DOI (0.2 nM) 0.2 nM (±)DOI (1 µM) (±)DOI (IC 50 : 5 nM) Choi, D.S. et al. (1994) FEBS Lett., 352: 393-399. specific binding (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 log [drug] (M) (±)DOI serotonin 5-methoxytryptamine BW 723C86 Cerep services Receptors [GPCRs] 5-HT 2B cellul ar Ref. 3344 Ref. 3345 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source human recombinant (CHO cells) Measured product IP 1 Detection method HTRF Agonist effect Control serotonin (1 µM) Reference serotonin (EC 50 : 10.1 nM) Antagonist effect Stimulant serotonin (30 nM) Reference SB 206553 (IC 50 : 28.4 nM) Porter, R.H.P. et al. (1999) Brit. J. Pharmacol., 128: 13-20. -10 -9 -8 -7 -6 -5 -4 -3 -11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 -5 -6 -10 -9 -8 -7 -5 -4 -10 -9 -8 -7 -6 -6 -5 -4 -12 -11 -10 -9 -8 -7 -3 -11 -10 -9 -8 -7 -6 -5 -12 Ion channels Transporters -11 -10 -9 -8 -7 -6 -5 -4 5-HT 2B tissue Ref. 0333 Q 4 weeks Source rat stomach fundus Agonist 5-CT (pD 2 = 7.5) Antagonist methiothepin (pA 2 = 8.4) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Baxter, G.S. et al. (1994) Brit. J. Pharmacol., 112: 323-331. tension (% of max.) 100 50 methiothepin none 0.1 µM 0 1 µM 10 µM -9 -8 -7 -6 -5 -4 log [agonist] (M) Kinases Epigenetic & DNA-related enzymes 5-HT 2C - antagonist radioligand Source human recombinant (HEK-293 cells) Ligand [ 3 H]mesulergine (1 nM) binding Kd 0.5 nM Ref. 0137 Non specific RS 102221 (10 µM) Q 3 weeks Reference RS 102221 (IC 50 : 3.1 nM) Included in: High-throughput profile Stam, N.J. et al. (1994) Eur. J. Pharmacol., 269: 339-348. specific binding (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 log [drug] (M) RS 102221 Ro 600175 serotonin ketanserin Other enzymes Specialized cellular assays 5-HT 2C - agonist radioligand binding Ref. 1003 Q 3 weeks Included in: BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (HEK-293 cells) [ 125 I](±)DOI (0.1 nM) 0.9 nM (±)DOI (10 µM) (±)DOI (IC 50 : 0.38 nM) Bryant, H.U. et al. (1996) Life Sci., 15: 1259-1268. specific binding (% of control) 100 -10 -9 -8 -7 -6 -5 -4 -3 -11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 50 -13 -12 -11 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -10 (±)DOI serotonin RS 102221 -10 -9 -8 -7 -6 -5 -4 0 Ro 600175 -11 - 10 -9 -8 -7 -6 -11 -10 -8 -6 -5 -12 -9 -7 -4 -3 log [drug] (M) -10 -9 -8 -7 -12 -11 -6 -5 -11 -10 -7 -6 -5 -4 -9 -8 Standard profiles Testing conditions 5-HT 2C cellul ar Ref. 3197 Ref. 3199 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source human recombinant (HEK-293 cells) Measured product IP 1 Detection method HTRF Agonist effect Control serotonin (1 µM) Reference serotonin (EC 50 : 1.81 nM) Antagonist effect Stimulant serotonin (30 nM) Reference SB 206553 (IC 50 : 20.2 nM) Porter, R.H.P. et al. (1999) Brit. J. Pharmacol., 128: 13-20. ❚ For 5-HT 3 assays, see "OTHER RECEPTORS", page 90 Ordering information Assay list & index
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in vitro pharmacology 2011 catalog
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Cerep services p. 4 Receptors [GPC
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5 ❚ tool-box for cell-based assay
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7 ❚ profile design Cerep offers a
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9 ❚ data online A powerful web-ba
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11 in vitro pharmacology assays Rec
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13 Cerep services receptors Recept
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15 Adenosine ❚ A 2B - antagonist
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17 alpha 1B - antagonist radioligan
Page 19 and 20: 19 adrenergic ❚ alpha 2C - antago
Page 21 and 22: adrenergic ❚ 21 beta 3 cellul ar
Page 23 and 24: -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 bo
Page 25 and 26: adykinin ❚ 25 B 2 cellul ar Ref.
Page 27 and 28: 27 ❚ cannabinoid CB 1 - agonist r
Page 29 and 30: 29 chemokines ❚ CCR2 cellul ar Re
Page 31 and 32: 31 cholecystokinin ❚ CCK 2 (CCK B
Page 33 and 34: 33 dopamine ❚ D 2S - antagonist r
Page 35 and 36: dopamine ❚ 35 D 5 cellul ar Ref.
Page 37 and 38: 37 Cerep services ❚ Free fatty ac
Page 39 and 40: 39 galanin ❚ GAL 2 - agonist radi
Page 41 and 42: 41 ❚ Growth hormone-releasing hor
Page 43 and 44: 43 H 3 - agonist radioligand Source
Page 45 and 46: 45 leukotrienes ❚ CysLT 2 (LTC 4
Page 47 and 48: melanin concentrating hormone ❚
Page 49 and 50: 49 ❚ melatonin Cerep services MT
Page 51 and 52: 51 M 2 - antagonist radioligand bin
Page 53 and 54: 53 muscarinic ❚ M 5 - antagonist
Page 55 and 56: 55 NK 3 - agonist radioligand bindi
Page 57 and 58: neuropeptide y ❚ 57 Y 1 cellul a
Page 59 and 60: 59 Cerep services ❚ opioid and op
Page 61 and 62: 61 NOP (ORL1) - agonist radioligand
Page 63 and 64: 63 platelet activating factor ❚ P
Page 65 and 66: 65 prostanoid ❚ EP 4 - agonist ra
Page 67 and 68: 67 proteinase-activated ❚ PAR2 ce
Page 69: serotonin ❚ 69 5-HT 1A cellul ar
Page 73 and 74: 73 5-HT 7 - agonist radioligand bin
Page 75 and 76: 75 ❚ thyrotropin releasing hormon
Page 77 and 78: 77 ❚ vasopressin Cerep services O
Page 79 and 80: 79 Cerep services receptors Recept
Page 81 and 82: 81 LXRb - agonist radioligand bindi
Page 83 and 84: 83 Cerep services receptors Recept
Page 85 and 86: 85 gaba ❚ GABA A1 (a1, b2, g2) -
Page 87 and 88: 87 glycine (strychnine-insensitive)
Page 89 and 90: 89 ❚ Melatonin MT 3 (ML 2 ) - ago
Page 91 and 92: 91 ❚ Sigma Cerep services sigma (
Page 93 and 94: 93 Cerep services [Voltage-gated ch
Page 95 and 96: voltage-gated channels [K + channel
Page 97 and 98: transient receptor potential channe
Page 99 and 100: 99 kainate - agonist radioligand bi
Page 101 and 102: 101 ❚ purinergic channels Cerep s
Page 103 and 104: 103 Cerep services transporters Rec
Page 105 and 106: 105 norepinephrine ❚ norepinephri
Page 107 and 108: 107 Cerep services Kinases Receptor
Page 109 and 110: 109 DDR2 kinase Ref. 2783 Q 3 weeks
Page 111 and 112: 111 protein-tyrosine kinases [Rtk]
Page 113 and 114: 113 FLT-3 kinase Ref. 2866 Q 3 week
Page 115 and 116: 115 KDR kinase (VEGFR2) Ref. 2864 Q
Page 117 and 118: 117 TRKB Ref. 2902 Q 3 weeks Includ
Page 119 and 120: 119 protein-tyrosine kinases [Ctk]
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121 JAK1 Ref. 2619 Q 3 weeks Includ
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123 TXK Ref. 2786 Q 3 weeks Include
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125 CDK6 (cycD3) Ref. 2909 Q 3 week
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protein-SERINE/THREONINE kinases [C
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129 JNK3 Ref. 2916 Q 3 weeks Includ
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131 CaMK1d Ref. 2922 Q 3 weeks Incl
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133 MAPKAPK2 Ref. 3367 Q 3 weeks I
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135 PhKg1 Ref. 2745 Q 3 weeks Inclu
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137 ❚ protein-SERINE/THREONINE ki
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139 MSK1 Ref. 1724 Q 3 weeks Source
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141 PKCe Ref. 2044 Q 3 weeks PKCz R
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143 ROCK2 Ref. 2884 Q 3 weeks Inclu
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145 COT kinase (MAP3K8) Ref. 2003 Q
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147 MKK6/p38a (mutant active) Ref.
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149 ❚ protein-SERINE/THREONINE ki
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151 RAF-1/MEK1 Ref. 1703 Q 3 weeks
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153 other kinases ❚ MYT1 kinase R
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155 other kinases ❚ TBK1 Ref. 33
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157 Cerep services Epigenetic & DNA
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159 HDACs ❚ HDAC3 Ref. 2083 Q 3 w
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161 HDACs ❚ sirtuin 3 Source Subs
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163 Cerep services Other enzymes Re
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165 phosphatases ❚ phosphatase LA
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167 phosphatase SHP2 (PTPN11) Sourc
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169 caspase-3 ❚ Cysteine protease
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171 proteases [aspartic proteases]
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173 proteases [metalloproteases]
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phosphodiesterases ❚ 175 PDE4A 1
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177 no synthases ❚ inducible NOS
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179 ❚ Monoamine & neurotransmitte
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181 Cerep services ❚ Transduction
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183 miscellaneous enzymes ❚ carbo
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185 Specialized cellular assays The
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187 ion transport systems ❚ Na +
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189 cytokine secretion ❚ IL-2 sec
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191 expression of endothelial adhes
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193 PDGF-stimulated Balb/c 3T3 prol
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195 cerep Standard profiles ExpresS
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197 ❚ Cellular functional GPCR pr
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Cerep standard profiles ❚ 199 Dr
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Cerep standard profiles ❚ 201 Sa
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203 testing conditions Binding, enz
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205 The reference compound for each
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207 ordering information Quotation
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209 REQUESTED COMPOUND INFORMATION
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shipment instructions ❚ 211 For
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213 assay list & index
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215 CDK5/p35 124 CDK6 (cycD3) 125 C
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217 MMP-3 172 MMP-7 172 MMP-8 172 M
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contacts ❚ france [Laboratories]
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