in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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98 in vitro pharmacology 2011 catalog ❚ membrane ligand-gated channels [gaba] GABA A (conventional patch-clamp) cellul ar Ref. 2859 Ref. 3395 Ref. 3396 Q 2 weeks Agonist effect Antagonist effect Potentiator effect Source GABA A (α1β2γ2) CHO-K1 cell line Test concentration 1 µM Detection method conventional whole-cell patch-clamp Agonist effect Reference muscimol (EC 50 : 1.7 μM) Antagonist effect Reference bicuculline (IC 50 : 700 nM) Potentiator effect Reference diazepam (EC 50 : 29 nM) Sieghart, W. (1995) Pharmacol. Rev. 47(2):181-234. GABA A tissue Source guinea-pig ileum Agonist 3-APSA (pD 2 = 4.7) Antagonist bicuculline (pA 2 = 5.7) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities tension (% of max.) 100 50 0 bicuculline none 3 µM 10 µM 30 µM Ref. 0314 Q 4 weeks [Solvent] must be kept ≤ 0.1% Giotti, A. et al. (1983) Brit. J. Pharmacol., 78: 469-478. -6 -5 -4 -3 log [agonist] (M) BZD (central) - agonist radioligand binding Ref. 0028 Q 3 weeks Included in: ExpresS Profile High-throughput profile Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 3 H]flunitrazepam (0.4 nM) 2.1 nM diazepam (3 µM) diazepam (IC 50 : 8.6 nM) Speth, R.C. et al. (1979) Life Sci., 24: 351-358. Cl – channel (GABA-gated) - antagonist radioligand binding Ref. 0170 Q 3 weeks Included in: ExpresS Profile High-throughput profile Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 35 S]TBPS (3 nM) 14.6 nM picrotoxinin (20 µM) picrotoxinin (IC 50 : 150 nM) Lewin, A.H. et al. (1989) Mol. Pharmacol., 35: 189-194. specific binding (% of control) 100 50 picrotoxinin muscimol 0 GABA -9 -8 -7 -6 -5 -4 log [drug] (M) ❚ See other GABA assays, pp. 38, 84 and 104 ❚ glutamate channels AMPA - agonist radioligand binding Ref. 0064 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 3 H]AMPA (8 nM) 82 nM L-glutamate (1 mM) L-glutamate (IC 50 : 535 nM) Murphy, D.E. et al. (1987) Neurochem. Res., 12: 775-781. specific binding (% of control) 100 50 0 -8 -7 -6 -5 -4 log [drug] (M) L-glutamate kainic acid CGS 19755
99 kainate - agonist radioligand binding Ref. 0065 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 3 H]kainic acid (5 nM) 19 nM L-glutamate (1 mM) kainic acid (IC 50 : 40 nM) Monaghan, D.T. and Cotman, C.W. (1982) Brain Res., 252: 91-100. membrane ligand-gated channels [glutamate] ❚ specific binding (% of control) 100 50 0 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) kainic acid L-glutamate CGS 19755 Cerep services Receptors NMDA - antagonist radioligand binding Ref. 0066 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 3 H]CGP 39653 (5 nM) 23 nM L-glutamate (100 µM) CGS 19755 (IC 50 : 550 nM) Sills, M.A. et al. (1991) Eur. J. Pharmacol., 192: 19-24. specific binding (% of control) 100 50 CGS 19755 L-glutamate 0 kainic acid -9 -8 -7 -6 -5 -4 log [drug] (M) Ion channels Transporters PCP - antagonist radioligand binding Ref. 0124 Q 3 weeks Included in: High-throughput profile Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 3 H]TCP (10 nM) 13 nM MK 801 (10 µM) MK 801 (IC 50 : 5.3 nM) Vignon, J. et al. (1986) Brain Res., 378: 133-141. Kinases Epigenetic & DNA-related enzymes glycine (strychnine-insensitive) - antagonist radioligand binding Ref. 0068 Q 3 weeks Included in: BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 3 H]MDL 105,519 (0.5 nM) 5 nM glycine (1 mM) glycine (IC 50 : 160 nM) Baron, B.M. et al. (1996) J. Pharmacol. Exp. Ther., 279: 62-68. specific binding (% of control) 100 50 0 -9 -8 -7 -6 -5 -4 log [drug] (M) glycine 7-Cl-kinurenate strychnine Other enzymes Specialized cellular assays ❚ glycine channels Standard profiles strychnine-sensitive - antagonist radioligand Source rat spinal cord Ligand [ 3 H]strychnine (2 nM) Kd 20 nM Non specific strychnine (100 µM) binding Ref. 0067 Reference strychnine (IC 50 : 6.6 nM) Q 3 weeks Marvizon, J.C. et al. (1986) Mol. Pharmacol., 30: 590-597 specific binding (% of control) 100 50 0 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) strychnine glycine 7-Cl-kinurenate Testing conditions Ordering information For further details and updated information on assays: ❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com ❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568 Assay developed in 2010 New assay conditions Human Q Standard turnaround time 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
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19 adrenergic ❚ alpha 2C - antago
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adrenergic ❚ 21 beta 3 cellul ar
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-12 -11 -10 -9 -8 -7 -6 -5 -4 -3 bo
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adykinin ❚ 25 B 2 cellul ar Ref.
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27 ❚ cannabinoid CB 1 - agonist r
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29 chemokines ❚ CCR2 cellul ar Re
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31 cholecystokinin ❚ CCK 2 (CCK B
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33 dopamine ❚ D 2S - antagonist r
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dopamine ❚ 35 D 5 cellul ar Ref.
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37 Cerep services ❚ Free fatty ac
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39 galanin ❚ GAL 2 - agonist radi
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41 ❚ Growth hormone-releasing hor
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43 H 3 - agonist radioligand Source
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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 and 70: serotonin ❚ 69 5-HT 1A cellul ar
Page 71 and 72: 71 serotonin ❚ 5-HT 2B - agonist
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: transient receptor potential channe
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]
Page 121 and 122: 121 JAK1 Ref. 2619 Q 3 weeks Includ
Page 123 and 124: 123 TXK Ref. 2786 Q 3 weeks Include
Page 125 and 126: 125 CDK6 (cycD3) Ref. 2909 Q 3 week
Page 127 and 128: protein-SERINE/THREONINE kinases [C
Page 129 and 130: 129 JNK3 Ref. 2916 Q 3 weeks Includ
Page 131 and 132: 131 CaMK1d Ref. 2922 Q 3 weeks Incl
Page 133 and 134: 133 MAPKAPK2 Ref. 3367 Q 3 weeks I
Page 135 and 136: 135 PhKg1 Ref. 2745 Q 3 weeks Inclu
Page 137 and 138: 137 ❚ protein-SERINE/THREONINE ki
Page 139 and 140: 139 MSK1 Ref. 1724 Q 3 weeks Source
Page 141 and 142: 141 PKCe Ref. 2044 Q 3 weeks PKCz R
Page 143 and 144: 143 ROCK2 Ref. 2884 Q 3 weeks Inclu
Page 145 and 146: 145 COT kinase (MAP3K8) Ref. 2003 Q
Page 147 and 148: 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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