in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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104 in vitro pharmacology 2011 catalog ❚ dopamine dopamine transporter - antagonist radioligand binding Ref. 0052 Q 3 weeks Included in: ExpresS Profile High-throughput profile Diversity profile BioPrint ® profile Organ safety profile dopamine uptake cellul ar Ref. 0394 Q 3 weeks ❚ gaba Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]BTCP (4 nM) 4.5 nM BTCP (10 µM) BTCP (IC 50 : 7.1 nM) specific binding (% of control) 100 50 0 -11 - 10 -9 -8 -7 -6 -5 -4 -3 log [drug] (M) Pristupa, Z.B. et al. (1994) Mol. Pharmacol., 45: 125-135. [Custom offer] rat striatum model (Ref. 0051), please contact us at customresearch@cerep.com Source rat striatum synaptosomes Tracer [ 3 H]DA (0.2 µCi/ml) Measured product [ 3 H]DA incorporation into synaptosomes Detection method scintillation counting Reference GBR 12909 (IC 50 : 3 nM) Janowsky, A. et al. (1986) J. Neurochem., 46: 1272-1276. GABA transporter - antagonist radioligand binding Ref. 0060 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source ❚ norepinephrine rat cerebral cortex Ligand [ 3 H]GABA (10 nM) (+ 10 µM isoguvacine) (+ 10 µM baclofen) Kd 4.6 µM Non specific GABA (1 mM) Reference nipecotic acid (IC 50 : 4.9 µM) Shank, R.P. et al. (1990) J. Neurochem., 54: 2007-2015. DA uptake (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 log [drug] (M) BTCP GBR 12909 nomifensine dopamine GBR 12909 ❚ See other dopamine assays, page 32 specific binding (% of control) 100 50 0 -9 -8 -7 -6 -5 -4 log [drug] (M) nipecotic acid GABA muscimol baclofen ❚ See other gaba assays, pp. 38, 84, and 97 norepinephrine transporter - antagonist radioligand binding Ref. 0355 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) [ 3 H]nisoxetine (1 nM) 2.9 nM desipramine (1 µM) protriptyline (IC 50 : 5.4 nM) Pacholczyk, T. et al. (1991) Nature, 350: 350-354. specific binding (% of control) 100 50 0 -11 - 10 -9 -8 -7 -6 -5 log [drug] (M) protriptyline desipramine imipramine GBR 12909 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
105 norepinephrine ❚ norepinephrine uptake Source rat hypothalamus synaptosomes Tracer [ 3 H]NE (0.2 µCi/ml) Measured product [ 3 H]NE incorporation into synaptosomes Detection method scintillation counting NE uptake (% of control) 100 50 Cerep services cellul ar Ref. 0393 Q 3 weeks Reference protriptyline (IC 50 : 1.5 nM) Perovic, S. and Muller, W.E.G. (1995) Arzneim-Forsch. Drug Res., 45: 1145-1148. 0 -11 -10 -9 -8 -7 -6 log [drug] (M) protryptiline Receptors ❚ serotonin Ion channels 5-HT transporter - antagonist radioligand binding Ref. 0439 Q 3 weeks Included in: ExpresS Profile High-throughput profile Diversity profile BioPrint ® profile Organ safety profile 5-HT uptake cellul ar Ref. 0392 Q 3 weeks Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]imipramine (2 nM) 1.7 nM imipramine (10 µM) imipramine (IC 50 : 2.1 nM) specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) Tatsumi, M. et al. (1999) Eur. J. Pharmacol., 368: 277-283. [Custom offer] rat brain model (Ref. 0145), please contact us at [CUSTOM OFFER] Source rat brain synaptosomes Tracer [ 3 H]5-HT (0.2 µCi/ml) Measured product [ 3 H]5-HT incorporation into synaptosomes Detection method scintillation counting imipramine serotonin zimelidine citalopram Reference imipramine (IC 50 : 30 nM) Perovic, S. and Muller, W.E.G. (1995) Arzneim-Forsch. Drug Res., 45: 1145-1148. ❚ See other serotonin assays, pp. 68, 90, and 101 Transporters Kinases Epigenetic & DNA-related enzymes Other enzymes Specialized cellular assays Standard profiles Testing conditions 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
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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
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melanin concentrating hormone ❚
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49 ❚ melatonin Cerep services MT
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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 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: 103 Cerep services transporters Rec
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.
Page 149 and 150: 149 ❚ protein-SERINE/THREONINE ki
Page 151 and 152: 151 RAF-1/MEK1 Ref. 1703 Q 3 weeks
Page 153 and 154: 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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in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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