in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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102 in vitro pharmacology 2011 catalog [Intracellular ligand-gated channels] ❚ Ca 2+ channels IP 3 - agonist radioligand Source rat cerebellum Ligand [ 3 H]D-(1,4,5)IP 3 (0.5 nM) Kd 11 nM Non specific D-(1,4,5)IP 3 (1 µM) binding Ref. 0083 Reference D-(1,4,5)IP 3 (IC 50 : 23 nM) Q 3 weeks Worley, P.F. et al. (1987) J. Biol. Chem., 262: 12132-12136. RY3 (ryanodine) - agonist radioligand Source rat cerebral cortex Ligand [ 3 H]ryanodine (3 nM) Kd 6 nM Non specific ryanodine (10 µM) binding Ref. 0627 Reference ryanodine (IC 50 : 7.7 nM) Q 3 weeks Padua, R. A. et al. (1992) Brain Res., 542: 135-140. specific binding (% of control) 100 50 0 ryanodine ruthenium red heparin -11 -10 -9 -8 -7 -6 -5 -4 -3 log [drug] (M) ❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are available? For some binding assays two models are available using either agonist or antagonist as radioligand. G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore, it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists. The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information about its functional activity at the receptor.
103 Cerep services transporters Receptors ❚ adenosine adenosine transporter - antagonist radioligand Source guinea-pig cerebral cortex binding Ligand [ 3 H]NBTI (0.15 nM) Kd 0.08 nM Ref. 0007 Non specific NBTI (5 µM) Q 3 weeks Reference NBTI (IC 50 : 0.2 nM) Included in: Organ safety profile Verma, A. and Marangos, P.J. (1985) Life Sci., 36: 286-290. specific binding (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) NBTI dipyridamole CPA Ion channels Transporters adenosine uptake cellul ar Ref. 3374 Q 3 weeks Source Hela cells Tracer [ 3 H]2-8 adenosine (0.1 µM) Measured product [ 3 H]2-8 adenosine incorporation into Hela cells Detection method scintillation counting Reference ❚ cannabinoid anandamide uptake cellul ar Ref. 0647 Q 4 weeks ❚ choline NBTI (IC 50 : 1.1 nM) Harley, E.R. et al.(1982) Cancer Res., 42: 1289-1295. Source U-937 cells Tracer [ 3 H]AEA (2 nM) + AEA (98 nM) Measured product [ 3 H]AEA incorporation into U-937 cells Detection method scintillation counting Reference AM 404 (IC 50 : 1 µM) Maccarrone, M. et al. (1998) J. Biol. Chem., 273: 32332-32339. choline transporter (CHT1) - antagonist radioligand binding Ref. 1552 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]hemicholinium-3 (3 nM) 3.9 nM hemicholinium-3 (10 µM) hemicholinium-3 (IC 50 : 14 nM) Apparsundaram, S. et al. (2000) Bioch. Biophys. Res. Com., 276: 862-867. ❚ See other Adenosine assays, page 13 AEA uptake (% of control) 100 50 0 -9 -8 -7 -6 -5 -4 log [drug] (M) AM 404 AEA ❚ See other Cannabinoid assays, page 27 specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 -3 -2 -1 log [drug] (M) hemicholinium-3 choline carbachol 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
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 and 98: transient receptor potential channe
Page 99 and 100: 99 kainate - agonist radioligand bi
Page 101: 101 ❚ purinergic channels Cerep s
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.
Page 149 and 150: 149 ❚ protein-SERINE/THREONINE ki
Page 151 and 152: 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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