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Biological Activity for (2R,4R)-APDC
(2R,4R)-APDC is a highly selective and relatively potent group II metabotropic glutamate receptor agonist. EC50 values are 0.4, 0.4, > 100, > 100, > 300 and > 300 μM for human mGlu2, mGlu3, mGlu1, mGlu5, mGlu4 and mGlu7 receptors respectively. Centrally active following systemic administration in vivo.
Sold with the permission of Eli Lilly and Company
Technical Data for (2R,4R)-APDC
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for (2R,4R)-APDC
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for (2R,4R)-APDC
The following data is based on the product molecular weight 174.16. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||5.74 mL||28.71 mL||57.42 mL|
|5 mM||1.15 mL||5.74 mL||11.48 mL|
|10 mM||0.57 mL||2.87 mL||5.74 mL|
|50 mM||0.11 mL||0.57 mL||1.15 mL|
References for (2R,4R)-APDC
References are publications that support the biological activity of the product.
Monn et al (1996) Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: identification of a potent, highly selective, and systemically active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase. J.Med.Chem. 39 2990 PMID: 8709133
Schoepp et al (1995) Selective inhibition of forskolin-stimulated cyclic AMP formation in rat hippocampus by a novel mGluR agonist, 2R,4R-4-aminopyrrolidine-2,4-dicarboxylate. Neuropharmacology 34 843 PMID: 8532165
Schoepp et al (1999) Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology 38 1431 PMID: 10530808
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Keywords: (2R,4R)-APDC, (2R,4R)-APDC supplier, selective, group, II, agonists, Group, Receptors, mGlu2, mGlu3, mGluR2, mGluR3, Glutamate, Metabotropic, (Metabotropic), 1208, Tocris Bioscience
8 Citations for (2R,4R)-APDC
Citations are publications that use Tocris products. Selected citations for (2R,4R)-APDC include:
Lee and Sherman (2012) Intrinsic modulators of auditory thalamocortical transmission. Hear Res 287 43 PMID: 22726616
Proudfoot et al (2006) Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain. Curr Biol 16 1591 PMID: 16920620
Jiang et al (2006) Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on DArgic neurons through a microtubule-dependent mechanism. J Neurosci 26 4318 PMID: 16624952
Ren et al (2012) Intrathecal injection of metabotropic glutamate receptor subtype 3 and 5 agonist/antagonist attenuates bone cancer pain by inhibition of spinal astrocyte activation in a mouse model. Anesthesiology 116 122 PMID: 22123524
Pasquale and Sherman (2013) A modulatory effect of the feedback from higher visual areas to V1 in the mouse. J Neurophysiol 109 2618 PMID: 23446698
Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236
Carlton et al (2009) Group II metabotropic glutamate receptor activation on peripheral nociceptors modulates TRPV1 function. J Neurosci 1248 86 PMID: 19026992
McIlwrath and Westlund (2015) Pharmacological attenuation of chronic alcoholic pancreatitis induced hypersensitivity in rats. Brain Res 21 836 PMID: 25624717
Do you know of a great paper that uses (2R,4R)-APDC from Tocris? Please let us know.
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Literature in this Area
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