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. Also available as part of the Group II mGlu Receptor Tocriset™.
Sold with the permission of Eli Lilly and Company
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 100 mM in water|
Preparing Stock Solutions
The following data is based on the product molecular weight 174.16. Batch specific molecular weights may vary from batch to batch due to solvent 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 are publications that support the products' biological activity.
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
If you know of a relevant reference for (2R,4R)-APDC, please let us know.
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Keywords: (2R,4R)-APDC, supplier, selective, group, II, agonists, Group, Receptors, mGlu2, mGlu3, mGluR2, mGluR3, Glutamate, Metabotropic, Glutamate, (Metabotropic), Group, II, Receptors, Glutamate, (Metabotropic), Group, II, Receptors, Tocris Bioscience
5 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
Carlton et al (2009) Group II metabotropic glutamate receptor activation on peripheral nociceptors modulates TRPV1 function. J Neurosci 1248 86 PMID: 19026992
Proudfoot et al (2006) Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain. Curr Biol 16 1591 PMID: 16920620
Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236
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? If so please let us know.
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