(2R,4R)-APDC
Chemical Name: (2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylate
Purity: ≥98%
Biological Activity
(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.Technical Data
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.
Additional Information
Background References
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Sphingosine regulates the NLRP3-inflammasome and IL-1beta release from macrophages.
Luheshi NM, Giles JA, Lopez-Castejon G, Brough D
Eur. J. Immunol., 2011;42(3):716-25. -
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.
Monn et al.
J.Med.Chem., 1996;39:2990 -
Selective inhibition of forskolin-stimulated cyclic AMP formation in rat hippocampus by a novel mGluR agonist, 2R,4R-4-aminopyrrolidine-2,4-dicarboxylate.
Schoepp et al.
Neuropharmacology, 1995;34:843 -
Pharmacological agents acting at subtypes of metabotropic glutamate receptors.
Schoepp et al.
Neuropharmacology, 1999;38:1431
Product Datasheets
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Citations for (2R,4R)-APDC
The citations listed below are publications that use Tocris products. Selected citations for (2R,4R)-APDC include:
8 Citations: Showing 1 - 8
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HTS-compatible FRET-based conformational sensors clarify membrane receptor activation.
Authors: Scholler
Nat Chem Biol 2017;13(4):372
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Pharmacological attenuation of chronic alcoholic pancreatitis induced hypersensitivity in rats.
Authors: McIlwrath and Westlund
Brain Res 2015;21:836
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A modulatory effect of the feedback from higher visual areas to V1 in the mouse.
Authors: Pasquale and Sherman
J Neurophysiol 2013;109:2618
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Intrinsic modulators of auditory thalamocortical transmission.
Authors: Lee and Sherman
Hear Res 2012;287:43
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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.
Authors: Ren Et al.
Anesthesiology 2012;116:122
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Group II metabotropic glutamate receptor activation on peripheral nociceptors modulates TRPV1 function.
Authors: Carlton Et al.
J Neurosci 2009;1248:86
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Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on DArgic neurons through a microtubule-dependent mechanism.
Authors: Jiang Et al.
J Neurosci 2006;26:4318
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Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain.
Authors: Proudfoot Et al.
Curr Biol 2006;16:1591
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