(2R,4R)-APDC - CAS 169209-63-6
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
(2R,4R)-APDC is a selective and relatively potent group II mGluR agonist (EC50 = 0.4, 0.4, > 100, > 100, > 300 and > 300 μM for human mGlu2, mGlu3, mGlu1, mGlu5, mGlu4 and mGlu7 receptors, respectively). (2R,4R)-APDC is centrally active following systemic administration in vivo.
Brife Description:
group II mGluR agonist
≥98% by HPLC
Canonical SMILES:
1.The striatum as a target for anti-rigor effects of an antagonist of mGluR1, but not an agonist of group II metabotropic glutamate receptors.
Ossowska K;Konieczny J;Pilc A;Wolfarth S Brain Res. 2002 Sep 20;950(1-2):88-94.
The aim of the present study was to find out whether the metabotropic receptor 1 (mGluR1) and group II mGluRs, localized in the striatum, are involved in antiparkinsonian-like effects in rats. Haloperidol (1 mg/kg ip) induced parkinsonian-like muscle rigidity, measured as an increased resistance of a rat's hind foot to passive flexion and extension at the ankle joint. (RS)-1-aminoindan-1,5-dicarboxylic acid (AIDA; 0.5-15 microg/0.5 microl), a potent and selective mGluR1 antagonist, or (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylate (2R,4R-APDC; 7.5-15 microg/0.5 microl), a selective group II agonist, was injected bilaterally into the striatum of haloperidol-treated animals. AIDA in doses of 7.5-15 microg/0.5 microl diminished the haloperidol-induced muscle rigidity. In contrast, 2R,4R-APDC injections were ineffective. The present results may suggest that the blockade of striatal mGluR1, but not the stimulation of group II mGluRs, may ameliorate parkinsonian muscle rigidity.
2.Activation of group I mGluRs is necessary for induction of long-term depression at striatal synapses.
Sung KW;Choi S;Lovinger DM J Neurophysiol. 2001 Nov;86(5):2405-12.
Activation of metabotropic glutamate receptors (mGluRs), which are coupled to G proteins, has important roles in certain forms of synaptic plasticity including corticostriatal long-term depression (LTD). In the present study, extracellular field potential and whole cell voltage-clamp recording techniques were used to investigate the effect of mGluR antagonists with different subtype specificity on high-frequency stimulation (HFS)-induced LTD of synaptic transmission in the striatum of brain slices obtained from 15-to 25-day-old rats. Induction of LTD was prevented during exposure to the nonselective mGluR antagonist (RS)-alpha-methyl-4-carboxyphenylglycine (500 microM). The group I mGluR-selective antagonists (S)-4-carboxy-phenylglycine (50 microM) and (RS)-1-aminoindan-1,5-dicarboxylic acid (100 microM) prevented induction of LTD when applied before and during HFS. The mGluR1-selective antagonist 7-(Hydroxyimino) cyclopropa[b]chromen-1a-carboxylate ethyl ester (80 microM) also blocked LTD induction. Unexpectedly, the mGluR5-selective antagonist 2-methyl-6-(phenylethyl)-pyridine (10 microM) also prevented LTD induction. The group II mGluR antagonist LY307452 (10 microM) did not block LTD induction at corticostriatal synapses, but LY307452 was able to block transient synaptic depression induced by the group II agonist LY314593.
3.1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.
Kozikowski AP;Araldi GL;Tückmantel W;Pshenichkin S;Surina E;Wroblewski JT Bioorg Med Chem Lett. 1999 Jun 21;9(12):1721-6.
The synthesis of the 1-amino derivative of (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid (1-amino-APDC), a selective metabotropic glutamate ligand, is disclosed. This compound acts as a partial agonist of the group II mGluRs and shows pronounced neuroprotective properties in the NMDA model of cell toxicity.
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CAS 169209-63-6 (2R,4R)-APDC

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