Excitatory Amino Acids - Metabotropic Agonists

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A155 trans-(±)-ACPD monohydrate solid, ≥97% (NMR) Excitatory amino acid receptor agonist; selective for the metabotropic glutamate receptor subtype.
human ... GRM1(2911), GRM2(2912), GRM3(2913), GRM4(2914), GRM5(2915), GRM6(2916), GRM7(2917), GRM8(2918)
A7929 L-(+)-2-Amino-4-phosphonobutyric acid optical purity optical purity: ≥95% (HPLC, Marfey′s reagent) mGluR4 and mGluR6 metabotropic glutamate receptor agonist.
human ... GRM1(2911), GRM2(2912), GRM3(2913), GRM4(2914), GRM6(2916), GRM7(2917), GRM8(2918)
rat ... Grm1(24414), Grm2(24415), Grm4(24417), Grm5(24418), Grm6(24419), Grm7(81672)
A7361 2R, 4R-APDC monohydrate ≥98% (HPLC) 2R,4R-APDC is a Group II mGluR metabotropic glutamate receptor.
 
B8688 Biphenyl-indanone A ≥98% (HPLC), powder Biphenyl-indanone A (BINA) is a potent selective positive allosteric modulator for the group II metabotropic glutamate receptor subtype mGluR2. In animal studies BINA showed anxiolytic and antipsychotic effects, and blocked the effects produced by the hallucinogenic drug DOB. It decreased cocaine self-administration in rats, with no effect on food self-administration. In recombinant systems, BINA selectively potentiated the response of mGluR2 to glutamate with no effect on the glutamate response of other mGluR receptor subtypes tested.
 
SML0235 CDPPB ≥98% (HPLC) Activation of metabotropic glutamate 5 receptor by CDPPB enhances the function of NMDA receptor and markers of neuronal plasticity. This improves recognition memory and cognition deficits in schizophrenia.
CDPPB is a glutamate metabotropic mGluR5 positive allosteric modulator.
 
SML0096 Cinnabarinic Acid ≥98% (HPLC) Cinnabarinic acid is a kynurenine pathway metabolite of tryptophan, produced by the oxidation of 3-Hydroxyanthranilic acid. Cinnabarinic acid leads to loss of mitochondrial respiration and apoptosis, and has also been shown to be an mGlu4R-specific agonist.
 
D3689 (S)-3,5-Dihydroxyphenylglycine hydrate ≥98% (HPLC), powder (S)-3,5-Dihydroxyphenylglycine hydrate is a group I metabotropic glutamate receptor agonist.
human ... GRM1(2911)
L4420 LY-367385 hydrochloride ≥98% (HPLC) LY-367385 is a selective metabotropic glutamate 1a receptor (mGlu1a) antagonist.
 
P0878 O-Phospho-L-serine Group III metabotropic glutamate receptor agonist (mGluR4, mGluR7, and mGluR8).
O-Phospho-L-serine (L-SOP) is a molecule which resembles phosphatidylserine head group and it mediates partial inhibition of microglial phagocytosis of apoptotic cells. In zebrafish, L-SOP inhibits Müller glia proliferation and blocks cone cell regeneration in the light-damaged retina. In vivo, L-SOP acts as a substrate for CysM, a cysteine synthase from Mycobacterium tuberculosis.
human ... GRM4(2914), GRM7(2917), GRM8(2918)
T2455 T3MG T3MG is a selective inhibitor of excitatory amino acid transporters GLT-1, EAAT2, and EAAT4. T3MG has long been utilized as a gold standard in the study of general EAAT function. It has more recently been shown to be selective for EAAT2 and EAAT4 as compared to EAAT1 and EAAT3 in electrophysiology and glutamate/aspartate uptake assays. Although there are other EAAT2-selective compounds, this is the first tool with selectivity for EAAT4. T3MG is not a substrate for the transporters themselves, nor does it have activity at glutamate ion channels.
 
SML0019 VU0357121 ≥98% (HPLC) VU0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax. Its site of action is distinct from the classical mGlu5 negative allosteric modulator (NAM) MPEP allosteric site or the site of a recetly discovered PAM, CPPHA. However, VU0357121shares a functional interaction with the MPEP site. VU0357121 is highly selective for activation of mGlu5 and is inactive or very weakly antagonizing at other mGlu receptor subtypes.
 
W0145 WAY-213613 ≥98% (HPLC) WAY-213613 is a selective GLT-1/EAAT2 inhibitor. GLT-1, aka excitatory amino acid transporter (EAAT)2, is a glutamate transporter highly expressed in both neurons and astrocytes. Members of the EAAT family function to prevent excitotoxicity by removing glutamate from the synapse in the normal brain and may be therapeutic targets for diseases characterized by decreased glutamatergic function. WAY-213613 is a novel EAAT2 inhibitor and is more potent than the general EAAT inhibitor trans-2,4-PDC. WAY-213613 is selective for EAAT2 as compared to EAAT1 and EAAT3 in electrophysiology, glutamate uptake, and synaptosome assays. WAY-213613 is not a substrate for the transporters themselves, nor does it have activity at glutamate ionotropic or metabotropic receptors.
WAY-213613 is a selective inhibitor of the GLT-1/EAAT2 (glutamate transporter/excitatory amino acid transporter) in neurons and astrocytes. Members of the EAAT family function to moderate excitation by removing glutamate from the synapse; they may be therapeutic targets for diseases of glutamatergic function. WAY-213613 is more potent than the general EAAT inhibitor trans-2,4-PDC, and is selective for EAAT2 over EAAT1 and EAAT3 in electrophysiology, glutamate uptake, and synaptosome assays. It is neither a substrate for the transporters themselves, nor an agonist at glutamate ionotropic or metabotropic receptors.