Excitatory Amino Acids - Metabotropic Antagonists

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A254 AIDA solid Selective mGluR1 metabotropic glutamate receptor antagonist.
human ... GRM1(2911)
rat ... Grm1(24414)
M5560 (S)-2-Amino-2-methyl-4-phosphonobutyric acid hydrochloride synthetic, solid Selective mGluR4,6,7 metabotropic glutamate receptor antagonist.
human ... GRM4(2914), GRM6(2916), GRM7(2917)
A4910 DL-2-Amino-3-phosphonopropionic acid Potent metabotropic glutamate receptor antagonist.
human ... GRM1(2911), GRM2(2912), GRM3(2913), GRM4(2914), GRM5(2915), GRM6(2916), GRM7(2917), GRM8(2918)
C9749   CBiPES hydrochloride ≥98% (HPLC) CBiPES is a positive allosteric modulator of the mGlu2 receptor. CBiPES attenuates stress-induced hyperthermia and blocks the hyperlocomotor effects of PCP in murine models. In rat brain, CBiPES attenuates ketamine-induced increase in extracellular histamine concentration. This compound is a sulfonamide, different chemical class from other mGlu2R agonists in the Sigma catalog.
 
C2247 CPPHA ≥98% (HPLC) CPPHA is a selective positive allosteric modulator of mGluR5 receptor. It has no agonist activity alone, but reduces threshold response and shifts dose-response curves to glutamate, quisqualate, and DHPG by 4- to 7-fold to the left in recombinant CHO cells expressing human or rat mGluR5.
 
M196 (+)-α-Methyl-4-carboxyphenylglycine solid (+)-α-Methyl-4-carboxyphenylglycine, also known as MCPG, is a competitive metabotropic glutamate receptor antagonist.
rat ... Grm1(24414)
M4796 (±)-α-Methyl-(4-carboxyphenyl)glycine Competitive antagonist at Group 1 (mGluR1 and mGluR5) and Group 2 (mGluR2 and mGluR3) metabotropic glutamate receptors.
human ... GRM1(2911), GRM2(2912), GRM3(2913), GRM5(2915)
rat ... Grm1(24414)
M5435 6-Methyl-2-(phenylethynyl)pyridine hydrochloride ≥98% (HPLC) GRIN2B (glutamate ionotropic receptor NMDA type subunit 2B) plays an important role in the growth of neurons and is highly essential for learning and memory. GRIN2B mutation is associated with neuropsychiatric and developmental disorders like schizophrenia, Parkinson′s disease and bipolar disorder. MPEP (2-methyl-6-(phenylethynyl)pyridine hydrochloride) is used to treat Alzheimer′s disease (AD).
Highly selective, non-competitive mGluR5 metabotropic glutamate receptor antagonist.
human ... GRIN2B(2904), GRM5(2915)
rat ... Grm5(24418)
M3074 MMPIP ≥98% (HPLC) MMPIP is a potent, selective, allosteric antagonist of metabotropic glutamate receptor 7 (mGluR7). It also displays intrinsic activity and acts as an inverse agonist.
 
M4699 MTEP hydrochloride ≥98% (HPLC) MTEP is a potent and highly selective antagonist for mGluR5.
 
S9186 SIB 1757 ≥99% (HPLC), crystalline SIB 1757 is a highly selective mGluR5 metabotropic glutamate receptor antagonist. It non-competitively inhibits glutamate-induced increase in Ca2+ at human metabotropic glutamate receptor 1 (hmGluR1).1 Inhibition of mGlu5 receptor renders protection to neurons2 against methamphetamine-induced oxidative damage.3
human ... GRM1(2911), GRM5(2915)
S9311 SIB 1893 >99%, solid SIB 1893 non-competitively inhibits glutamate-induced increase in Ca2+ at human metabotropic glutamate receptor 1 (hmGluR1).1 It also acts as a positive allosteric modulator of hmGluR4.2
Selective and noncompetitive mGlu5 metabotropic glutamate receptor antagonist.
human ... GRM1(2911), GRM5(2915)
Y1271 YM-202074 sesquifumarate salt hydrate ≥98% (HPLC) YM-202074 is a potent and selective allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist. It bound an allosteric site of rat mGluR1 with a Ki value of 4.8 nM. It also inhibited the mGluR1-mediated inositol phosphates production in rat cerebellar granule cells with an IC50 value of 8.6 nM, while showing selectivity over mGluR(2-7).