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 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) Highly selective, non-competitive mGluR5 metabotropic glutamate receptor antagonist.
human ... GRIN2B(2904), GRM5(2915)
rat ... Grm5(24418)
M5046 (±)-α-Methyl-(4-sulfonophenyl)glycine Antagonist at Group III metabotropic glutamate receptors.
 
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).