Metabotropic Antagonists

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M4796 (±)-α-Methyl-(4-carboxyphenyl)glycine Competitive antagonist at Group 1 (mGluR1 and mGluR5) and Group 2 (mGluR2 and mGluR3) metabotropic glutamate receptors.
M5046 (±)-α-Methyl-(4-sulfonophenyl)glycine Antagonist at Group III metabotropic glutamate receptors.
M196 (+)-α-Methyl-4-carboxyphenylglycine solid Competitive metabotropic glutamate receptor antagonist.
M5560 (S)-2-Amino-2-methyl-4-phosphonobutyric acid hydrochloride synthetic, solid Selective mGluR4,6,7 metabotropic glutamate receptor antagonist.
M5435 6-Methyl-2-(phenylethynyl)pyridine hydrochloride ≥98% (HPLC) Highly selective, non-competitive mGluR5 metabotropic glutamate receptor antagonist.
A4910 DL-2-Amino-3-phosphonopropionic acid Potent metabotropic glutamate receptor antagonist.
A154 L-(+)-2-Amino-3-phosphonopropionic acid Potent antagonist at metabotropic glutamic acid receptors.
A254 AIDA solid Selective mGluR1 metabotropic glutamate receptor antagonist.
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.
SML0258 CPPG ≥98% (HPLC) CPPG is a potent group II/III metabotropic glutamate receptor antagonist, with approximately 20-fold selectivity for mGlu group III over group II (IC50 values of 2.2 and 46.2 nM respectively).
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.
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 Highly selective mGluR5 metabotropic glutamate receptor antagonist.
S9311 SIB 1893 >99%, solid Selective and noncompetitive mGlu5 metabotropic glutamate receptor antagonist.
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).
SML0574 YM-298198 hydrochloride ≥98% (HPLC) New YM-298198 is an orally active, noncompetitive mGlu1 receptor antagonist. The compound inhibits glutamate-induced inositol phosphate production in NIH3T3 cells (IC50 = 16 nM). YM-298198 displays analgesic and antinociceptive properties in vivo.