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.
M196 (+)-α-Methyl-4-carboxyphenylglycine solid (+)-α-Methyl-4-carboxyphenylglycine, also known as MCPG, is a 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) 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.
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.
SML0818   A-841720 ≥98% (HPLC) A-841720 is a potent, selective, non-competitive mGluR1 antagonist that displays greater than 30-fold selectivity over another Group I metabotopic glutamate receptor, mGluR5. The compound has potent analgesic properties, and can also diminish motor and cognitive activity.
A254 AIDA solid Selective mGluR1 metabotropic glutamate receptor antagonist.
SML1764 AZD9272 ≥98% (HPLC) AZD9272 is a long acting, CNS penetrant, potent and selective mGluR5 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.
SML1124 CPCCOEt ≥98% (HPLC) CPCCOEt is a selective non-competitive metabotropic glutamate receptor mGluR1 antagonist with no agonist or antagonist activity at mGlu2, 4a, 5a, 7b, 8a or ionotropic receptors at concentrations of up to 100 μM.
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.
PZ0293 GRN-529 ≥97% (HPLC) GRN-529 is a brain penetrant, potent and selective negative allosteric modulator of the mGluR5 receptor (metabotropic glutamate receptor subtype 5) with an IC50 of 3.1 nM and >1000-fold selectivity vs mGluR1. GRN-529 was shown to alleviate multiple diagnostic behavioral symptoms of autism in BTBR and C58 mice models.
SML0665   LY-456236 ≥98% (HPLC) LY-456236 is a selective mGlu1 receptor antagonist with an IC50 value of 143 nM for mGlu1 compared to > 10 μM for mGlu5 receptors.
SML1273 ML347 ≥98% (HPLC) ML347 is a derivative of dorsomorphin that is a highly selective antagonist of BMP receptor isotypes ALK1 and ALK2 (IC50 values = 46 and 32 nM, respectively). ML347 has little effect on other ALK isoforms, including ALK3 (IC50 = 10 μM).
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.
PZ0219 PF-06297470 ≥98% (HPLC) PF-06297470 is a potent negative allosteric modulator of the Metabotropic Glutamate Receptor 5 (mGluR5). PF-06297470 binds to mGluR5 with a Ki of 0.9 nM. The compound PF-06297470 displays slight antagonism of mGluR1 (IC50 = 30.5 mM), with no agonist or antagonist activities against any other mGlu receptor subtype at concentrations up to 50 mM. PF-06297470 reduces dyskinesia in a rodent (MPTP)-rendered Parkinsonian model of L-DOPA-induced dyskinesia (PD-LID).
PZ0334 PF-06422913 ≥98% (HPLC) PF-06422913 is an orally active, potent and selective metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
PZ0231 PF-06462894 ≥98% (HPLC) PF-06462894 is a muscarinic metabotropic receptor mGluR5 ligand.
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
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.
SML1799 UCPH-102 ≥98% (HPLC) UCPH-102 is a selective inhibitor of the Excitatory Amino Acid Transporter subtype-1 (EAAT1, GLAST) with an IC50 value of 420 nM for EAAT1 and >300 μM for EAAT2-5. UCPH-102 has been shown to cross the blood-brain barrier, so should become a valuable tool for studying the role of EAAT1 in brain.
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) 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.