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.
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.
SML0555   ML289 ≥98% (HPLC) ML289 (VU0463597) is a potent, selective and centrally penetrant negative allosteric modifier (NAM) of metabotropic glutamate receptor 3 (mGlu3). ML289 is >15-fold selective vs mGlu2 with an IC50 value of 0.66 μM.
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.