2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. mGluR
  5. mGluR1 Isoform
  6. mGluR1 Antagonist

mGluR1 Antagonist

mGluR1 Antagonists (18):

Cat. No. Product Name Effect Purity
  • HY-70059
    LY341495
    		Antagonist 99.50%
    LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC50s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively.
  • HY-100407
    JNJ16259685
    		Antagonist 98.66%
    JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
  • HY-124406
    A-794282
    		Antagonist
    A-794282 is an antagonist with analgesic activity, selectively targeting to mGlu1 receptor that significantly reduces pain behaviors in a postoperative pain model, but motor side effects may occur at higher doses.
  • HY-107510
    YM-230888
    		Antagonist
    YM-230888 is an orally active, selective and allosteric mGlu1 receptor antagonist with a Ki of 13 nM. YM-230888 inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 13 nM. YM-230888 shows antinociceptive response in Streptozotocin (HY-13753)-induced hyperalgesia models. YM-230888 significantly reduces pain parameters in complete Freund's adjuvant (HY-153808)-induced arthritic pain models.
  • HY-103556
    YM-202074 fumarate
    		Antagonist
    YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity and neuroprotective properties in vivo. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki value of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 value of 8.6 nM. YM-202074 fumarate can be used in stroke research.
  • HY-11095
    NPS 2390
    		Antagonist 98.83%
    NPS 2390 is a noncompetitive antagonist of mGluR1 and mGluR5. NPS 2390 is also a potent CaSR (calcium-sensing receptor) inhibitor.
  • HY-107515A
    LY367385 hydrochloride
    		Antagonist 99.44%
    LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects.
  • HY-100786
    DL-AP3
    		Antagonist ≥98.0%
    DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect.
  • HY-101311
    UPF-523
    		Antagonist 99.89%
    UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis.
  • HY-101356
    CPCCOEt
    		Antagonist 98.31%
    CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b).
  • HY-103568
    YM-298198 hydrochloride
    		Antagonist 99.61%
    YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders.
  • HY-100382
    FPTQ
    		Antagonist 99.92%
    FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.
  • HY-100402
    CFMTI
    		Antagonist ≥98.0%
    CFMTI inhibits L-glutamate-induced intracellular Ca2+ mobilization in CHO cells expressing human and rat mGluR1a, with IC50s of 2.6 and 2.3 nM, respectively.
  • HY-136587
    Oxomemazine
    		Antagonist 99.18%
    Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment.
  • HY-107515
    LY367385
    		Antagonist ≥99.0%
    LY367385 is a highly selective and potent mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.
  • HY-103550
    A-841720
    		Antagonist ≥98.0%
    A-841720 is a potent, non-competitive and selective mGlu1 receptor antagonist with an IC50 of 10 nM for human mGlu1 receptor. A-841720 displays 34-fold selectivity over mGlu5 (IC50 of 342 nM), and no significant activity at a range of other neurotransmitter receptors, ion channels, and transporters. A-841720 has the potential for chronic pain research.
  • HY-107513
    BAY 36-7620
    		Antagonist
    BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research.
  • HY-100840A
    (RS)-4C3HPG
    		Antagonist
    (RS)-4C3HPG (4-Carboxy-3-hydroxyphenylglycine) is an effective competitive antagonist at the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system, and it is also an agonist at mGluR2/3. (RS)-4C3HPG exhibits neuroprotective effects in an acute global ischemia rat model.