mGluR
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB12757 | YM 202074 | 299900-83-7 | YM-202074 is a high affinity, selective metabotropic glutamate receptor type 1 (mGlu1) antagonist. YM-202074 binds an allosteric site of the rat mGlu1 receptor with a Ki of 4.8 nM. It inhibits mGlu1-mediated inositol phosphates production (IC50 = 8.6 nM in rat cerebellar granule cells). |
| FB12737 | XAP 044 | 196928-50-4 | XAP044 is a potent and selective mGlu7 antagonist (IC50 = 88 nM). It inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice. XAP044 displays no effects on the LTP of mGlu7 deficient mice. |
| FB15536 | VU6005649 | 2137047-43-7 | VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively. |
| FB12735 | VU 0422288 | 1630936-95-6 | VU0422288, also known as ML 396, is a positive allosteric modulator (EC50 values are 108, 125 and 146 nM for mGlu4, mGlu8 and mGlu7 respectively). |
| FB12736 | VU 0409106 | 1276617-62-9 | VU0409106 is a potent and selective inhibitor of mGlu5. |
| FB12750 | VU 0469650 | 1443748-47-7 | VU 0469650 hydrochloride is a potent and selective negative allosteric modulator of mGlu1 (IC50 = 99 nM). VU 0469650 hydrochloride exhibits >100-fold selectivity for mGlu1 over mGlu2-8 and 68 other GPCRs, ion channels, kinases and transporters. |
| FB12753 | VU 0469650 HCl | N/A | VU 0469650 hydrochloride is a potent and selective negative allosteric modulator of mGlu1 (IC50 = 99 nM). VU 0469650 hydrochloride exhibits >100-fold selectivity for mGlu1 over mGlu2-8 and 68 other GPCRs, ion channels, kinases and transporters. |
| FB12759 | VU 0155041 | 1093757-42-6 | UV0155041 is a potent, positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively). |
| FB12686 | TASP 0433864 | 1431980-60-7 | TASP0433864 is a novel positive allosteric modulator of metabotropic glutamate 2 receptor. TASP0433864 exhibited PAM activity at human and rat mGlu2 receptors with EC50 values of 199 and 206 nM, respectively, without exerting agonist activity at rat mGlu2 receptor. TASP0433864 produced a leftward and upward shift in the concentration-response curve of glutamate-increased guanosine 5'-O-(3-[(35)S]thio)triphosphate binding to mGlu2 receptor. The inhibitory effect of TASP0433864 on cortical activation was also observed in the mouse 2-deoxy-glucose uptake study. TASP0433864 is a selective mGlu2 receptor PAM with antipsychotic activity, and the attenuation of excess glutamatergic neurotransmission may be involved in the action of TASP0433864. |
| FB12389 | Spaglumic Acid | 3106-85-2 | Spaglumic Acid is a neuropeptide found in millimolar concentrations in brain. |
| FB12661 | SIB 1757 | 31993-01-8 | SIB-1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype. SIB-1757 displays an IC50 value of 0.4 μM at hmGlu5 compared with > 30 μM at hmGlu1b, hmGlu2, hmGlu4, hmGlu6, hmGlu7 and hmGlu8. |
| FB12738 | YM 230888 | 446257-23-4 | Selective mGlu1 antagonist |
| FB12641 | Ro 64-5229 | 246852-46-0 | Ro64-5229 is a selective, non-competitive mGlu2 antagonist. Ro64-5229 inhibits GTPγ35S binding to mGlu2-containing membranes (IC50 = 0.11 μM). |
| FB12438 | VU 29 | 890764-36-0 | Potent positive allosteric modulator of mGlu5 receptors |
| FB12752 | VU 0155041 Sodium Salt | 1259372-69-4 | Potent positive allosteric modulator of mGlu4 receptors; sodium salt of VU 0155041 (Cat. No. 3248) |
| FB12714 | TC-N 22A | 1314140-00-5 | Potent and selective positive allosteric modulator of mGlu4 receptors |
| FB12497 | NPS 2390 | 226878-01-9 | NPS 2390 is a Group I mGlu antagonist. |
| FB20328 | L-Cysteinesulfinic acid | 1115-65-7 | NMDA and mGlu agonist. |
| FB12382 | MMPEP | 823198-78-3 | MPEP HCl is both a selective non-competitive mGlu5 receptor antagonist with IC50 value of 36 nM, and a mGlu4 receptor positive allosteric modulator. |
| FB12455 | MNI 137 | 946619-21-2 | MNI 137 is a selective negative allosteric modulator of group II mGlu receptors. |
| FB12472 | MMPIP | 479077-02-6 | MMPIP HCl is an allosteric mGlu7-selective receptor antagonist. |
| FB12463 | MMPIP HCl | 1215566-78-1 | MMPIP HCl is a 5-HT2C receptor antagonist. |
| FB12459 | ML 337 | 1443118-44-2 | ML 337 is a selective negative allosteric modulator of mGlu3 with IC50 of 593 nM. |
| FB12479 | ML 289 | 1382481-79-9 | ML 289 is a selective negative allosteric modulator at mGlu3 receptors with IC50 of 660 nM. |
| FB06794 | Mavoglurant | 543906-09-8 | Mavoglurant is a structurally non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5. |
| FB12406 | MAP4 | 157381-42-5 | MAP4 is a potent group II mGlu agonist and also group III mGlu antagonist. |
| FB04002 | LY354740 | 176199-48-7 | LY354740 is a highly potent, efficacious and selective group II (mGlu2/3) receptor agonist, produces > 90% suppression of forskolin-stimulated cAMP formation with an EC50 of 5.1 ± 0.3 nM. |
| FB16788 | LY 2140023 | 635318-55-7 | LY-404,039 is a highly selective and potent agonist of mGlu2 and mGlu3 receptors with Ki values of 149nM and 92nM, respectively. |
| FB12429 | LY 2389575 HCl | 885104-09-6 | LY 2389575 HCl is a selective negative allosteric modulator of mGlu3 with IC50 of 190 nM. |
| FB17767 | L-Cysteinesulfinic acid monohydrate | 207121-48-0 | L-Cysteinesulfinic acid monohydrate is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively. |
| FB12524 | L-CCG-l | 117857-93-9 | L-CCG-l is a potent group II metabotropic glutamate receptor agonist. |
| FB09934 | IEM 1754 Dihydrobromide | 162831-31-4 | IEM 1754 dihydrobromide is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM. |
| FB12748 | YM 202074 fumarate salt | 299900-84-8 | High affinity, selective mGlu1 antagonist |
| FB12341 | HexylHIBO | 334887-43-3 | HexylHIBO is a Group I mGlu receptor antagonist with Kis of 140 and 110 μM at mGlu1a and mGlu5a receptors respectively. |
| FB12436 | H-Ser(PO3H2)-OH | 407-41-0 | H-Ser(PO3H2)-OH is both a Group III metabotropic glutamate receptor (mGluR4, mGluR7, and mGluR8) agonist, and a competitive NMDA antagonist. |
| FB12311 | FTIDC | 873551-53-2 | FTIDC is a potent and selective mGlu1 receptor negative allosteric modulator with IC50 of 5.8 nM. |
| FB15529 | Foliglurax | 1883329-51-8 | Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM[1]. Antiparkinsonian effect[1]. |
| FB12294 | DL-AP3 | 5652-28-8 | DL-AP3 is a competitive group I metabotropic glutamate receptor antagonist and inhibitor of phosphoserine phosphatase. |
| FB12575 | CPPG | 183364-82-1 | CPPG is a potent group II/III mGlu receptor antagonist, with IC50s of 46.2 and 2.2 nM respectively. |
| FB12521 | CPCCOEt | 179067-99-3 | CPCCOEt is a hmGlu1 subtype-selective non-competitive antagonist with IC50 of 6.5 μM. |
| FB12512 | Cinnabarinic Acid | 606-59-7 | Cinnabarinic Acid is a elective mGlu4 agonist. |
| FB12315 | CHPG Sodium Salt | 1303993-73-8 | CHPG Sodium Salt is a selective mGlu5 agonist. |
| FB12267 | CHPG | 170846-74-9 | CHPG is a selective mGlu5 metabotropic glutamate receptor agonist. |
| FB17651 | AZD-8529 mesylate | 1314217-69-0 | AZD-8529 is a a positive allosteric modulator at the mGluR2 receptor. AZD8529 decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. AZD8529 potentiated agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus, and striatum. In monkeys, AZD8529 decreased nicotine self-administration at doses (.3-3 mg/kg) that did not affect food self-administration. AZD8529 also reduced nicotine priming- and cue-induced reinstatement of nicotine seeking after extinction of the drug-reinforced responding. In rats, AZD8529 decreased nicotine-induced accumbens dopamine release. The positive allosteric modulators of metabotropic glutamate receptor 2 should be considered for relapse prevention. |
| FB12275 | AZD 9272 | 327056-26-8 | AZD 9272 is a potent and selective mGlu5 antagonist with IC50s of 2.6 and 7.6 nM for rat and human receptors, respectively. |
| FB12208 | AZD 2066 | 934282-55-0 | AZD 2066 is an orally bioavailable and brain penetrant mGlu5 antagonist. |
| FB12184 | ACPT-I | 194918-76-8 | ACPT-I is an agonist for group III mGlu receptors with EC50 of 7.2 and 8.2 μM for mGlu4a and mGlu8 respectively. |
| FB12345 | ACDPP HCl | N/A | ACDPP HCl is the hydrochloride form of ACDPP. ACDPP is a modest mGlu5 receptor antagonist. |
| FB12271 | ABP 688 | 924298-51-1 | ABP 688 is a high affinity human mGlu5 receptor antagonist with Ki of 1.7 nM. |
| FB12570 | 3-MATIDA | 518357-51-2 | 3-MATIDA is a potent metabotropic glutamate mGlu1 receptor antagonist with IC50 of 6.3 μM at rat mGlu1a. |