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mGluR

mGluR

货号 产品名 CAS号 信息
CSN23268 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).
CSN23198 XAP044 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.
CSN26264 Xanthurenic acid 59-00-7 Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus, which activates mGlu2/3 metabotropic glutamate receptors (mGlu2 and mGlu3).
CSN23892 VU6012962 2313526-86-0 VU6012962 is a CNS-penetrant metabotropic glutamate receptor 7 (mGlu7) negative allosteric modulator (NAM) with an IC50 of 347 nM.
CSN24066 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.
CSN23184 VU0422288 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).
CSN23183 VU0409106 1276617-62-9 VU0409106 is a potent and selective inhibitor of mGlu5.
CSN83995 VU0364289 1242443-29-3 VU0364289 is a novel N-aryl piperaxine mGlu5 positive allosteric modulator.
CSN23186 VU0469650 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.
CSN23267 (R)-3-(4-(Adamantane-1-carbonyl)-3-methylpiperazin-1-yl)picolinonitrile hydrochloride 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.
CSN23181 VU0155041 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).
CSN26379 TCN238 125404-04-8 TCN238 is a orally available and brain penetrant positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.
CSN23141 TASP0433864 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.
CSN23124 Spaglumic Acid 3106-85-2 Spaglumic Acid is a neuropeptide found in millimolar concentrations in brain.
CSN23116 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.
CSN23203 YM 230888 446257-23-4 Selective mGlu1 antagonist
CSN23070 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).
CSN23187 VU-29 890764-36-0 Potent positive allosteric modulator of mGlu5 receptors
CSN23182 VU0155041 sodium 1259372-69-4 Potent positive allosteric modulator of mGlu4 receptors; sodium salt of VU 0155041 (Cat. No. 3248)
CSN23155 TC-N 22A 1314140-00-5 Potent and selective positive allosteric modulator of mGlu4 receptors
CSN18031 PHCCC 179068-02-1 PHCCC is a Group I metabotropic glutamate receptor antagonist with EC 50 of 6 μM and a positive allosteric modulator of mGluR4.
CSN23007 NPS 2390 226878-01-9 NPS 2390 is a Group I mGlu antagonist.
CSN26699 NPEC-caged-LY379268 1315379-62-4 NPEC-caged-LY379268 is a type II mGluR agonist[1].
CSN29465 L-Cysteinesulfinic acid 1115-65-7 NMDA and mGlu agonist.
CSN22913 2-((3-Methoxyphenyl)ethynyl)-6-methylpyridine hydrochloride 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.
CSN22984 MNI137 946619-21-2 MNI 137 is a selective negative allosteric modulator of group II mGlu receptors.
CSN23218 MMPIP 479077-02-6 MMPIP HCl is an allosteric mGlu7-selective receptor antagonist.
CSN22982 MMPIP HCl 1215566-78-1 MMPIP HCl is a 5-HT2C receptor antagonist.
CSN22978 ML337 1443118-44-2 ML 337 is a selective negative allosteric modulator of mGlu3 with IC50 of 593 nM.
CSN22977 ML289 1382481-79-9 ML 289 is a selective negative allosteric modulator at mGlu3 receptors with IC50 of 660 nM.
CSN13469 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.
CSN22960 MAP4 157381-42-5 MAP4 is a potent group II mGlu agonist and also group III mGlu antagonist.
CSN18024 Eglumegad 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.
CSN25583 Pomaglumetad methionil anhydrous 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.
CSN22952 LY2389575 hydrochloride 885104-09-6 LY 2389575 HCl is a selective negative allosteric modulator of mGlu3 with IC50 of 190 nM.
CSN22065 Lu AF21934 1445605-23-1 Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with IC50 of 500 nM for human mGlu4.
CSN27529 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.
CSN18792 IEM-1754 162831-31-4 IEM 1754 dihydrobromide is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
CSN23202 YM 202074 fumarate salt 299900-84-8 High affinity, selective mGlu1 antagonist
CSN23016 L-O-Phosphoserine 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.
CSN24075 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].
CSN26363 FITM 932737-65-0 FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
CSN18005 E4CPG 170846-89-6 E4CPG is a group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .
CSN27612 CDPPB 781652-57-1 CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5.
CSN26700 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.
CSN22665 ACDPP hydrochloride N/A ACDPP HCl is the hydrochloride form of ACDPP. ACDPP is a modest mGlu5 receptor antagonist.
CSN24484 (S)-4CPG 134052-73-6 (S)-4CPG is a selective competitive group I mGlu antagonist.
CSN32737 Decoglurant 911115-16-7
CSN42041 UBP316 936095-50-0
CSN43844 HTL14242 1644645-32-8
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