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VU 0357121 is a positive and highly selective mGlu5Rallostericmodulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes .
mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positiveallostericmodulator, with an EC50 of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect .
VU0486321 is a compound in a class of mGlu1 positiveallostericmodulators (PAMs). VU0486321 maintains acceptable mGlu1 PAM potency, DMPK profile, CNS permeability, and mGluR selectivity.
Lu AF11205 is a mGlu5 receptor positiveallostericmodulator with activity modulatingmGlu5 receptor activity. Optimization of Lu AF11205 resulted in a series of potent fused thiazole analogs whose structures and activities were influenced by substituents and which could affect receptor function in cell lines expressing mGlu5 receptors.
VU0483605 is a potent and brain-penetrated mGlu1 receptor positiveallostericmodulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively .
NCFP is a metabotropic glutamate receptor 5 (mGlu5)positiveallostericmodulator (PAM). NCFP can be used in the study of central nervous system diseases .
VU0415374 is a positiveallostericmodulator that modulatesmGlu4 receptor activity. VU0415374 could help achieve precise light control of physiological responses. VU0415374 has high selectivity and can be used to further study the role of mGlu4 in co-expression of other mGlu receptor systems. The improved properties of VU0415374 make it an important candidate for studying mGlu4 with high precision in space and time .
TASP0433864 is a selective positiveallostericmodulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity .
VU0360172 hydrochloride is a potent and selective mGlu5 receptorpositiveallostericmodulator (PAM) with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .
JNJ-46356479 is a selective and orally bioavailable mGlu2 receptorpositiveallostericmodulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo .
VU6004909 is a blood-brain barrier penetrated mGlu1 positiveallostericmodulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positiveallostericmodulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research .
VU0418506 is a selective positiveallostericmodulator of mGlu4, with EC50 values of 68 nM and 46 nM for hmGlu4 and rmGlu4, respectively. VU0418506 exhibits antiparkinsonian activity .
THIIC (LY2607540) is a compound with anxiolytic and antidepressant potential. It is a positiveallostericmodulator of mGlu? receptors, exhibits anxiolytic and antidepressant-like activities in multiple animal models, and can also affect sleep and neurochemical changes.
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positiveallostericmodulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71) .
CBiPES hydrochloride is a mGlu2 receptorpositiveallostericmodulator (EC50: 92.8 nM). CBiPES hydrochloride attenuates stress-induced hyperthermia and PCP-induced hyperlocomotor activity. CBiPES hydrochloride can be used for research of neurological disease .
CBiPES is a potent mGlu2positiveallostericmodulator with an EC50 value of 92.8 nM. CBiPES attenuates stress-induced hyperthermia and Phencyclidine-induced hyperlocomotor activity. CBiPES can be used for research of neurological diseases .
LY487379 hydrochloride is a selective human mGluR2positiveallostericmodulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
VU0364770 is a selective and potent positiveallostericmodulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
VU0364770 hydrochloride is a selective and potent positiveallostericmodulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
VU0424465 is a potent and partial PAM (positiveallostericmodulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .
RO4988546 is a negative allostericmodulator (NAM) that targets metabotropic glutamate receptors 2 and 3 (mGlu2,mGlu3). RO4988546 can reduce the binding of [ 3h]-LY354740 at the positive binding site, while affecting the receptor's G protein coupling and intracellular signaling. RO4988546 can be used in the development of antidepressants and cognitive enhancers .
VU0360172 is a potent and selective mGlu5 receptorpositiveallostericmodulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice . VU0360172 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
LY487379 is a selective human mGluR2positiveallostericmodulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
3,3'-Difluorobenzaldazine (DFB) is a selective positiveallostericmodulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range .
JNJ-40411813 (ADX-71149) is a novel positiveallostericmodulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM. JNJ-40411813 has orally bioactivity and penetrate the blood-brain barriers. JNJ-40411813 has the potential property of anti-depression .
VU0364289 is a highly selective mGlu5positiveallostericmodulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research .
Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positiveallostericmodulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease .
VU-29 is a positiveallostericmodulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM) .
LSN2463359 is positiveallostericmodulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ro 67-4853 is a positiveallostericmodulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
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