mGluR5 Agonist

DHPG is the agonist for mGluR 1/5 (EC₅₀ for mGluR 1 is 60 nM) that activates the phospholipase C (PLC) pathway, and leads ultimately to the activation of protein kinase C (PKC).

CHPG is a selective mGluR5 agonist, and attenuates SO₂-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.

ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC₅₀ of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.

CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO₂-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..

L-Cysteinesulfinic acid 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.

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.

JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC₅₀ of 260 nM.

(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with K_i values of 0.9 μM and 3.9 μM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.

VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC₅₀ value of 16 nM and a K_i 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.

DCG-IV is a potent agonist of group II mGluRs with EC₅₀s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC₅₀: mGlu1R/5R=389/630 μM) and III receptors (IC₅₀: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects.

VU0364770 is a selective and potent positive allosteric modulator (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 K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.

VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC₅₀=9 nM and K_i=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).

VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu₅ mediated iCa²⁺ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a K_i value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons.

VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a K_i of 156 nM and an EC₅₀ of 9.6 nM.

VU0364770 hydrochloride is a selective and potent positive allosteric modulator (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 K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.

VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC₅₀ value of 16 nM and a K_i of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice.

VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC₅₀ of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.

VU0092273 is a potent mGlu5 positive allosteric modulator (PAM) that also binds to the MPEP site, with an EC₅₀ of 0.27 μM.