mglu5

CHPG sodium salt is a selective agonist of mGluR5 that activates ERK and Akt signaling pathways and is utilized in studies on traumatic brain injury.

CHPG hydrochloride is a selective agonist of mGluR5.

Methoxy-PEPy is a potent and selective mGlu5 receptor inhibitor, exhibiting an IC50 value of 1 nM.

JNJ-46778212 (VU 0409551) is a potent and selective mGlu5 allosteric modulator (EC50: 260 nM) used for neurodissection studies.

CHPG is a selective mGluR5 agonist that reduces LDH release and neuronal apoptosis, activates the ERK and Akt pathways, and protects against traumatic brain injury. It also increases the number of differentiated human OPCs and alleviates LPS-induced inflammation.

Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM).

VU0364770 hydrochloride is a potent and selective mGlu4 positive allosteric modulator (PAM) (EC50s: 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively).

VU0652835 is a negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGlu5) (IC50: 81 nM).

(R)-ADX-47273 is a potent positive allosteric modulator of mGluR5, with an EC50 of 168 nM for potentiation.

VU-1545 is mGlu5 positive allosteric modulator.

LSN2463359 is a positive allosteric modulators of the mGlu5 receptor.

VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM).

ML353 (VU0478006) is a selective activator of TREK-1 and TREK-2 and a selective ligand (Ki =18.2 nM) for the mGlu5 Silencing Allosteric Modulator (SAM). ML353 has potential as a solution to the intrinsic activity or pharmacological blockade of SAM in vivo.

VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

ADX-47273 (BA 94673139) is a positive and selective allosteric modulator for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).

VU0092273 is a positive allosteric modulator of mGlu5 that binds to the MPEP site, with an EC50 value of 0.27 μM.

MPEP hydrochloride is an effective and highly specific non-competitive antagonist at the mGlu5 receptor subtype (IC50: 36 nM).

VU0364289 is a positive allosteric modulator of mGlu5.

VU0409106 is a potent and highly selective mGlu5 negative allosteric modulator with an IC₅₀ of 24 nM. It exhibits concentration-dependent anxiolytic effects in mouse models and can penetrate the blood–brain barrier.

FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompetitive manner and displays IC50 val

CTEP (RO 4956371) (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.

MTEP hydrochloride (MTEP) is non-competitive mGlu5 antagonist (IC50 and Ki of 5 nM and 16 nM, respectively)

SIB-1757 (6-methyl-2-[(E)-phenyldiazenyl]pyridin-3) is a selective antagonist of mGlu5 metabotropic glutamate receptor subtype (hmGlu5, IC50 : 0.4 μM)

HexylHIBO is a type I mGluR antagonist that inhibits mGlu1a and mGlu5a, with Kb values of 140 and 110 μM, respectively.HexylHIBO decreases sEPSC in rats.