Ro 67-4853

Ro 67-4853 is a positive allosteric modulator (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[1][2][3][4].

Product Specifications

CAS Number

[302841-89-0]

UNSPSC

12352005

Hazard Statement

H302, H361, H372, H410

Target

MGluR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ro-67-4853.html

Purity

99.90

Solubility

DMF : 16 mg/mL (ultrasonic; warming)

Smiles

CCCCOC(NC(C1C2=CC=CC=C2OC3=CC=CC=C13)=O)=O

Molecular Formula

C19H19NO4

Molecular Weight

325.36

Precautions

H302, H361, H372, H410

References & Citations

[1]Knoflach F, et al. Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site [published correction appears in Proc Natl Acad Sci U S A 2001 Dec 18;98 (26) :15393]. Proc Natl Acad Sci U S A. 2001;98 (23) :13402-13407. |[2]Jiang JY, et al. Extracellular calcium modulates actions of orthosteric and allosteric ligands on metabotropic glutamate receptor 1α. J Biol Chem. 2014;289 (3) :1649-1661.|[3]Salt TE, et al. Potentiation of sensory responses in ventrobasal thalamus in vivo via selective modulation of mGlu1 receptors with a positive allosteric modulator. Neuropharmacology. 2012;62 (4) :1695-1699. |[4]Sheffler DJ, et al. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology. 2008;55 (4) :419-427.